Selleck Chemicals - Leading Supplier of Bioactive Screening Libraries and FDA-Approved Inhibitors

About Us Selleck Chemicals
Sellecks Bioactive Screening Libraries consist of over 2,500

small molecules with validated biological and pharmacological
activities. The safety and effectiveness of these molecules has
been demonstrated through preclinical and clinical research,
and many of themare FDA-approved compounds.
Selleck Chemicals supplies over 3,000 inhibitors used in the
study of cell signaling pathways. We actively tracks the latest
science so our customers can rely on us to be the leading
supplier of the newest inhibitors.
Selleck is a Licensed Supplier of Pfizer Compounds
All bioactive compounds are licensed by Pfizer and have been marketed and/or have been clinically
demonstrated to be safe and efficacious in humans
These compounds span a range of potential uses: fromanti-cancer compounds (e.g. Bosutinib) to a
glycylcycline antiobiotic (Tigecycline) to combat the growing prevalence of antibiotic resistance
Reliability Guarantee: all Pfizer licensedcompounds are developed, and validated by Pfizer, and some
even manufactured by Pfizer
Quality Assurance: all compounds are validated using NMR and HPLC
Detailed preclinical research data and safety information available
In 2013, Selleck became a licensed supplier of Pfizer pharmaceuticals. This has granted
our customers access to Pfizers exclusive and high quality compounds. Purchased
individually or as a library, these compounds have a wide range of applications in preclinical
research of human diseases.
Inhibitors
PI3K/Akt/mTOR
ProteinTyrosine Kinase
Cell Cycle
Epigenetics
Others
MAPK
Apoptosis
For Selleck customers located in Boston and Houston, we offer same day rush courier service
as an option.
For other U.S. based customers, we guarantee that over 90% of orders placed by 2:30 p.m.
(U.S. CST) will arrive the next day before 10:30 a.m (U.S. local time).
Selleck Chemicals has an established network of sophisticated warehouse systems in
Europe, and Asia. No matter where you are located across the globe, if your purchased items
are in stock, Selleck will initiate the shipping process within 24 hours.
Quick Delivery:
At Selleck Chemicals, we have a professional expert team dedicated to ensuring our customers
are completely satisfied with their purchase. Dont hesitate to contact us by phone or email.
Phone: (832) 582-8158 x3
E-mail: tech@selleckchem.com(We strive to reply to all email inquiries within one business day)
Techical Support:
The quality of our products is strictly monitored and controlled. In the first ten months of 2013,
610 scientific articles referenced Selleck products in their work. Among them, 11 were published in
top-notch scientific journals (IF>30):
Quality & Validation:
Our Product Portfolio
Why is Selleck Your Best Choice Compared to Other Suppliers?
Nature, 2013, 500(7461): 222-6. Nature, 2013, 498(7452): 109-12. Nature, 2013, 501(7466): 237-41.
Nature, 2013, 496(7446): 523-7. Nature, 2013, 493(7430): 51-5. Nat Genet, 2013, 45(9): 1013-20.
Cell, 2013, 154(5): 1036-46. Cell, 2013, 153(4): 840-54. Science, 2013, 339(6120): 700-4.
Nat Biotechnol, 2013, 31(7): 630-7. Nat Biotechnol, 2013, 31(10): 898-907.
Table of Contents
PI3K
mTOR
Akt
GSK-3
ATM/ATR
PDK-1
S6 Kinase
AMPK (AMP-activated Protein Kinase)
DNA-PK
1
6
9
11
12
13
13
14
14
VEGFR
EGFR
PDGFR
c-Met
HER2
IGF-1R
FLT3(Fms-like Tyrosine Kinase)
FGFR
c-Kit
ALK (Anaplastic Lymphoma Kinase, CD246)
Tie-2
c-RET
Trk Receptor (Tropomyosin Receptor Kinase Receptor)
Ephrin Receptor
Axl (AXL Receptor Tyrosine Kinase)
CSF-1R (Colony stimulating factor 1 receptor)
15
22
26
28
30
31
32
33
34
35
36
36
36
36
37
37
PI3K/Akt/mTOR
Protein Tyrosine Kinase
VEGFR
J AK
EGFR
PDGFR
HER2
FLT3(Fms-like Tyrosine Kinase)
FGFR
ALK (Anaplastic Lymphoma Kinase, CD246)
HIF
VDA (Vascular-targetingAgent)
Bcr-Abl
Src
Syk(SpleenTyrosine Kinase)
FAK
BTK (Bruton's Tyrosine Kinase)
38
38
38
38
38
38
38
38
39
39
39
41
41
42
42
Angiogenesis
c-RET
Bcl-2
Caspase
p53
TNF-alpha
Mdm2
Survivin
IAP (Inhibitor of apoptosis protein)
43
43
45
45
45
46
46
46
Apoptosis
EGFR
J AK
STAT
Pim(Proto-oncogene Serine/threonine-protein Kinase)
47
47
50
50
JAK/STAT
MEK
Raf
p38 MAPK
J NK
ERK
51
54
55
57
57
MAPK
Akt
Bcr-Abl
FAK
Wnt/beta-catenin
PKC
Rac(Ras-related C3 botulinumtoxin substrate)
HSP (e.g. HSP90)
Kinesin
Microtubule Associated
PAK (p21 activated kinases)
Dynamin
Integrin
58
58
58
58
59
60
60
62
62
63
63
63
Cytoskeletal Signaling
Rac(Ras-related C3 botulinumtoxin substrate)
CDK
Aurora Kinase
Chk
ROCK
PLK
APC
Wee1
c-Myc
64
64
68
71
71
72
73
73
73
Cell Cycle
GSK-3
J AK
STAT
TGF-beta/Smad
ROCK
Wnt/beta-catenin
Gamma-secretase
Hedgehog/Smoothened
87
87
87
87
87
87
88
89
Stem Cells and Wnt
Proteasome
DUB
E1 Activating
Autophagy
E2 conjugating
E3 Ligase
91
91
92
92
94
94
Ubiquitin
85
86
DNA Methyltransferase
Histone Methyltransferase
PARP
Pim(Proto-oncogene Serine/threonine-protein Kinase)
Aurora Kinase
J AK
HIF
Sirtuin
HDAC
Histone Demethylases
Histone Acetyltransferase
Epigenetic Reader Domain
82
82
82
82
82
82
82
85
85
85
Epigenetics
Bcr-Abl
PKC
ROCK
TGF-beta/Smad
74
74
74
74
TGF-beta/Smad
HDAC
ATM/ATR
DNA-PK
PARP
DNA/RNA Synthesis
Sirtuin
Topoisomerase
Telomerase
76
76
76
76
78
80
80
81
DNA Damage
Gamma-secretase
Beta Amyloid
5-HT Receptor
COX
GluR
Adrenergic Receptor
AChR
Histamine Receptor
Dopamine Receptor
Opioid Receptor
GABA Receptor
P-gp(Permeability Glycoprotein)
P2 Receptor
OX Receptor (Orexin Receptor)
MT Receptor (Melatonin Receptor)
BACE (Beta-secretase)
95
95
95
96
97
97
98
98
99
99
99
100
100
100
100
100
Neuronal Signaling
HDAC
NF-B
IB/IKK (IB/IB Kinase)
NOD1(Nucleotide-bindingOligomerizationDomain-containingProtein1)
101
101
101
101
NF-B
104
104
104
Protease-activated Receptor
Vasopressin Receptor
CaSR (Calcium-sensing Receptor)
5-HT Receptor
Adrenergic Receptor
Histamine Receptor
Dopamine Receptor
Opioid Receptor
Hedgehog/Smoothened
OX Receptor (Orexin Receptor)
MT Receptor (Melatonin Receptor)
Cannabinoid Receptor
Endothelin Receptor
S1P Receptor (Sphingosine 1-phosphate Receptor)
SGLT (Sodium-dependent Glucose Cotransporter)
LPA Receptor (Lysophosphatidic Acid Receptor)
CGRP Receptor (Calcitonin Gene-related Peptide Receptor)
PAFR (Platelet-activating Factor Receptor)
cAMP
CXCR
102
102
102
102
102
102
102
102
103
103
103
103
103
104
104
104
104
GPCR & G Protein
HCV Protease
HIV Protease
Integrase
Reverse Transcriptase
CCR (C-C Chemokine Receptor)
121
121
121
122
122
Microbiology
Cathepsin K
FXR (Farnesoid X Receptor)
gp120/CD4
IL Receptor
123
123
123
123
Others
123
123
123
123
123
123
Thrombin
TRPV (Transient Receptor Potential Vanilloid)
Liver X Receptor
Phosphorylase
PKA
Substance P
Bioactive Screening
Libraries
Customize Your Library
Bioactive Compound Library
Kinase Inhibitor Library
FDA-approved Drug Library
Inhibitor Library
Epigenetics Compound Library
Target Selective Inhibitor Library
Natural Product Library
GPCR Compound Library
Anti-cancer Compound Library
Tyrosine Kinase Inhibitor Library
StemCell Signaling Compound Library
Cambridge Cancer Compound Library
Pfizer Licensed Compound Library
Autophagy Compound Library
Ion Channel Ligand Library
PI3K/Akt Inhibitor Library
Apoptosis Compound Library
MAPK Inhibitor Library
Protease Inhibitor Library
Anti-infection Compound Library
Anti-diabetic Compound Library
124
125
125
126
126
127
127
128
128
129
129
130
130
131
131
131
132
132
132
133
133
133
ProductAlphabetical Index
Product Catalog Number Index
View More Online
134
143
148
Indices
Caspase
Gamma-secretase
Proteasome
HCV Protease
DPP-4
HIV Protease
MMP (Matrix Metalloproteinase)
118
118
118
119
120
120
120
Proteases
Opioid Receptor
5-alpha Reductase
Estrogen/progestogen Receptor
Androgen Receptor
RAAS
Aromatase
GPR (Glycoprotein Receptor)
105
105
105
106
107
108
108
Endocrinology & Hormones
GABA Receptor
P-gp(Permeability Glycoprotein)
CalciumChannel
SodiumChannel
ATPase
PotassiumChannel
Proton Pump
CFTR (Cystic Fibrosis Transmembrane Conductance Regulator)
109
109
109
110
110
110
111
111
Transmembrane Transporters
HSP (e.g.HSP90)
PPAR
P450 (e.g. CYP17)
PDE
Hydroxylase
Factor Xa
DHFR (Dihydrofolate Reductase)
Aminopeptidase
Dehydrogenase
Phospholipase (e.g. PLA)
Carbonic Anhydrase
MAO (Monoamine Oxidase)
FAAH(FattyAcidAmide Hydrolase)
HMG-CoA Reductase
112
112
113
113
115
115
115
115
115
116
116
116
116
116
Metabolism
Transferase
IDO (Indoleamine-2,3-dioxygenase)
CETP (Cholesteryl Ester Transfer Protein)
Procollagen C Proteinase BoneMorphogeneticProtein1(BMP1)
117
117
117
117
2
info@selleckchem.com Toll Free:(877)796-6397
Phone:+1-832-582-8158
---USA and Canada only---
www.selleckchem.com
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PI3K
CAL-101 is a selective p110 inhibitor with
IC50 of 2.5 nM; shown to have 40- to 300-fold
greater selectivity for p110 than p110//,
and400- to 4000-foldmore selectivityto p110
than C2, hVPS34, DNA-PK and mTOR.
Phase 3.
S2226 CAL-101 (Idelalisib, GS-1101) PI3K p110 selective
Product Citations:
Blood, 2012, 120(19): 3978-85
Haematologica, 2013, 98(1): 57-64
Data from [ Blood, 2012,
120(19): 3978-85 ]
CAL-101 purchased from
Selleck
Product Citation:
Cancer Cell, 2012, 21(2): 155-67
BKM120 is a selective PI3K inhibitor of p110
/// with IC50 of 52 nM/166 nM/116 nM
/262 nM, respectively. Reduced potency
against VPS34, mTOR, DNAPK, with little
activity to PI4K. Phase 1/2.
S2247 BKM120 (NVP-BKM120, Buparlisib)
Data from [ Cancer Cell,
2012, 21(2): 155-67 ]
BKM120 purchased from
Selleck
NU7441 is a highly potent and selective
DNA-PK inhibitor with IC50 of 14 nM and also
inhibits PI3K with IC50 of 5 M.
S2638 NU7441 (KU-57788)
Product Citation:
Nucleic Acids Res, 2013, ahead of print
***
***
***
**
**
*
***
+ + + +
+
+ +
+
lgM
CAL-101
%
via
b
le
ce
lls
0
25
50
75
100
ABT-737
GAPDH
S6
pS6
AKT
pAKT (Ser473)
D
M
S
O
B
E
Z-235 (5uM
)
B
E
Z-235 (1uM
)
B
K
M
-120 (5uM
)
B
K
M
-120 (1uM
)
R
A
D
-001 (5uM
)
R
A
D
-001 (1uM
)
C
yclopam
ine (2.5uM
)
C
yclopam
ine (1uM
)
Data independently produced
by Dr. Zhang of Tianjin
Medical University
NU7441 purchased from
Selleck
PI-103 is a third multi-targeted PI3K inhibitor,
mostly for p110 with IC50 of 2 nM (less
potent to p110//), also inhibits mTORC1/2
and DNA-PK with IC50 of 20 nM/83 nM and 8
nM, respectively.
S1038 PI-103
Product Citations:
Leukemia, 2013, 27(3): 650-60
Leukemia, 2012, 26(5): 927-33
Data from [ J Cell Mol Med,
2013, 17(5): 648-56 ]
PI-103 purchased from
Selleck
TGX-221 is a p110-specific inhibitor with
IC50 of 5 nM, 1000-fold more selective for
p110 than p110.
S1169 TGX-221
Product Citations:
J Pharmacol Exp Ther, 2012, 341(1): 104-14
Mol Med, 2012, 18: 336-45
PI3K p110 selective
Data from [ Mol Med, 2012,
18: 336-45 ]
TGX-221 purchased from
Selleck
AKT
p-AKT
NU-7441 (uM) EGF+ EGF- 0.01 0.1 1.0 1.0
10 mM/1 mL in DMSO 5 mg 200 mg 10 mg
Size
A66 is a potent and specific p110 inhibitor
with IC50 of 32 nM, >100 fold selectivity for
p110 over other class-I PI3K isoforms.
S2636 A66
Product Citation:
Genes Dev, 2012, 26(14): 1573-86
PI3K p110 selective
Data from [ Genes Dev, 2012,
26(14): 1573-86 ]
A66 purchased fromSelleck
10 mM/1 mL in DMSO
5 mg 100 mg 25 mg
Size
GDC-0941 is a potent inhibitor of PI3K/
with IC50 of 3 nM, with modest selectivity
against p110 (10-fold) and p110 (25-fold).
S1065 GDC-0941
Product Citations:
Cell Stem Cell, 2012, 10(2): 210-7
Proc Natl Acad Sci U S A, 2012, 109(31): E2127-33
Data from [ J Cell Sci, 2012,
125(Pt 5): 1259-73 ]
GDC-0941 purchased from
Selleck
no ATP
no GST-Akt1
no Rictor Ab
TGF- (min)
m
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a
s
s
a
y
Insulin (min)
SB431542
GDC-0941
pAktS473
Akt
Rictor
mTOR
15 30 30 30 30 30
30 30
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 100 mg 25 mg
Size
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
GDC-0032 is a potent, next-generation
isoform-sparing PI3K inhibitor targeting PI3K
// with IC50 of 0.29 nM/0.12 nM/0.97nM,
>10 fold selective over PI3K.
S7103 GDC-0032
5 mg 50 mg
Size
BYL719 is a potent and selective PI3K
inhibitor with IC50 of 5 nM, and minimal effect
on PI3K//. Phase 1/2.
S2814 BYL719 PI3K selective
new
N
O
N
N
N
N
N
N
O H2N
N
O
H
N
O
H2N
S
N
N
F
F
F
Excellent Validation, Technical Support and Prompt Delivery
1
PI3K
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BEZ235 (NVP-BEZ235) is a dual ATP-
competitive PI3K and mTOR inhibitor for
p110/// and mTOR(p70S6K) with IC50 of
4 nM/5 nM/7 nM/75 nM/6 nM, respectively.
Inhibits ATR with IC50 of 21 nM; shown to be
poorly inhibitory to Akt and PDK1. Phase 1/2.
S1009 BEZ235 (NVP-BEZ235)
PI3K/Akt/mTOR Pathway
PI3K Inhibitors
Product Citations:
Nature, 2012, 487(7408): 505-9
Blood, 2011, 118(14): 3911-21
Data from [ Cancer Res,
2011, 71(15): 5067-74 ]
BEZ235 purchased from
Selleck
10 mM/1 mL in DMSO
100 mg 50 mg
Size
10 mM/1 mL in DMSO
25 mg 200 mg 10 mg
Size
LY294002 is the first synthetic molecule
known to inhibit PI3K// with IC50 of 0.5 M
/0.57 M/0.97 M, respectively; more stable
in solution than Wortmannin, and also blocks
autophagosome formation.
S1105 LY294002
Product Citations:
Clin Cancer Res, 2011, 17(22): 7116-26
Oncogene, 2012, 31(27): 3277-86
Data from [ Oncogene, 2012,
31(27): 3277-86]
LY294002 purchased from
Selleck
co
n
tro
l
Inhibitor: none
PI3K
(LY294002)
MAPK
(AZD6244)
pERK
pAKT S473
p
11
0
p
3
7
co
n
tro
l
p
11
0
p
3
7
co
n
tro
l
p
11
0
p
3
7
Data from [Cancer Res 2011.August;71:5067-74]
BEZ235 purchased fromSelleck
MEK1/2, rather than B-RAF, targeting in combination with dual PI3K and
mTORC1/2 suppression augments apoptosis induction. Live (green) versus dead
(orange) cells in PPRM spheroids treated with DMSO, 1 mol/L PLX4032, 1 mol/L
AZD6244, 0.1 mol/L BEZ235, or the indicated combinations (dosed every 48
hours) for 6 days.
DMSO PLX4032 AZD6244 BEZ235
PLX4032
+
BEZ235
AZD6244
+
BEZ235
M
2
2
9
R
5
M
2
3
8
R
1
P
1
4
8
R
PI3K
PI3K
PI3K
PI3K
RTK GPCR Cytokines
BCR
Cell Cycle
Apoptosis
Cyclin D1
C-Abl Syk
Ras
PKC
Bcl-2
NF-B
mTOR
ROCK
GSK-3
Wee1
Akt
PDK-1
Caspase
MDM2
p53
Bcl-2
Bax
Bim
Foxo3A
eNOS
NO
Cardiovascular Homeostasis
HSP
DNA-PK
Rictor
GBL
mTOR
mTOR
DEPTOR
DEPTOR
GBL
Raptor
p70S6K S6
Protein Synthesis
Ca2+
m
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PDK-1 inhibitors
BX-912
BX-795
OSU-03012
PHT-427
BEZ235
LY294002
GDC-0941
Selective PI3K inhibitors
BYL719(p110)
GSK2636771(p110)
TGX-221(p110)
AS-252424(p110)
CAL-101(p110)
IPI-145(p110)
Pan-PI3K inhibitors
Selective mTOR inhibitors
Pan-mTOR inhibitors
PF-04691502(mTORC1)
AZD8055
INK 128
Rapamyci n
Everol i mus(mTORC1)
Pan-GSK3 inhibitors
CHIR-99021
CHIR-98014
LY2090314
Selective GSK3 inhibitors
SB 216763(GSK-3)
Tideglusib(GSK-3)
TWS119(GSK-3)
CCT128930(Akt2)
Pan-Akt inhibitors
MK-2206
GSK690693
GDC-0068
Selective Akt inhibitors
A-674563(Akt1)
Pan-mTOR inhibitors
AZD8055
INK 128
PF-04691502(mTORC1)
Rapamyci n
S6 kinase inhibitors
BI-D1870
H 89
PF-4708671
FMK
AT7867
DNA-PK inhibitors
NU7441
PI-103
NU7026
PIK-75
Excellent Validation, Technical Support and Prompt Delivery 3
PI3K
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ZSTK474 inhibits class I PI3K isoforms with
IC50 of 37 nM, mostly PI3K.
S1072 ZSTK474
Product Citation:
J Biomol Screen, 2012, 17(8): 1018-29
by Saraswati Sukumar of
Johns Hopkins University
School of Medicine
ZSTK474 purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 50 mg
Size
XL147 (SAR245408) is a selective and
reversible class I PI3K inhibitor for PI3K//
with IC50 of 39 nM/36 nM/23 nM, less potent
to PI3K. Phase 1/2.
S1118 XL147
Product Citation:
Autophagy, 2012, 8(6): 903-14
by Dr. Chunrong Yu of
RoswelI Park Cancer Institute
XL147 purchased from
Selleck
10 mg 200 mg 50 mg
Size
5 mg 100 mg 10 mg
Size
AS-605240 selectively inhibits PI3K with
IC50 of 8 nM, over 30-fold and 7.5-fold more
selective for PI3K than PI3K/ and PI3K,
respectively.
S1410 AS-605240
Product Citation:
PLoS One, 2013, 8(2): e57809
PI3K selective
Medical University
AS-605240 purchased from
Selleck
PIK-75 is a p110 inhibitor with IC50 of 5.8nM
(200-fold more potently than p110),
isoform-specific mutants at Ser773, and also
potently inhibits DNA-PK with IC50 of 2 nM.
S1205 PIK-75
Product Citation:
Mol Carcinog, 2013, 52(9): 667-75
PI3K p110 selective
10 mg 200 mg 25mg
Size
Data from [ Mol Carcinog,
2013, 52(9): 667-75 ]
PIK-75 purchased from
Selleck
10 mM/1 mL in DMSO
50 mg 500 mg
Size
3-Methyladenine (3-MA) is a selective PI3K
inhibitor for Vps34 and PI3K with IC50 of 25 M
and 60 M; blocks class I PI3K consistently,
whereas suppression of class III PI3K is
transient, and also blocks autophagosome
formation.
S2767 3-Methyladenine
by Magorzata Durbas from
J agiellonian University Poland
3-Methyladenine purchased
fromSelleck
10 mM/1 mL in DMSO
5 mg 200 mg 10 mg
Size
XL765 is a dual inhibitor of mTOR/PI3K,
mostly for p110 with IC50 of 9 nM; also
inhibits DNA-PK and mTOR. Phase 1/2.
S1523 SAR245409 (XL765)
Product Citation:
Endocrinology, 2013, 154(3): 1247-59
Data from [ Endocrinology,
2013, 154(3): 1247-59 ]
SAR245409 purchased from
Selleck
2 mg 50 mg 10 mg
Size
GSK2126458 is a highly selective and potent
inhibitor of p110///, mTORC1/2 with Ki of
0.019 nM/0.13 nM/0.024 nM/0.06 nM and
0.18 nM/0.3 nM, respectively. Phase 1.
S2658 GSK2126458 (GSK458)
by one customer
GSK2126458 purchased from
Selleck
-actin
Akt
P-Akt
mTOR
P-mTOR
0 0.03 0.1 0.3 1 3 GSK2126458 (M)
PIK-75 (M)
BRCA1-siRNA
Control-siRNA
0
0
20
40
60
80
100
120
0.01 0.1 1
%
o
f C
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l
* *
* * *
* * *
5 mg 50 mg 10 mg
Size
IC-87114 is a selective PI3K inhibitor with
IC50 of 0.5 M, 58-fold more selective for
PI3K than PI3K, and over 100-fold more
selective than PI3K/.
S1268 IC-87114
Product Citations:
Clin Cancer Res, 2012, 18(21): 5878-87
J Inves Der, 2011, 131(2): 495-503
PI3K selective
Data from [ J Inves Der,
2011, 131(2): 495-503 ]
IC-87114 purchased from
Selleck
IC87114 (mol l-1) 0 2.5 7.5 10 5
0
20
40
60
80
100
120
140
V
ia
b
ility
(%
)
4
Phone:+1-832-582-8158
www.selleckchem.com
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PI3K
10 mg 200 mg 50 mg
Size
10 mg 50 mg
Size
by Dr. Yong-Weon Yi from
Georgetown University
Medical Center
Selleck
by Antonino Maria Spart
fromUniversity of Bologna
Selleck
PIK-90 is a PI3K// inhibitor with IC50 of 11
nM/18 nM/58 nM, respectively, less potent to
PI3K.
S1187 PIK-90
Product Citation:
J Cell Biol, 2012, 198(2): 185-94
GSK1059615 is a dual inhibitor of PI3K//
/ (reversible) and mTOR with IC50 of 0.4 nM
/0.6 nM/2 nM/5 nM and 12 nM, respectively.
Phase 1.
S1360 GSK1059615
30 kDa
35 kDa
Caspase 7
CTRL
GSK-1059615
Product Citation:
Nature, 2012, 486(7404): 532-36
M
IC50 2.678
R square 0.9450
-3
0
20
40
60
80
100
-2 2 -1 1 0
%
Inhibition vs C
T
R
L
Log[C], (M)
10 mM/1 mL in DMSO
5 mg 200 mg 10 mg
Size
Medical University
Selleck
PIK-294 is a highly selective p110 inhibitor
withIC50 of 10 nM, 1000-, 49- and 16-fold less
potent to PI3K//, respectively.
S2227 PIK-294 PI3K p110 selective
Product Citation:
Mol Cell Biol, 2012, 32(12): 2268-78
10 mM/1 mL in DMSO
2 mg 100 mg 25 mg
Size
Medical University
Selleck
AS-604850 is a selective, ATP-competitive
PI3K inhibitor with IC50 of 250 nM, over 80-fold
selectivity for PI3K than PI3K/, and 18-fold
more selective for PI3K than PI3K.
S2681 AS-604850 PI3K selective
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
Medical University
CAY10505 purchased from
Selleck
CAY10505 is dehydroxyl of AS-252424,
which is a PI3K inhibitor with IC50 of 33 nM.
S2682 CAY10505 PI3K selective
5 mg 50 mg 10 mg
Size
5 mg 200 mg 10 mg
Size
10 mM/1 mL in DMSO
5 mg 200 mg 10 mg
Size
10 mM/1 mL in DMSO
5 mg 100 mg 25 mg
Size
AZD6482 is a PI3K inhibitor with IC50 of 10
nM, 8-, 86- and 109-fold more selective to
PI3K than PI3K, PI3K and PI3K. Phase 1.
S1462 AZD6482
Product Citation:
Diabetologia, 2013, 56(6): 1339-49
by one customer
AZD6482 purchased from
Selleck
Medical University
PF-05212384 purchased from
Selleck
by Dr.Wang Wei from
NanFang Hospital
Selleck
Medical University
Selleck
PKI-587 is a highly potent dual inhibitor of
PI3K, PI3K and mTOR with IC50 of 0.4 nM,
5.4 nM and 1.6 nM, respectively. Phase 2.
S2628 PF-05212384 (PKI-587)
GDC-0980 (RG7422) is a potent, class I PI3K
inhibitor for PI3K/// with IC50 of 5 nM/27
nM/7 nM/14 nM, respectively. Also a mTOR
inhibitor with Ki of 17 nM, and highly selective
versus others PIKK family kinases. Phase 2.
S2696 GDC-0980 (RG7422)
GDC-0980(M)
P-mTOR
0 0.03 0.1 0.3 1 3
mTOR
P-Akt
Akt
-actin
PIK-93 is the first potent, synthetic PI4K
(PI4KIII) inhibitor with IC50 of 19 nM; shown
to inhibit PI3K with IC50 of 39 nM.
S1489 PIK-93
WM9
WM46
WM88
WM164
451LU
WM983B
1205LU
WM1366
WM3451
WM3692
WM3918
G
ro
w
th
In
h
ib
itio
n
10 2
0.4
0.08
0.016
0.032
0.00064
0.000128
0.0000256
0.00000512
0
0.2
0.4
0.6
0.8
1
1.2 uMAZD6482
PF-04691502 is an ATP-competitive PI3K
(///)/mTOR dual inhibitor with Ki of 1.8
nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little
activity against either Vps34, AKT, PDK1,
p70S6K, MEK, ERK, p38, or JNK. Phase 2.
S2743 PF-04691502
Medical University
Selleck
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
PF-04691502(M)
P-Akt
0.01 0.1 1.0 10 EGF+ EGF-
Akt
Licensed by Pfizer
Product Citation:
J Pharmacol Exp Ther, 2013, ahead of print
6
Phone:+1-832-582-8158
www.selleckchem.com
P
I
3
K
/
A
k
t
/
m
T
O
R
PI3K / mTOR
PI-103
GDC-0941
ZSTK474
LY294002
XL147
TGX-221
PIK-90
PIK-75
TG100-115
GSK1059615
AS-605240
AZD6482
PIK-93
XL765
PIK-293
CAL-101
PIK-294
BKM120
PF-05212384
A66
NU7441
AS-252424
AS-604850
CAY10505
GDC-0980
CH5132799
PKI-402
PF-04691502
3-Methyladenine
BAY80-6946
TG 100713
IPI-145
GSK2636771
S1038
S1065
S1072
S1105
S1118
S1169
S1187
S1205
S1352
S1360
S1410
S1462
S1489
S1523
S2207
S2226
S2227
S2247
S2628
S2636
S2638
S2671
S2681
S2682
S2696
S2699
S2739
S2743
S2767
S2802
S2870
S7028
S8002
+++
+++
++
+++
++
++
+++
++++
+
+
++++
++
+
+++
++++
++
++
+
++
+++
+++
+++
+++
+++
++++
+
8 nM [IC50]
3 nM [IC50]
16 nM [IC50]
0.5 M [IC50]
39 nM [IC50]
11 nM [IC50]
5.8 nM [IC50]
0.4 nM [IC50]
60 nM [IC50]
1.4 M [IC50]
39 nM [IC50]
39 nM [IC50]
100 M [IC50]
52-99 nM [IC50]
0.4 nM [IC50]
32 nM [IC50]
5 M [IC50]
935 nM [IC50]
4.5 M [IC50]
0.94 M [IC50]
5 nM [IC50]
14 nM [IC50]
2 nM [IC50]
1.8 nM [Ki]
0.469 nM [IC50]
165 nM [IC50]
+
++
++
+++
+
+++
+
++++
+
++
+
+
+
+
++
+
+
++
++
+++
+++
+++
+
+
88 nM [IC50]
33 nM [IC50]
44 nM [IC50]
0.97 M [IC50]
383 nM [IC50]
8.5 nM [IC50]
350 nM [IC50]
0.6 nM [IC50]
270 nM [IC50]
21 nM [IC50]
0.59 M [IC50]
113 nM [IC50]
25 M [IC50]
490 nM [IC50]
166 nM [IC50]
>20 M [IC50]
20 M [IC50]
27 nM [IC50]
0.12 M [IC50]
7 nM [IC50]
2.1 nM [Ki]
3.72 nM [IC50]
215 nM [IC50]
61 nM [IC50]
++
+++
++
+++
++
+
+
+++
+
+
+
++
+++
+++
+++
++
+
+
+++
++
++
+++
++
++++
48 nM [IC50]
3 nM [IC50]
4.6 nM [IC50]
0.57 M [IC50]
36 nM [IC50]
58 nM [IC50]
235 nM [IC50]
2 nM [IC50]
300 nM [IC50]
80 nM [IC50]
0.12 M [IC50]
43 nM [IC50]
0.24 M [IC50]
2.5 nM [IC50]
10 nM [IC50]
116 nM [IC50]
>20 M [IC50]
20 M [IC50]
7 nM [IC50]
0.5 M [IC50]
14 nM [IC50]
1.6 nM [Ki]
24 nM [IC50]
1 nM [IC50]
+
+
++
++
++
+
+++
+++
+
++++
+++
++
+
+
+++
+++
++++
+
++
+++
++
+++
+
++
++
105 nM [IC50]
75 nM [IC50]
49 nM [IC50]
33 nM [IC50]
18 nM [IC50]
83 nM [IC50]
5 nM [IC50]
8 nM [IC50]
1.2 M [IC50]
16 nM [IC50]
9 nM [IC50]
10 M [IC50]
160 nM [IC50]
262 nM [IC50]
5.4 nM [IC50]
33 nM [IC50]
250 nM [IC50]
30 M [IC50]
14 nM [IC50]
36 nM [IC50]
16 nM [IC50]
1.9 nM [Ki]
60 M [IC50]
50 nM [IC50]
50 nM [IC50]
+ 25 M [IC50]
Inhibitory Selectivity
p110 p110 p110 p110 Vps34-like Cat.No. Inhibitor Name
Product Citations:
Cancer Cell, 2012, 21(2): 155-67
Clin Cancer Res, 2013, 19(3): 598-609
Everolimus (RAD001) is an mTOR inhibitor of
FKBP12 with IC50 of 1.6-2.4 nM.
S1120 Everolimus (RAD001)
2012, 21(2): 155-67 ]
Everolimus purchased from
Selleck
10 mM/1 mL in DMSO
100 mg 25 mg
Size
GAPDH
S6
pS6
AKT
pAKT (Ser473)
D
M
S
O
B
E
Z
-2
3
5
(5
u
M
)
B
E
Z
-2
3
5
(1
u
M
)
B
K
M
-1
2
0
(5
u
M
)
B
K
M
-1
2
0
(1
u
M
)
R
A
D
-0
0
1
(5
u
M
)
R
A
D
-0
0
1
(1
u
M
)
C
yclo
p
a
m
in
e
(2
.5
u
M
)
C
yclo
p
a
m
in
e
(1
u
M
)
mTOR Inhibitors
Rapamycin (Sirolimus, AY-22989,
WY-090217) is a specific mTOR inhibitor
with IC50 of ~0.1 nM.
S1039 Rapamycin
(Sirolimus, AY22989, NSC226080)
Product Citations:
Cancer Cell, 2011, 19(6): 792-804
Cell Res, 2012, 22(6): 1003-21
10 mM/1 mL in DMSO
100 mg 5 mg
Size
2011, 19(6): 792-804 ]
Rapamycin purchased from
Selleck
Licensed by Pfizer
Notes: 1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is.
2.Black "+" corresponds to IC50 or Ki values in nMs, gray "+" refers to values in Ms.
5
PI3K
P
I
3
K
/
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k
t
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m
T
O
R
BAY 80-6946 is a potent and highly selective
reversible PI3K inhibitor for PI3K/ with IC50
of 0.469 nM/3.72 nM. Phase 1.
S2802 BAY80-6946
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 10 mM/1 mL in DMSO 50 mg 25 mg
Size
5 mg 200 mg 50 mg
Size
Size
Size
TG100-115 is a PI3K/ inhibitor with IC50 of
83 nM/235 nM, with little effect on PI3K/.
Phase 1/2.
S1352 TG100-115
YM201636 is a selective PIKfyve inhibitor
with IC50 of 33 nM, less potent to p110 and
insensitive to Fabl (yeast orthologue).
S1219 YM201636
CH5132799 inhibits class I PI3Ks,
particularly PI3K with IC50 of 14 nM; less
potent to PI3K//, while sensitive in
PIK3CA mutations cell lines. Phase 1.
S2699 CH5132799 PI3K selective
NVP-BGT226 is a novel class I PI3K/mTOR
inhibitor for PI3K// with IC50 of 4 nM/63
nM/38 nM. Phase 1/2.
S2749 NVP-BGT226 (BGT226)
CUDC-907 is a dual PI3K and HDAC
inhibitor for PI3K and HDAC1/2/3/10 with
IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8
nM, respectively. Phase 1.
S2759 CUDC-907 PI3K selective
Medical University
Selleck
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
PI3K selective
PIK-293 is a PI3K inhibitor, mostly for PI3K
with IC50 of 0.24 M, 500-, 100- and 50-fold
less potent to PI3K//, respectively.
S2207 PIK-293
HN
N
N
N
O
O
N
O
O
N
N
NH2
Size
10 mg 10 mM/1 mL in DMSO 200 mg
Size
Size
Medical University
Selleck
10 mM/1 mL in DMSO
2 mg 100 mg 25 mg
Size
PI3K selective
AS-252424 is a novel, potent PI3K inhibitor
with IC50 of 30 nM with 30-fold selectivity for
PI3K than PI3K, and low inhibitory activity
towards PI3K/.
S2671 AS-252424
10 mg 200 mg
Size
TG 100713 is a pan-PI3K inhibitor against
PI3K, PI3K, PI3K and PI3K with IC50 of
50 nM, 24 nM, 165 nM and 215 nM,
respectively.
S2870 TG 100713
IPI-145 (INK1197) is a novel and selective
PI3K / inhibitor with Ki and IC50 of 23
pM/243 pM and 1 nM/50 nM, highly selective
PI3K / than other protein kinases. Phase 2.
S7028 IPI-145 (INK1197)
GSK2636771 is a potent, orally bioavailable,
PI3K-selective inhibitor, sensitive to PTEN
null cell lines. Phase 1/2a.
S8002 GSK2636771 PI3K selective
5 mg 200 mg 50 mg
Size
PKI-402 is a potent dual pan-PI3K/mTOR
inhibitor targeting PI3K/// and mTOR
with IC50 of 2 nM/7 nM/16 nM/14 nM and 3
nM, respectively; also potent to PI3K
mutants E545K and H1047R.
S2739 PKI-402
Wortmannin is a PI3K with IC50 of 3 nM, first
described PI3K inhibitors, but little selectivity
within the PI3K family. Also blocks
autophagosome formation and potently
inhibits DNA-PK/ATM with IC50 of 16 nM and
150 nM. Phase 4.
S2758 Wortmannin
Product Citation:
J Cell Sci, 2013, 126(Pt 3): 715-21
N
N
N
N
NH2
H2N
OH
N
N
F
F
F
N
O OH
O
N
Cl O
NH N
N
HN
N
7
mTOR
P
I
3
K
/
A
k
t
/
m
T
O
R
10 mg 50 mg 25 mg
Size
AZD8055 is a novel ATP-competitive mTOR
inhibitor with IC50 of 0.8 nM with excellent
selectivity (~1,000-fold) against PI3K
isoforms and ATM/DNA-PK. Phase 1.
S1555 AZD8055
Data from [ Autophagy,
2013, 9(1): 74-92 ]
Selleck
Product Citations:
Autophagy, 2013, 9(1): 74-92
Biochem Pharmacol, 2012, 83(9): 1183-94
INK 128 is a potent and selective mTOR
inhibitor with IC50 of 1 nM; >200-fold less
potent to class I PI3K isoforms, superior in
blocking mTORC1/2 and sensitive to
pro-invasion genes (vs Rapamycin). Phase
1.
S2811 INK 128
10 mM/1 mL in DMSO
10 mg 50 mg
Size
Product Citation:
Autophagy, 2012, 8(6): 903-14
2012, 8(6): 903-14]
PP242 purchased from
Selleck
PP242 is a selective mTOR inhibitor with IC50
of 8 nM; targets both mTOR complexes with
>10- and 100-fold selectivity for mTOR than
PI3K or PI3K//, respectively.
S2218 PP242
by one customer
INK 128 purchased from
Selleck
30 kDa
35 kDa
Caspase 7
CTRL
INK-128
M
IC50 1.868
R square 0.9637
Log[C], (M)
BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR
inhibitor for p110/// and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7
nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown
to be poorly inhibitory to Akt and PDK1. Phase 1/2.
S1038 PI-103
PI-103 is a third multi-targeted PI3K inhibitor, mostly for p110 with
IC50 of 2 nM (less potent to p110//), also inhibits mTORC1/2 and
DNA-PK with IC50 of 20 nM/83 nM and 8 nM, respectively.
10 mM/1 mL in DMSO
5 mg 100 mg 10 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg
Size
Page 2
Page 1
N
N N
N
NH2
N
O
NH2
Torin 1 is a potent inhibitor of mTORC1/2 with
IC50 of 2 nM/10 nM; exhibits 1000-fold
selectivity for mTOR than PI3K.
S2827 Torin 1
GSK2126458 is a highly selective and potent inhibitor of p110///,
mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18
nM/0.3 nM, respectively. Phase 1.
Product Citation:
Mol Genet Meta, 2010, 100(4): 309-15
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 100 mg 50 mg
Size
Data from [ Mol Genet Meta,
2010, 100(4): 309-15 ]
Ridaforolimus purchased
fromSelleck
Deforolimus (Ridaforolimus MK-8669) is a
selective mTOR inhibitor with IC50 of 0.2 nM;
while not classified as a prodrug, mTOR
inhibition and FKBP12 binding is similar to
rapamycin.
S1022 Ridaforolimus (Deforolimus)
Data from [ Tuberc Respir
Dis (Seoul), 2012, 72(4):
343-51 ]
Temsirolimus purchased
fromSelleck
Temsirolimus (CCI-779, Torisel) is a specific
mTOR inhibitor with IC50 of 1.76 M.
S1044 Temsirolimus (CCI-779, NSC-683864)
Product Citations:
Autophagy, 2011, 7(2): 176-87
Tuberc Respir Dis (Seoul), 2012, 72(4): 343-51
Control GSK690693
A549
Temsirolimus GSK690693+Temsirolimus
Product Citations:
Cell Stem Cell, 2012, 10(2): 210-7
Circ Res, 2010, 107(10): 1265-74
Data from [ Circ Res, 2010,
107(10): 1265-74]
Ku-0063794 purchased from
Selleck
KU-0063794 is a potent and highly specific
dual-mTOR inhibitor of mTORC1 and
mTORC2 with IC50 of ~10 nM; no effect on
PI3Ks.
S1226 Ku-0063794
S2658 GSK2126458 (GSK458)
Page 3
Page 3
S1523 SAR245409 (XL765)
XL765 is a dual inhibitor of mTOR/PI3K, mostly for p110 with IC50
of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
N
N
O
N
F
F F
N
N
O
8
Phone:+1-832-582-8158
www.selleckchem.com
P
I
3
K
/
A
k
t
/
m
T
O
R
mTOR
Size
Size
PF-04691502 is an ATP-competitive PI3K(///)/mTOR dual
inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little
activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38,
or JNK. Phase 2.
S2743 PF-04691502 mTORC1 selective
PKI-587 is a highly potent dual inhibitor of PI3K, PI3K and mTOR
with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2.
S2628 PF-05212384 (PKI-587)
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
Product Citation:
Exp Eye Res, 2013, 113C: 9-18
Data from [ Exp Eye Res,
2013, 113C: 9-18 ]
OSI-027 purchased from
Selleck
OSI-027 is a selective and potent dual
inhibitor of mTORC1 and mTORC2 with IC50
of 22 nM and 65 nM, and more than 100-fold
selectivity observed for mTOR than PI3K,
PI3K, PI3K or DNA-PK.
S2624 OSI-027
WYE-125132 is a highly potent,
ATP-competitive mTOR inhibitor with IC50 of
0.19 nM; highly selective for mTOR versus
PI3Ks or PI3K-related kinases hSMG1 and
ATR.
S2661 WYE-125132 (WYE-132)
WYE-687 is an ATP-competitive and
selective inhibitor of mTOR with IC50 of 7nM;
blocks mTORC1/pS6K(T389) and
mTORC2/P-AKT(S473) but no effect
observed on P-AKT(T308). Selectivity for
mTOR is greater than PI3K (>100-fold) and
PI3K (>500-fold).
S2668 WYE-687
Torin 2 is a potent and selective mTOR
inhibitor with IC50 of 0.25 nM; 800-fold
greater selectivity for mTOR than PI3K and
improved pharmacokinetic properties.
Inhibition of ATM/ATR/DNA-PK with EC50 of
28 nM/35 nM/118 nM, respectively.
S2817 Torin 2
Medical University
Palomid 529 purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
Palomid 529 inhibits both the mTORC1 and
mTORC2 complexes, reduces
phosphorylation of pAktS473, pGSK3S9,
and pS6 but no effect observed on pMAPK
or pAktT308. Phase 1.
S2238 Palomid 529 (P529)
S2696 GDC-0980 (RG7422)
AZD2014 is a novel mTOR inhibitor with IC50
of 2.8 nM; highly selective against multiple
PI3K isoforms (///). Phase 2.
S2783 AZD2014
10 mM/1 mL in DMSO
5 mg 200 mg 10 mg
Size
by Dr. Milica Pesic from
Institute for Biological
Research
Selleck
WYE-354 is a potent, specific and
ATP-competitive inhibitor of mTOR with IC50
of 5 nM, blocks mTORC1/P-S6K(T389) and
mTORC2/P-AKT(S473) not P-AKT(T308),
selective for mTOR than PI3K (>100-fold)
and PI3K (>500-fold).
S1266 WYE-354
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
Data from [ Mol Cancer Res,
2012, 10(6): 821-33 ]
WYE-354 purchased from
Selleck
Product Citation:
Mol Cancer Res, 2012, 10(6): 821-33
GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3K
/// with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a
mTOR inhibitor with Ki of 17 nM, and highly selective versus others
PIKK family kinases. Phase 2.
Page 4
Page 4
Page 4
GSK1059615 is a dual inhibitor of PI3K/// (reversible) and
mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
Phase 1.
S1360 GSK1059615
Page 4
CH5132799 inhibits class I PI3Ks, particularly PI3K with IC50 of 14
nM; less potent to PI3K//, while sensitive in PIK3CAmutations cell
lines. Phase 1.
S2699 CH5132799
Page 5
5 mg 200 mg 50 mg
Size
N N
N
N
O
N
H
O
N
O
N
N
O
F F
F
N H2N
9
mTOR / Akt
P
I
3
K
/
A
k
t
/
m
T
O
R
Size
10 mM/1 mL in DMSO 5 mg 50 mg
Size
Data from [ J Clin Invest,
2011, 121(9): 3623-34 ]
MK-2206 2HCl purchased
fromSelleck
Product Citations:
J Clin Invest, 2011, 121(9): 3623-34
Mol Cell, 2012, 47(3): 422-33
MK-2206 2HCl is a highly selective inhibitor of
Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM,
respectively; no inhibitory activities against
250 other protein kinases observed. Phase 2.
S1078 MK-2206 2HCl
Akt Inhibitors
10 mM/1 mL in DMSO
50 mg 5 mg
Size
PI-103
Ku-0063794
OSI-027
Torin 1
S1038
S1226
S2624
S2827
++
+++
++
+++
20 nM [IC50]
10 nM [IC50]
22 nM [IC50]
0.29-2 nM [IC50]
+
+++
+
+++
83 nM [IC50]
10 nM [IC50]
65 nM [IC50]
0.29-2 nM [IC50]
p110,DNA-PK,p110,p110,p110
Cat.No. Inhibitor Name mTORC1 mTORC2 Other
Medical University
PP-121 purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
PP-121 is a multi-targeted inhibitor of
PDGFR, Hck, mTOR, VEGFR2, Src and Abl
withIC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM
and 18 nM, also inhibits DNA-PK with IC50 of
60 nM.
S2622 PP-121
NVP-BGT226 is a novel class I PI3K/mTOR inhibitor for PI3K//
with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
S2749 NVP-BGT226 (BGT226)
Page 5
10
Phone:+1-832-582-8158
www.selleckchem.com
P
I
3
K
/
A
k
t
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m
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R
Akt
Size
Size
Size
GDC-0068 is a highly selective pan-Akt
inhibitor targeting Akt1/2/3 with IC50 of 5 nM
/18 nM/8 nM, 620-fold selectivity over PKA.
Phase 2.
S2808 GDC-0068
Product Citations:
Mol Cancer Ther, 2012, 11(7): 1510-17
J Biol Chem, 2013, 286(43): 37389-98
Data from [ Mol Cancer Ther,
2012, 11(7): 1510-17 ]
Selleck
GSK690693 is a pan-Akt inhibitor targeting
Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also
selective for Akt as compared to the AGC
kinase family: PKA, PrkX and PKC isozymes.
Phase 1.
S1113 GSK690693
by Lee lay hoon from National
University of Singapore
A-674563 purchased from
Selleck
A-674563 is an Akt1 inhibitor with Ki of 11 nM,
modest potent to PKA and >30-fold selective
for Akt1 over PKC.
S2670 A-674563
control
H
3 In
c
o
rp
o
ra
tio
n
R848 akti
50nM
TLR7 induced cell proliferation is
dependent onAKT
100nM 1uM 10uM 50uM 500nM
akti akti akti akti akti
0
2000
4000
6000
8000
10000
12000
Triciribine phosphate (TCN-P, NSC-280594,
API-2), the active metabolite of TCN, is a
potent Akt inhibitor with IC50 of 130 nM, that
inhibits the phosphorylation of Akt in intact
cells but not in vitro, more active in cells
lacking adenosine kinase. Phase 1/2.
S2732 Triciribine phosphate
S2743 PF-04691502
PF-04691502 is an ATP-competitive PI3K(///)/mTOR dual
inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little
activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38,
or JNK. Phase 2.
Page 4
5 mg 100 mg 50 mg
Size
50 mg 500 mg 100 mg
Size
50 mg 200 mg 50 mg
Size
N
N
O
NH
Cl
N
N
HO
Product Citations:
Cancer Research, 2012, 72(5): 1229-38
PLoS One, 2013, 8(2): e57508
Data from [ PLoS One, 2013,
8(2): e57508 ]
AT7867 purchased from
Selleck
AT7867 is a potent ATP-competitive inhibitor
of Akt1/2/3 and p70S6K/PKA with IC50 of 32
nM/17 nM/47 nM and 85 nM/20 nM,
respectively; little activity outside the AGC
kinase family.
S1558 AT7867
Input
pAktS473
FLAG
HA
HA
FLAG IP: FLAG
FKBP51TPR_mut_FLAG
HA_Akt1
inhibitor V
III
AT
7867
D
M
S
O
+ + + + + +
+ + + + + +
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 100 mg 50 mg
Size
NH
HN N
Cl
Miltefosine inhibits PI3K/Akt activity with ED50
of 17.2 M and 8.1 M in carcinoma cell lines
A431 and HeLa, first oral drug for Visceral
leishmaniasis, effective against both
promastigotes and amastigotes.
S3056 Miltefosine
N+
O P O
O-
O
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
Product Citation:
Blood, 2011, 118(10): 2840-8
Data from [ Blood, 2011,
118(10): 2840-8 ]
PHT-427 purchased from
Selleck
PHT-427 is a dual Akt and PDPK1 inhibitor
(high affinity binding for the PH domains of
Akt and PDPK1) with Ki of 2.7 M and 5.2 M,
respectively.
S1556 PHT-427
Honokiol is the active principle of magnolia
extract that inhibits Akt-phosphorylation and
promotes ERK1/2 phosphorylation. Phase 3.
S2310 Honokiol
Triciribine (TCN, API-2) is a DNA synthesis
inhibitor, also inhibits Akt and HIV-1 with IC50
of 130 nM and 20 nM, respectively; does not
inhibit PI3K/PDK1; 5000-fold less active in
cells lacking adenosine kinase. Phase 1/2.
S1117 Triciribine
CCT128930 is a potent, ATP-competitive and
selective inhibitor of Akt2 with IC50 of 6 nM,
28-fold greater selectivity for Akt2 than the
closely related PKA kinase.
S2635 CCT128930 Akt2 selective
WAY-600 is a potent, ATP-competitive and
selective inhibitor of mTOR with IC50 of 9nM;
blocks mTORC1/P-S6K(T389) and
mTORC2/P-AKT(S473) but not P-AKT(T308);
selective for mTOR than PI3K (>100-fold)
and PI3K (>500-fold).
S2689 WAY-600
GDC-0349 is a potent and selective
ATP-competitive inhibitor of mTOR with Ki of
3.8 nM, 790-fold inhibitory effect against
PI3K and other 266 kinases. Phase 1.
S8040 GDC-0349
HN O
NH
N
N
N
O
N
O
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
Data from [ PLoS Biol, 2011,
9(9): e1001148 ]
Perifosine purchased from
Selleck
Perifosine (KRX-0401) is a novel Akt inhibitor
with IC50 of 4.7 M, targets pleckstrin
homology domain of Akt. Phase 2.
S1037 Perifosine (KRX-0401)
Product Citations:
Cell, 2012, 149(3): 656-70
PLoS Biol, 2011, 9(9): e1001148
11
Akt / GSK-3
P
I
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K
/
A
k
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/
m
T
O
R
GSK690693
AT7867
CCT128930
A-674563
GDC-0068
AZD5363
S1113
S1558
S2635
S2670
S2808
S8019
+++
++
+++
+++
+++
2 nM [IC50]
32 nM [IC50]
11 nM [Ki]
5 nM [IC50]
3 nM [IC50]
++
++
+++
++
+++
13 nM [IC50]
17 nM [IC50]
6 nM [IC50]
18 nM [IC50]
8 nM [IC50]
+++
++
+++
+++
9 nM [IC50]
47 nM [IC50]
8 nM [IC50]
8 nM [IC50]
S6K1
PKA
PKA,Cdk2
Cat.No. Inhibitor Name AKT1 AKT2 AKT3 Other
5 mg 25 mg
Size
50 mg 200 mg
Size
TIC10 inactivates Akt and ERK to induce
TRAIL through Foxo3a, possesses superior
drug properties: delivery across the
blood-brain barrier, superior stability and
improved pharmacokinetics.
S7127 TIC10 new
N
N
N
N
O
AZD5363 potently inhibits all isoforms of
Akt(Akt1/Akt2/3) with IC50 of 3 nM/8 nM/8
nM, similar to P70S6K/PKA and lower
activity towards ROCK1/2. Phase 1/2.
S8019 AZD5363
N
O
N
H
N
N
N
H
Cl NH2
OH
Size
Product Citations:
Nat Protoc, 2012, 8(1): 162-75
Data from [ Carcinogenesis,
2012, 33(3): 529-37 ]
CHIR-99021 HCl purchased
fromSelleck
CHIR-99021 HCl (CT99021) is hydrochloride
of CHIR-99021, which is a GSK-3/ inhibitor
with IC50 of 10 nM/6.7 nM; ability to
distinguish between GSK-3 and its closest
homologs Cdc2 and ERK2.
S2924 CHIR-99021 (CT99021) HCl
GSK-3 Inhibitors
10 mM/1 mL in DMSO
100 mg 2 mg
Size
SB 216763 is a potent and selective GSK-3
inhibitor with IC50 of 34.3 nM; low inhibitory
effect exhibited on GSK-3.
S1075 SB 216763 GSK-3 selective
N
N
H
N
N
H
N
N
HN
N
Cl Cl
HCl
TWS119 is a GSK-3 inhibitor with IC50 of 30
nM; capable of inducing neuronal
differentiation and may be useful to stem cell
biology.
S1590 TWS119 GSK-3 selective
Size
new
Tideglusib (NP031112, NP-12) is an
irreversible, non ATP-competitive GSK-3
inhibitor with IC50 of 60 nM; fails to inhibit
kinases with a Cys homologous to Cys-199
located in the active site. Phase 1/2.
S2823 Tideglusib GSK-3 selective
S
N
N
O
O
SB 415286 is a potent GSK3 inhibitor with
IC50/Ki of 78 nM/31 nM with equally effective
inhibition of GSK-3.
S2729 SB 415286
10 mM/1 mLin DMSO
25 mg 5 mg
Size
Product Citation:
Stem Cells Dev, 2013, 22(13): 1893-906
Data from [ Stem Cells Dev,
2013, 22(13): 1893-906 ]
CHIR-98014 purchased from
Selleck
CHIR-98014 is a potent GSK-3/ inhibitor
with IC50 of 0.65 nM/0.58 nM, with the ability
to distinguish GSK-3 from its closest
homologs Cdc2 and ERK2.
S2745 CHIR-98014
Beta-catenin expression in hESCs
(20X magnification)
no GSKi
control
CHIR99021
CHIR98014
Size
Size
12
Phone:+1-832-582-8158
www.selleckchem.com
P
I
3
K
/
A
k
t
/
m
T
O
R
GSK-3 / ATM/ATR
SB 216763
TWS119
SB 415286
CHIR-98014
Tideglusib
CHIR-99021 HCl
TDZD-8
LY2090314
S1075
S1590
S2729
S2745
S2823
S2924
S2926
S7063
++
+
++++
+++
+++
34.3 nM [IC50]
78 nM [IC50]
0.65 nM [IC50]
10 nM [IC50]
1.5 nM [IC50]
++
+
++++
+
+++
++
++++
30 nM [IC50]
~78 nM [IC50]
0.58 nM [IC50]
60 nM [IC50]
6.7 nM [IC50]
2 M [IC50]
0.9 nM [IC50]
Cat.No. Inhibitor Name GSK-3 GSK-3
5 mg 50 mg
Size
LY2090314 is a potent GSK-3 inhibitor for
GSK-3/ with IC50 of 1.5 nM/0.9 nM; may
improve the efficacy of platinum-based
chemotherapy regimens. Phase 1/2.
S7063 LY2090314 new
N
N
N
O
NH
O
O
N
N
TDZD-8 is a non-ATP competitive GSK-3
inhibitor with IC50 of 2 M; minimal inhibitory
effect observed on CDK1, casein kinase II,
PKA and PKC.
S2926 TDZD-8 GSK-3 selective
S
N
N
O
O
KU-60019 is an improved analogue of
KU-55933, with IC50 of 6.3 nM for ATM, 270-
and 1,600-fold selective for ATM than
DNA-PK and ATR, a highly effective
radiosensitizer.
S1570 KU-60019
Product Citation:
Brain Pathol, 2012, 22(5): 677-88
Product Citations:
Autophagy, 2012, 8(2): 236-51
Sci Signal, 2013, 6(259): ra5
2012, 8(2): 236-51 ]
KU-55933 purchased from
Selleck
KU-55933 is a potent and specific ATM
inhibitor with IC50/Ki of 12.9 nM/2.2 nM, highly
selective to DNA-PK, PI3K/PI4K, ATR and
mTOR.
S1092 KU-55933
ATM/ATR Inhibitors
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
25 mg
VE-821 is a potent and selective ATP
competitive inhibitor of ATR with Ki/IC50 of 13
nM/26 nM, shows inhibition of H2AX
phosphorylation, minimal activity against
PIKKs ATM, DNA-PK, mTOR and PI3K.
S8007 VE-821
Product Citations:
PLoS One, 2012, 7(11): e50423
J Neurooncol, 2012, 110(3): 349-57
2 mg 5 mg
Size
Data from [ PLoS One, 2012,
7(11): e50423 ]
CP-466722 purchased from
Selleck
CP-466722 is a potent and reversible ATM
inhibitor, does not affect ATR and inhibit PI3K
or PIKK family members in cells.
S2245 CP-466722
N
N
O
NH
S
O
O
H2N
Size
Size
Size
S
O
O
N
H
N
O
N
O
O
13
ATM/ATR / PDK-1 / S6 Kinase
P
I
3
K
/
A
k
t
/
m
T
O
R
KU-55933
KU-60019
Wortmannin
VE-821
S1092
S1570
S2758
S8007
++
++
1.8 M [IC50]
13 nM [Ki]
+++
+++
2.2 nM [Ki]
6.3 nM [IC50]
DNA-PK
Cat.No. Inhibitor Name ATR ATM Other
S2758 Wortmannin
Wortmannin is a PI3K with IC50 of 3 nM, first described PI3K
inhibitors, but little selectivity within the PI3K family. Also blocks
autophagosome formation and potently inhibits DNA-PK/ATM with
IC50 of 16 nM and 150 nM. Phase 4.
BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR
inhibitor for p110/// and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7
nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown
to be poorly inhibitory to Akt and PDK1. Phase 1/2.
Page 1
Page 5
10 mg 50 mg
Size
10 mg 50 mg
Size
10 mg 50 mg
Size
KU59403 is a novel ATM inhibitor with IC50 of
3 nM.
S7166 KU59403 new
S2817 Torin 2
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM;
800-fold greater selectivity for mTOR than PI3K and improved
pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50
of 28 nM/35 nM/118 nM, respectively.
Page 8
S
S
O N
O
O
N
H
O
N
N
CGK 733 is a potent and selective inhibitor of
ATM/ATR with IC50 of ~200 nM.
S7136 CGK 733 new
F
NO2
H
N
H
N
S
CCl3
HN O
Product Citations:
Am J Physiol Renal Physiol, 2011, 302(4): F466-76
Eukaryot Cell, 2012, 12(1): 12-22
10 mM/1 mL in DMSO
5 mg 100 mg 25 mg
Size
Data from [ Am J Physiol
Renal Physiol, 2011, 302(4):
F466-76 ]
OSU-03012 purchased from
Selleck
OSU-03012 is a potent inhibitor of
recombinant PDK-1 with IC50 of 5 M and
2-fold increase in potency over OSU-02067.
S1106 OSU-03012 (AR-12)
BI-D1870 is an ATP-competitive inhibitor of
S6 ribosome for RSK1/2/3/4 with IC50 of 31
nM/24 nM/18 nM/15 nM, respectively; 10- to
100-fold selectivity for RSK than MST2,
GSK-3, MARK3, CK1 and Aurora B.
S2843 BI-D1870
S6 Kinase Inhibitors
HO
F
F
N
H
N
N
N
N O
Size
BX912 is a potent and specific PDK1 inhibitor
with IC50 of 12 nM, 9- and 105- fold greater
selectivity for PKD1 than PKA and PKC,
respectively. In comparison to GSK3,
selectivity for PDK1 is 600-fold.
S1275 BX-912
PDK-1 Inhibitors
BX795 is a potent and specific PDK1 inhibitor
with IC50 of 6 nM, 140- and 1600-fold more
selective for PDK1 than PKA and PKC,
respectively. Meanwhile, in comparison to
GSK3 more than 100-fold selectivity
observed for PDK1.
S1274 BX-795
S1556 PHT-427
PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for
the PH domains of Akt and PDPK1) with Ki of 2.7 M and 5.2 M,
respectively.
GSK2334470 is a potent and highly selective
PDK1 inhibitor with IC50 of ~10 nM.
S7087 GSK2334470 new
N N
N
HN
N
H
N
NH2
O
NH
Page 10
Size
Size
14
Phone:+1-832-582-8158
www.selleckchem.com
P
I
3
K
/
A
k
t
/
m
T
O
R
S6 Kinase / AMPK / DNA-PK
FMK is a potent and selective inhibitor of p90
ribosomal protein S6 kinase RSK2 (wt) with
IC50 of 15 nM, > 600- and 200-fold selectivity
for RSK2 than the C436V and T493M
mutants.
S7064 FMK
AT7867
BI-D1870
PF-4708671
S1558
S2843
S2163
++
++
17 nM [IC50]
20 nM [Ki]
++ 31 nM [IC50] ++ 24 nM [IC50] ++ 18 nM [IC50] ++ 15 nM [IC50]
Cat.No. Inhibitor Name S6K1 RSK1 RSK2 RSK3 RSK4 Other
AKT3,AKT2,AKT1
S1558 AT7867
AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and
p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM,
respectively; little activity outside the AGC kinase family.
Page 10
50 mg 200 mg
Size
N
N
N
NH2
O F
HO
S1038 PI-103
NU7026 is a potent DNA-PK inhibitor with
IC50 of 0.23 M, 60-fold selective for DNA-PK
than PI3K and inactive against both ATM and
ATR.
S2893 NU7026
S1205 PIK-75
PIK-75 is a p110 inhibitor with IC50 of 5.8nM (200-foldmore potently
than p110), isoform-specific mutants at Ser773, and also potently
inhibits DNA-PK with IC50 of 2 nM.
S2622 PP-121
PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2,
Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM,
also inhibits DNA-PK with IC50 of 60 nM.
DNA-PK Inhibitors
S2638 NU7441 (KU-57788)
NU7441 is a highly potent and selective DNA-PK inhibitor with IC50
of 14 nM and also inhibits PI3K with IC50 of 5 M.
Page 2
Page 2
Page 3
Page 9
O
N
O
O
PF-4708671 is a cell-permeable inhibitor of
p70 ribosomal S6 kinase (S6K1 isoform) with
Ki/IC50 of 20 nM/160 nM, 400-fold greater
selectivity for S6K1 than S6K2, and 4- and
>20-fold selectivity for S6K1than MSK1 and
RSK1/2, respectively. First S6K1-specific
inhibitor to be reported.
S2163 PF-4708671
Licensed and Manufactured by Pfizer
HN
N
N
N
N
N
F
F
F
Size
Acadesine results in accumulation of ZMP,
which mimics the stimulating effect of AMP
onAMPK andAMPKK. Phase 3.
S1802 Acadesine
Phenformin hydrochloride is a hydrochloride
salt of phenformin that is an anti-diabetic
drug from the biguanide class.
S2542 Phenformin HCl
Product Citation:
Biochem Biophys Res Commun, 2013, ahead of print
AMPK Activators
A-769662 is a potent, reversible AMPK
activator with EC50 of 0.8 M, little effect on
GPPase/FBPase activity.
S2697 A-769662
N
H
N
H
NH
NH NH2
HCl
Size
10 mM/1 mL in DMSO 50 mg
Size
5 mg 100 mg 25 mg
Size
5 mg 200 mg 50 mg
Size
VEGFR
P
r
o
t
e
i
n

T
y
r
o
s
i
n
e

K
i
n
a
s
e
Protein Tyrosine Kinase
15
Product Citations:
Nature, 2011, 478(7369): 349-55
Cell Death Differ, 2010, 17(9): 1381-91
Data from[ Mol Cancer Ther,
2011, 11(3): 690-9 ]
Nintedanib purchased from
Selleck
BIBF1120 (Vargatef) is a potent triple
angiokinase inhibitor for VEGFR1/2/3,
FGFR1/2/3 and PDGFR/ with IC50 of 34
nM/13 nM/13 nM, 69 nM/37 nM/108 nM and
59 nM/65 nM. Phase 3.
S1010 Nintedanib (BIBF 1120)
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
Product Citation:
Surgery, 2012, 152(6): 1238-47
Data from[ Surgery, 2012,
152(6): 1238-47 ]
XL-184 purchased from
Selleck
XL184 (Cabozantinib) is a potent VEGFR2
inhibitor with IC50 of 0.035 nM and also
inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and
AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12
nM/11.3 nM/6 nM, 14.3 nM and 7 nM,
respectively.
S1119 XL-184 (Cabozantinib, BMS907351) VEGFR2selective
VEGFR Inhibitors
Phospho-RET(Tyr905)
Phospho-mTOR(Ser2448)
Phospho-4E-BP1(Thr37/46)
Phospho-p706S kinase
Phospho-ERK1/2(Thr42/Tyr44)
ERK1/2
actin
Phospho-Akt(Ser473)
Akt
RET
XL184 [M]
12h 24h
0 0.5 1 3 6 0 0.5 1 3 6
mTOR
4E-BP1
P70 S6 kinase
10 mM/1 mL in DMSO
5 mg 200 mg 10 mg
Size
16
Phone:+1-832-582-8158
www.selleckchem.com
P
r
o
t
e
i
n

T
y
r
o
s
i
n
e

K
i
n
a
s
e
VEGFR
Product Citations:
Cancer Res, 2011, 71(5): 1637-46
Dis Model Mech, 2010, 3(5-6): 343-53
Data from[ Dis Model Mech,
2010, 3(5-6): 343-53 ]
Sunitinib Malate purchased
fromSelleck
Sunitinib Malate (Sutent, SU11248) is a
multi-targeted RTK inhibitor targeting
VEGFR2 (Flk-1) and PDGFR with IC50 of 80
nM and 2 nM, and also inhibits c-Kit.
S1042 Sunitinib Malate VEGFR2selective
0.1%DMSO
s
ib
lin
g
v
h
l-/-
10M 676475 0.2M sunitinib
VEGFR2selective
Product Citations:
Cancer Cell, 2012, 22(5): 656-67
Exp Hematol, 2013, 41(4): 335-45
Data from[ Cancer Cell,
2012, 22(5): 656-67 ]
Ponatinib purchased from
Selleck
AP24534 is a novel, potent multi-target
inhibitor of Abl, PDGFR, VEGFR2, FGFR1
and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM,
2.2 nM and 5.4 nM, respectively.
S1490 Ponatinib (AP24534)
VEGFR2selective
Product Citations:
Blood, 2012, 120(19): 4104-15
Clin Cancer Res, 2011, 17(24): 7595-604
Data from[ Haematologica,
2012, 97(11): 1722-30 ]
Sorafenib purchased from
Selleck
SorafenibTosylate (Bay43-9006, Nexavar) is
a multikinase inhibitor of Raf-1, B-Raf and
VEGFR-2 with IC50 of 6 nM, 22 nM and 90
nM, respectively.
S1040 Sorafenib
10 mM/1 mL in DMSO
100 mg 5 mg
Size
Licensed by Pfizer
10 mM/1 mL in DMSO
50 mg 500 mg 100 mg
Size
Product Citations:
Hypertension, 2011, 58(1): 85-92
Antivir Res, 2010, 89(1): 64-70
Data from[ Hypertension,
2011, 58(1): 85-92 ]
Vandetanib purchased from
Selleck
Vandetanib (Zactima, ZD6474) is a potent
inhibitor of VEGFR2 with IC50 of 40 nM.
S1046 Vandetanib (ZD6474)
Product Citations:
Cancer Discov, 2013, 3(6): 636-47
J Virol, 2011, 85(5): 2296-303
Data from[ Cancer Discov,
2013, 3(6): 636-47 ]
Pazopanib HCl purchased
fromSelleck
Pazopanib Hydrochloride (GW786034,
Votrient, Armala) is a novel multi-target
inhibitor of VEGFR1, VEGFR2, VEGFR3,
PDGFR, FGFR, c-Kit and c-Fms with IC50 of
10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM
and 146 nM, respectively.
S1035 Pazopanib HCl (GW786034 HCl)
Product Citations:
Cancer Discov, 2012, 2(4): 344-55
Glia, 2012, 60(6): 936-47
Axitinib(AG-013736) is a multi-target inhibitor
of VEGFR1, VEGFR2, VEGFR3, PDGFR
and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3
nM, 1.6 nM and 1.7 nM, respectively.
S1005 Axitinib
2012, 2(4): 344-55 ]
Axitinib purchased from
Selleck
Licensed by Pfizer
10 mM/1 mL in DMSO
50 mg 100 mg
Size
10 mM/1 mL in DMSO
10 mg 100 mg 25 mg
Size
10 mM/1 mL in DMSO
25 mg 500 mg 100 mg
Size
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
E
E
E
E
L
L
C
C
C C
C
C
C
C
C C C
F
F
F
F F F F
F
F
F
F
F
F
F F
F
F
A
A
F
Kinase
Fibronectin
Cysteine Rich
Leucine Rich
EGF-Like
Acid box
Cadherin
IG-Like
Glycine Rich
EGFR
HER2/ErbB2
ErbB3
ErbB4
INSR
IGF-1R
IRR
FGFR PDGFR
CSF1R
Kit
Flk2
VEGFR Met
Ron
Sea
TrkA
TrkB
TrkC
Tie
Tie2
Eph
Eck
Eek
Erk
Elk
Ros Ret Ltk
Alk
PLC
PDK-1
Akt
PKC
IKK
Syk Bcr-Abl
Ras
Raf
c-Src
GSK-3
c-J un c-Fos
J AK ROCK
Rho PAK
J AK
STAT
PI3K/Akt
Pathway
NF-B
Pathway
MAPK
Pathway
Cell-Cycle
J AK/STAT
Pathway
HER2 inhibitors
Pan-FGFR inhibitors
Pan-PDGFR inhibitors Pan-VEGFR inhibitors
Pan-Trk receptor inhibitor c-RET inhibitors
ALK inhibitors
Tie-2 inhibitors
c-Met inhibitors c-Kit inhibitors IGF-1R inhibitors
Pan-ErbB inhibitors
Selective ErbB inhibitors
Selective Trk receptor inhibitor
Selective VEGFR inhibitors Selective PDGFR inhibitors
Lapatinib Ditosylate
Afatinib
AG-490
Lapatinib
Erlotinib(ErbB1/EGFR)
Gefitinib(ErbB1/EGFR)
CP-724714(HER2/ErbB2)
BGJ398
Imatinib BIBF1120
BMS-754807 Danusertib
TAE684
Tie2 kinase inhibitor
Crizotinib Crizotinib Linsitinib
GSK1904529A
NVP-ADW742
NVP-AEW541
BMS-536924
GSK1838705A
Amuvatinib
OSI-930
Dasatinib
Sunitinib Malate
Imatinib Mesylate
Foretinib
PHA-665752
SU11274
PF-04217903
XL-184
XL-184 free base
MGCD-265
CH5424802
GSK1838705A
Crizotinib
TG101209
Amuvatinib GW441756(TrkA)
Pazopanib
Axitinib
ZM 306416(VEGFR1)
XL-184(VEGFR2)
Vandetanib(VEGFR2)
SAR131675(VEGFR3)
PP-121
Crenolanib(PDGFR)
Sunitinib Malate(PDGFR)
BIBF1120
CP 673451(PDGFR)
AZD4547
BIBF1120
PD173074(FGFR1)
Ponatinib(FGFR1)
Selective FGFR inhibitors
CP-724714
Mubritinib
Neratinib
AZD8931
Afatinib
17
VEGFR
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VEGFR2selective
Product Citations:
Science, 2011, 331(6019): 912-16
PLoS Genet, 2012, 8(2): e1002500
Mol Cell Proteomics, 2012, 11(9): 745-57
Data from[ Science, 2011,
331(6019): 912-16 ]
PD173074 purchased from
Selleck
PD173074 is a potent FGFR1 inhibitor with
IC50 of ~25 nM and also inhibits VEGFR2 with
IC50 of 100-200 nM, ~1000-fold selectivity
over PDGFR and c-Src.
S1264 PD173074
Regorafenib (BAY 73-4506, Fluoro-Sorafenib)
is a multi-target inhibitor for VEGFR1,
VEGFR2, VEGFR3, PDGFR, Kit, RET and
Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22
nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
S1178 Regorafenib (BAY 73-4506)
Product Citations:
Nat Genet, 2012, 44(8): 852-60
Cancer Res, 2011, 71(15): 5255-64
Data from[ Nat Genet, 2012,
44(8): 852-60 ]
Foretinib purchased from
Selleck
Foretinib (GSK1363089, XL880) is an
ATP-competitive inhibitor of HGFR and
VEGFR, mostly for Met and KDR with IC50 of
0.4 nM and 0.9 nM. Less potent against Ron,
Flt-1/3/4, Kit, PDGFR/ and Tie-2, and little
activity to FGFR1 and EGFR. Phase 2.
S1111 Foretinib (GSK1363089)
pAXL
tAXL
GAPDH
P
a
re
n
ta
l
V
e
c
to
r
A
X
L
W
T
A
X
L
L
6
2
0
M
A
X
L
K
D
K
5
6
7
R
V
e
c
to
r
A
X
L
W
T
A
X
L
L
6
2
0
M
A
X
L
K
D
K
5
6
7
R
XL880(1M) :
- +
Product Citation:
Hepatology, 2012, 56(6): 2363-74
RAF265 (CHIR-265) is a potent selective
inhibitor of C-Raf/B-Raf/B-Raf
V600E
with IC50 of
3-60 nM, and exhibits potent inhibition on
VEGFR2 phosphorylation with EC50 of 30nM.
Phase 2.
S2161 RAF265 (CHIR-265) VEGFR2selective
Licensed by Pfizer
H
N
O
H
N
O
F
F
O
N
O
O
N
O
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
Size
Product Citations:
Haematologica, 2011, 96(6): 922-26
Mol Cancer Ther, 2012, 11(3): 690-9
Data from[ Haematologica,
2011, 96(6): 922-26 ]
Dovitinib purchased from
Selleck
Dovitinib (TKI258, CHIR258) is a
multitargeted RTK inhibitor, mostly for class
III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also
potent to class IV (FGFR1/3) and class V
(VEGFR1-4) RTKs with IC50 of 8-13 nM, less
potent to InsR, EGFR, c-Met, EphA2, Tie2,
IGFR1 and HER2. Phase 4.
S1018 Dovitinib (TKI-258, CHIR-258)
Product Citation:
Mol Cancer Ther, 2011, 10: 1028-35
Data from[ J Pharmacol Exp
Ther, 2012, 341(2): 386-95 ]
Cediranib purchased from
Selleck
Cediranib (AZD2171) is a highly potent
VEGFR(KDR) inhibitor with IC50 of <1 nM,
also inhibits Flt1/4 with IC50 of 5 nM/3 nM,
similar activity against c-Kit and PDGFR,
36-, 110-fold and >1000-fold selective more
for VEGFR than PDGFR-, CSF-1R and Flt3,
Phase 2/3.
S1017 Cediranib (AZD217)
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
Product Citation:
Exp Eye Res, 2013, 112: 125-33
Data from[ Exp Eye Res,
2013, 112: 125-33 ]
Tivozanib purchased from
Selleck
Tivozanib (AV-951, KRN-951) is a potent and
selective VEGFR inhibitor for VEGFR1/2/3
with IC50 of 0.21 nM/0.16 nM/0.24 nM, and
also inhibits PDGFR and c-Kit, low activity
observed against FGFR-1, Flt3, c-Met EGFR
and IGF-1R. Phase 3.
S1207 Tivozanib (AV-951)
10 mM/1 mL in DMSO
5 mg 50 mg 10 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg 25 mg
Size
Cediranib Concentration (g/ml)
0.1
0
2
4
6
8
10
12
14
1 100 10
18
Phone:+1-832-582-8158
www.selleckchem.com
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VEGFR
10 mM/1 mL in DMSO
10 mg 100 mg 50 mg
Size
Product Citations:
Mol Cell Proteomics, 2012, 11(6): M112
Liver Int, 2011, 32(3): 400-9
Data from[ Liver Int, 2011,
32(3): 400-9 ]
Linifanib purchased from
Selleck
Linifanib (ABT-869) is a novel, potent
ATP-competitive VEGFR/PDGFR inhibitor for
KDR, CSF-1R, Flt-1/3 and PDGFR with IC50
of 4 nM, 3 nM, 3 nM/4 nM and 66 nM
respectively, mostly effective in mutant
kinase-dependent cancer cells (i.e. FLT3).
Phase3.
S1003 Linifanib (ABT-869)
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
Product Citations:
J Clin Invest, 2011, 121(8): 3005-23
Circ Res, 2011, 108(10): 1190-8
Cell Res, 2011, 21(7): 1080-7
Data from[ Circ Res, 2011,
108(10): 1190-8 ]
Vatalanib 2HCl purchased
fromSelleck
Vatalanib (PTK787) is an inhibitor of
VEGFR2/KDR with IC50 of 37 nM, less potent
against VEGFR1/Flt-1, 18-fold against
VEGFR3/Flt-4. Phase 1/2.
S1101 Vatalanib (PTK787) 2HCl
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
MGCD-265 is a potent, multi-target and
ATP-competitive inhibitor of c-Met and
VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4
nM, respectively; also inhibits Ron and Tie2.
Phase 1/2.
S1361 MGCD-265
Medical University
MGCD-265 purchased from
Selleck
SAR131675 is a VEGFR3 inhibitor with
IC50/Ki of 23nM/12nM, about 50- and10-fold
more selective for VEGFR3 than VEGFR1/2,
little activity against Akt1, CDKs, PLK1,
EGFR, IGF-1R, c-Met, Flt2 etc.
S2842 SAR131675 VEGFR3selective
N N
O HN
O
NH2
HO
O
Size
by Dr. Yong-WeonYi from
Medical Center
Brivanib purchased from
Selleck
Brivanib is an ATP-competitive inhibitor
against VEGFR2 with IC50 of 25 nM,
moderate potency against VEGFR-1 and
FGFR-1, but >240-fold against PDGFR-.
Phase 3.
S1084 Brivanib (BMS-540215)
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
Product Citations:
Angiogenesis, 2012, 15(4): 569-80
Data from[ Angiogenesis,
2012, 15(4): 569-80 ]
TSU-68 purchased from
Selleck
SU6668 has greatest potency against
PDGFR autophosphorylation with Ki of 8 nM,
but also strongly inhibits Flk-1 and FGFR1
trans-phosphorylation, little activity against
IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2;
does not inhibit EGFR. Phase 3.
S1470 TSU-68 (SU6668)
10 mM/1 mL in DMSO
2 mg 100 mg 10 mg
Size
Product Citation:
PLoS One, 2013, 8(5): e64369
Data from[ PLoS One, 2013,
8(5): e64369 ]
E7080 purchased from
Selleck
E7080 (Lenvatinib) is a multi-target inhibitor,
mostly for VEGFR2(KDR)/VEGFR3(Flt-4)
with IC50 of 4 nM/5.2 nM, less potent against
VEGFR1/Flt-1, ~10-fold more selective for
VEGFR2/3 against FGFR1, PDGFR/.
Phase 3.
S1164 E7080 (Lenvatinib)
Control Len Dex Len
+Dex
Len
+Bor +Dex
Len
+Bor
Bor
T
F
m
R
N
A
ra
tio
n
GAPDH
TF (283 bp)
Size
19
VEGFR
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Product Citation:
Cardiovasc Res, 2011, 91(3): 402-11
Data from[ Cardiovasc Res,
2011, 91(3): 402-11 ]
Motesanib Diphosphate
purchased fromSelleck
Motesanib Diphosphate (AMG-706) is a
potent ATP-competitive inhibitor of
VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM,
respectively; similar activity against Kit,
~10-fold more selective for VEGFR than
PDGFR and Ret. Phase 1/2.
S1032 Motesanib Diphosphate (AMG-706)
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
Product Citation:
J Virol, 2010, 85(5): 2296-303
Pazopanib is a potent and selective
multi-targeted receptor tyrosine kinase
inhibitor of VEGFR1, VEGFR2, VEGFR3,
PDGFR-/, and c-Kit.
S3012 Pazopanib
Product Citations:
Haematolog, 2011, 96(6): 922-6
Mol Cancer Ther, 2011, 10: 1028-35
Data from[ Brit J Cancer,
2010, 104(1): 75-82 ]
Dovitinib Dilactic acid
DovitinibDilactic acid(TKI258Dilactic acid) is
a multitargetedRTK inhibitor, mostlyfor class
III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also
potent to class IV (FGFR1/3) and class V
(VEGFR1-4) RTKs with IC50 of 8-13 nM, less
potent to InsR, EGFR, c-Met, EphA2, Tie2,
IGFR1 and HER2. Phase 4.
S2769 Dovitinib Dilactic acid (TKI258 Dilactic acid)
NVP-BHG712 is a specific EphB4 inhibitor
with ED50 of 25 nM that discriminates
between VEGFR and EphB4 inhibition; also
shows activity against c-Raf, c-Src and c-Abl
with IC50 of 0.395 M, 1.266 M and 1.667
M, respectively.
S2202 NVP-BHG712
NVP-BHG712 purchased
fromSelleck
Medical University
ENMD-2076 purchased from
Selleck
ENMD-2076 has selective activity against
Aurora A and VEGFR(Flt3) with IC50 of 14 nM
and 1.86 nM, 25-fold selective to Aurora B
and less potent to VEGFR2/KDR and
VEGFR3, FGFR1 and FGFR2 and PDGFR.
Phase 2.
S1181 ENMD-2076
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
Golvatinib (E7050) is a dual c-Met and
VEGFR-2 inhibitor with IC50 of 14 nM and 16
nM, does not inhibit bFGF-stimulated HUVEC
growth (up to 1000 nM). Phase 1/2.
S2859 Golvatinib (E7050) VEGFR2selective
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
CYC116 purchased from
Selleck
CYC116 is a potent inhibitor of Aurora A/B
with Ki of 8.0 nM/9.2 nM, less potent to
VEGFR2 with Ki of 44 nM, with 50-fold more
potent than CDKs, not active against PKA,
Akt/PKB, PKC, no effect on GSK-3/, CK2,
Plk1 and SAPK2A. Phase 1.
S1171 CYC116
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mg 500 mg 25 mg
Size
S O O
NH2
N
H
N
N
N N
N
F H
N
O
H
N
O F O
N N
H
N
O
N
N
0
20
40
60
80
100
120
140
160
180
C
X
C
R
4
e
x
p
re
s
s
io
n
(%
C
o
n
tro
l)
CtrlCM + - - - -
+ +
+
+
+
+
+ -
- - - -
- - - -
- - - -
VEGFCM
AMG
VEDFR2-1
MAZ
Size
Size
25 mg 100 mg
Size
20
Phone:+1-832-582-8158
www.selleckchem.com
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VEGFR
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
Medical Center
Selleck
OSI-930 is a potent inhibitor of Kit, KDR and
CSF-1R with IC50 of 80 nM, 9 nM and 15 nM,
respectively; modest activity to Flt-1, c-Raf
and Lck, and low activity against PDGFR/,
Flt-3 andAbl. Phase 1.
S1220 OSI-930
Product Citation:
Biochem Pharmacol, 2012, 84(6): 766-74
Data from[ Mol Cell
Proteomics, 2012, 11(9):
745-57 ]
Ki8751 purchased from
Selleck
Ki8751 is a potent and selective inhibitor of
VEGFR2 with IC50 of 0.9 nM, >40-fold
selective for VEGFR2 than c-Kit, PDGFR
and FGFR-2, little activity to EGFR, HGFR
and InsR.
S1363 Ki8751
Product Citations:
J Exp Med, 2012, 209(3): 507-20
VEGFR2selective
10 mM/1 mL in DMSO
10 mg 50 mg
Size
by one customer
Brivanib alaninate
Brivanib alaninate (BMS-582664) is the
prodrug of BMS-540215, anATP-competitive
inhibitor against VEGFR2 with IC50 of 25 nM.
S1138 Brivanib alaninate (BMS-582664)
AEE788 is a potent inhibitor of EGFR and
HER2/ErbB2 with IC50 of 2nM and6nM, less
potent to VEGFR2/KDR, c-Abl, c-Src, and
Flt-1, does not inhibit Ins-R, IGF-1R, PKC
and CDK1/cyclin B. Phase 1/2.
S1486 AEE788 (NVP-AEE788)
KRN 633 is an ATP-competitive inhibitor of
VEGFR1/2/3 with IC50 of 170 nM/160 nM/125
nM, weakly inhibits PDGFR-/ and c-Kit,
does not block the phosphorylation of
FGFR-1, EGFR or c-Met in cell.
S1557 KRN 633
Apatinib (YN968D1) is an orally bioavailable,
selective VEGFR2 inhibitor with IC50 of 1 nM.
S2221 Apatinib VEGFR2selective
ZM-323881 is a potent and selective
VEGFR2 inhibitor with IC50 of <2 nM, almost
no activity against VEGFR1, PDGFR,
FGFR1, EGFR and ErbB2.
S2896 ZM 323881 HCl VEGFR2selective
BMS794833 is a potent ATP competitive
inhibitor of Met/VEGFR2 with IC50 of 1.7
nM/15 nM, also inhibits Ron, Axl and Flt3 with
IC50 of <3 nM; a prodrug of BMS-817378.
Phase 1.
S2201 BMS 794833 VEGFR2selective
Aderivative of Raf265, however, the effects of
this derivative are not known.
S2200 Raf265 derivative VEGFR2selective
Semaxanib (SU5416) is a potent and
selective VEGFR(Flk-1/KDR) inhibitor with
IC50 of 1.23 M, 20-fold more selective for
VEGFR than PDGFR, lack of activity
against EGFR, InsR and FGFR. Phase 3.
S2845 Semaxanib (SU5416)
ZM-306416 is a VEGFR (Flt and KDR)
inhibitor for VEGFR1 with IC50 of 0.33 M, but
also found to inhibit EGFR with IC50 of <10nM.
S2897 ZM 306416 VEGFR1selective
Product Citation:
Clin Cancer Res, 2013, ahead of print
N
H
O
N
H
N
HN
N
O
O
F Cl
HN
N
N
O
F
OH
HCl
Size
Size
Size
Size
Size
Size
Size
10 mg 50 mg 100 mg
Size
Telatinib(BAY 57-9352) is a potent inhibitor of
VEGFR2/3, c-Kit and PDGFR with IC50 of 6
nM/4 nM, 1 nM and 15 nM, respectively.
Phase 2.
S2231 Telatinib
21
VEGFR
P
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K
i
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a
s
e
BIBF1120
Cediranib
Dovitinib
Motesanib Diphosphate
Sunitinib Malate
Vandetanib
Brivanib
XL-184
Brivanib alaninate
E7080
CYC116
Regorafenib
ENMD-2076
Tivozanib
PD173074
MGCD-265
Ki8751
AEE788
Ponatinib
KRN 633
BMS 794833
Apatinib
Telatinib
SAR131675
Semaxanib
Golvatinib
ZM 323881 HCl
ZM 306416
Pazopanib
Cabozantinib malate
S1010
S1017
S1018
S1032
S1042
S1046
S1084
S1119
S1138
S1164
S1171
S1178
S1181
S1207
S1264
S1361
S1363
S1486
S1490
S1557
S2201
S2221
S2231
S2842
S2845
S2859
S2896
S2897
S3012
S4001
++
+++
++++
+
++
++
++++
+++
+
+++
+++
34 nM [IC50]
10nM [IC50]
2 nM [IC50]
380 nM [IC50]
22 nM [IC50]
13 nM [IC50]
0.21 nM [IC50]
3 nM [IC50]
170 nM [IC50]
0.33 M [IC50]
10 nM [IC50]
+++
++++
++
++++
+
++
++
++++
++
+++
++
+++
+
++++
+
+++
++++
+
+++
+
++
+++
+++
++
++
+++
++
++++
5 nM [IC50]
0.5 nM [IC50]
13 nM [IC50]
3 nM [IC50]
80 nM [IC50]
40 nM [IC50]
25 nM [IC50]
0.035 nM [IC50]
25 nM [IC50]
4 nM [IC50]
44 nM [IC50]
4.2 nM [IC50]
58.2 nM [IC50]
0.16 nM [IC50]
100-200 nM [IC50]
3 nM [IC50]
0.9 nM [IC50]
77 nM [IC50]
1.5 nM [IC50]
160 nM [IC50]
15 nM [IC50]
2.43 nM [IC50]
6 nM [IC50]
1.04 M [IC50]
16 nM [IC50]
<2 nM [IC50]
30 nM [IC50]
0.035 nM [IC50]
+++
+++
+++
+++
++
++++
+++
+
+++
++
++
5 nM [IC50]
8 nM [IC50]
6 nM [IC50]
5.2 nM [IC50]
46 nM [IC50]
0.24 nM [IC50]
4 nM [IC50]
125 nM [IC50]
4 nM [IC50]
20 nM [IC50]
47 nM [IC50]
Cat.No. Inhibitor Name VEGFR1 VEGFR2 VEGFR3 Other
FGFR-2, PDGFR-, PDGFR-,
FGFR-3, FGFR-1
FLT3, FGFR-1, PDGFR-, c-Kit,
PDGFR-, FGFR-3
c-Kit, c-RET, FLT4, c-Met, Axl,
FLT1, FLT3, Tie-2
PDGFR-, FGFR-1, PDGFR-
Aurora A, Aurora B
A-Raf, c-Kit, c-RET, PDGFR-
PDGFR-, c-Kit
FGFR-1
Tie-2, c-Met
PDGFR-, c-Kit, FGFR-2
ERBB1(EGFR), HER2,
ERBB2(Her2)
PDGFR-, c-Kit, PDGFR-,
FGFR-1
FLT3, c-Met, c-Kit, FLT4, Axl,
c-RET, FLT1, Tie-2
SRC, FGFR-1, PDGFR-, Abl
PDGFR-, PDGFR-
c-Met
c-Kit, PDGFR-
c-Met
Aurora A, Aurora B, FLT4, FLT3
c-Kit, c-RET
PDGFR-
FGFR-1
ENMD-2076 L-(+)-Tartaric acid is the tartaric
acid of ENMD-2076, selective activity against
Aurora A and VEGFR(Flt3) with IC50 of 14 nM
and 1.86 nM, 25-fold more selective for
Aurora A than Aurora B and less potent to
VEGFR2/KDR and VEGFR3, FGFR1 and
FGFR2 and PDGFR. Phase 2.
S2018 ENMD-2076 L-(+)-Tartaric acid
N
HN
NH
N
N
N
N
L-(+)-Tartaric acid
E) 934353-76-1
R) 934353-77-2
Cabozantinib malate is the malate of
Cabozantinib, a potent VEGFR2 inhibitor with
IC50 of 0.035 nM and also inhibits c-Met, Ret,
Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3
nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3
nM and 7 nM, respectively.
S4001 Cabozantinib malate (XL184) VEGFR2selective
N O
O
O
N
H
O
N
H
O
F
OH
O
OH
O
OH
Size
10 mg 50 mg
Size
22
Phone:+1-832-582-8158
www.selleckchem.com
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EGFR
EGFRselective
Product Citations:
Nat Genet, 2012, 44(8): 852-60
Cell, 2012, 151(5): 937-50
Cell Metab, 2013, 17(6): 1000-8
44(8): 852-60 ]
Erlotinib HCl purchased from
Selleck
Erlotinib HCl (OSI-744, CP358774,
NSC718781) is an EGFR inhibitor with IC50 of
2 nM, >1000-fold more sensitive for EGFR
than human c-Src or v-Abl. Phase 3.
S1023 Erlotinib HCl (OSI-744)
EGFR Inhibitors
200 mg 10 mg 50 mg
Size
CI-1033 is a pan-ErbB inhibitor for EGFR and
ErbB2 with IC50 of 1.5 nM and 9.0 nM, no
activity to PDGFR, FGFR, InsR, PKC, or
CDK1/2/4. Phase 3.
S1019 Canertinib (CI-1033)
Data from[ Carcinogenesis,
2010, 31(11): 1948-55 ]
Canertinib purchased from
Selleck
Product Citation:
Cancer Discov, 2012, 2(5): 458-71
EGFRselective
Data from[ Biochem
Biophys Res Commun,
2013, 435(4): 533-9 ]
AG-490 purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 25 mg
Size
AG-490 (Tyrphostin B42) is an inhibitor of
EGFR with IC50 of 0.1 M, 135-fold more
selective for EGFR versus ErbB2, also
inhibits JAK2 with no activity to Lck, Lyn, Btk,
Syk and Src.
S1143 AG-490
Product Citation:
Prostate, 2013, 73(3): 267-77
CNX-2006 is a novel irreversible
mutant-selective EGFR inhibitor with IC50 of
<20 nM.
S7206 CNX-2006 EGFRselective
new
PD168393 is an irreveasible EGFR inhibitor
with IC50 of 0.70 nM, irreversibly alkylate
Cys-773; inactive against insulin, PDGFR,
FGFR and PKC.
S7039 PD168393 EGFRselective
new
N
N
HN
F3C
N
H
HN
O
O
H
N
N
F
N
N
N
H
O
HN Br
10 mM/1 mL in DMSO
100 mg 500 mg
Size
RANKL
AG490
pSer727-STAT3
STAT3
pAkt
Akt
pERK
ERK
-actin
0 5 15 45 0 5 15 45 (min)
Size
5 mg 25 mg
Size
Data from[ Nature, 2012,
483(7387): 100-3 ]
Gefitinib purchased from
Selleck
Gefitinib (Iressa, ZD-1839) is an EGFR
inhibitor for Tyr1173, Tyr992, Tyr1173 and
Tyr992 in the NR6wtEGFR and NR6W cells
with IC50 of 37 nM, 37nM, 26 nM and 57 nM,
respectively.
S1025 Gefitinib (ZD1839) EGFRselective
Product Citations:
Nature, 2012, 483(7387): 100-3
Cell, 2012, 151(5): 937-50
Mol Syst Biol, 2011, 7: 486
10 mM/1 mL in DMSO
100 mg 250 mg
Size
Data from[ Eur J Cancer,
2012, 49(6): 1458-66 ]
Afatinib purchased from
Selleck
BIBW2992 irreversibly inhibits EGFR/HER2
including EGFR(wt), EGFR(L858R),
EGFR(L858R/T790M) and HER2 with IC50 of
0.5 nM, 0.4 nM, 10 nM and 14 nM,
respectively; 100-fold more active against
Gefitinib-resistant L858R-T790M EGFR
mutant. Phase 3.
S1011 Afatinib (BIBW2992)
Product Citations:
Clin Cancer Res, 2012, 18(6): 1663-71
Eur J Cancer, 2012, 49(6): 1458-66
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
pHER2
Sham 100 200 100 200
2.5 10
Radiation (Gy)
Afatinib (nM)
HER2
pEGFR
EGFR
pAkt
Akt
-actin
100 200
23
EGFR
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Data from[ Biochem
Pharmacol , 2011, 82(10):
1457-66 ]
Lapatinib Ditosylate (GW572016, GW2016,
Tykerb, Tyverb) is a potent EGFR and ErbB2
inhibitor with IC50 of 10.8 nM and 9.2 nM,
respectively.
S1028 Lapatinib Ditosylate (GW-572016)
Product Citations:
Proc Natl Acad Sci U S A, 2012, 109(17): 6584-9
Oncogene, 2013, 32(37): 4331-42
Biochem Pharmacol , 2011, 82(10): 1457-66
2013, 3(2): 224-37 ]
Neratinib purchased from
Selleck
Neratinib (HKI-272) is a highly selective
HER2 and EGFR inhibitor with IC50 of 59 nM
and 92 nM; weakly inhibits KDR and Src, no
significant inhibition to Akt, CDK1/2/4, IKK-2,
MK-2, PDK1, c-Raf and c-Met. Phase 3.
S2150 Neratinib (HKI-272)
Product Citations:
Cancer Discov, 2012, 2(5): 458-71
Cancer Discov, 2013, 3(2): 168-81
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
10 mM/1 mL in DMSO
100 mg 5 mg 25 mg
Size
CP-724,714 is a potent, selective inhibitor of
HER2/ErbB2 with IC50 of 10 nM, >640-fold
selectivity against EGFR, IR, IRG-1R,
PDGFR, VEGFR2, Abl, Src, c-Metetc. Phase2.
S1167 CP-724714 HER2selective
by Reto Baumann fromETH
Zurich
CP-724714 purchased from
Selleck
CUDC-101 is a potent multi-target inhibitor
targeting HDAC, EGFR and HER2 with IC50 of
4.4 nM, 2.4 nM, and 15.7 nM, inhibits both
class I/II HDACs, but not class III, Sir-type
HDACs. Phase 1.
S1194 CUDC-101
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
Medical University
CUDC-101 purchased from
Selleck
10 mM/1 mL in DMSO
25 mg 100 mg
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
2012, 11(10): 2149-57 ]
WZ4002 purchased from
Selleck
Product Citations:
Clin Cancer Res, 2012, 18(6): 1663-71
Mol Cancer Ther, 2012, 11(10): 2149-57
WZ4002 is a novel, mutant-selective EGFR
inhibitor for EGFR(L858R)/(T790M) with IC50
of 2 nM/8 nM; does not inhibit ERBB2
phosphorylation (T798I).
S1173 WZ4002 EGFRselective
100 mg 5 mg 25 mg
Size
Medical University
PD153035 HCl purchased
fromSelleck
EGFRselective
PD153035is a potent andspecific inhibitor of
EGFR with Ki and IC50 of 5.2 pM and 29 pM;
little effect noted against PGDFR, FGFR,
CSF-1, InsR and Src.
S1079 PD153035 HCl
Product Citation:
Antivir Res, 2010, 89(1): 64-70
AZD8931 is a reversible, ATP competitive
inhibitor of EGFR, ErbB2 and ErbB3 with IC50
of 4 nM, 3 nM and 4 nM, more potent than
Gefitinib or Lapatinib against NSCLC cell,
100-fold more selective for the ErbB family
than MNK1 and Flt. Phase 1/2.
S2192 AZD8931
EGFRselective
Pelitinib (EKB-569) is a potent irreversible
EGFR inhibitor with IC50 of 38.5 nM. Phase 2.
S1392 Pelitinib (EKB-569)
Product Citation:
J Immunol, 2012, 188(9): 4581-9
Data from[ J Immunol, 2012,
188(9): 4581-9 ]
Pelitinib purchased from
Selleck
10 mM/1 mL in DMSO
100 mg 5 mg 25 mg
Size
Size
24
Phone:+1-832-582-8158
www.selleckchem.com
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EGFR
100 mg
BMS-599626 (AC480) is a selective and
efficacious inhibitor of HER1 and HER2 with
IC50 of 20 nM and 30 nM, ~8-fold less potent
to HER4, >100-fold to VEGFR2, c-Kit, Lck,
MET etc. Phase 1.
S1056 AC480 (BMS-599626)
Product Citation:
Cancer Cell, 2012, 22(5): 656-67
10 mM/1 mL in DMSO
5 mg 25 mg
Size
2012, 22(5): 656-67 ]
AC480 purchased from
Selleck
TAK-285 is a novel dual HER2 and
EGFR(HER1) inhibitor with IC50 of 17 nM and
23 nM, >10-fold selectivity for HER1/2 than
HER4, less potent to MEK1/5, c-Met, Aurora
B, Lck, CSK etc. Phase 1.
S2784 TAK-285
AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2
nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1,
does not inhibit Ins-R, IGF-1R, PKC and CDK1/cyclin B. Phase 1/2.
N
N
N
HN
NH
O
HO
Cl
O
F F
F
Page 20
EGFRselective
WZ8040 is a novel mutant-selective
irreversible EGFR
T790M
inhibitor, does not
inhibit ERBB2 phosphorylation (T798I).
S1179 WZ8040
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Medical Center
Selleck
Lapatinib, used in the form of Lapatinib
Ditosylate, is a potent EGFR and ErbB2
respectively.
S2111 Lapatinib
Product Citations:
Cancer Cell, 2012, 21(4): 488-503
ACS Nano, 2012, 6(10): 8525-35
Data from[ Mol Oncol, 2013,
7(3): 392-401 ]
Lapatinib purchased from
Selleck
PF299804 is a potent, irreversible pan-ErbB
inhibitor, mostly to EGFR with IC50 of 6 nM,
effective against NSCLCs with EGFR or
ERBB2 mutations (resistant to gefitinib) as
well as those harboring the EGFR T790M
mutation. Phase 2.
S2727 Dacomitinib (PF299804, PF299)
EGFRselective
AG-1478 (TyrphostinAG-1478) is a selective
EGFR inhibitor with IC50 of 3 nM, almost no
activity on HER2-Neu, PDGFR, Trk, Bcr-Abl
and InsR.
S2728 AG-1478 (Tyrphostin AG-1478)
Product Citation:
J Pharmacol Exp Ther, 2012, 341(2): 386-95
HER2selective
ARRY-380 is a potent and selective HER2
inhibitor with IC50 of 8 nM, equipotent against
truncatedp95-HER2, 500-foldmore selective
for HER2 versus EGFR. Phase 1.
S2752 Arry-380
N
N
HN Cl
O
F
O
NH
S
O O
10 mM/1 mL in DMSO
100 mg 5 mg 25 mg
Size
EGFRselective
Product Citation:
Carcinogenesis, 2010, 31(11): 1948-55
Data from[ Sci Pharm, 2012,
80(3): 633-46 ]
Selleck
OSI-420 is the active metabolite of Erlotinib
(EGFR inhibitor with IC50 of 2 nM).
S2205 OSI-420
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
EGFRselective
WZ3146 is a mutant-selective irreversible
inhibitor of EGFR(L858R) and
EGFR(E746_A750) with IC50 of 2 nM and 2
nM; does not inhibit ERBB2 phosphorylation
(T798I).
S1170 WZ3146
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Medical University
Selleck
5 mg 10 mg 100 mg
Size
5 mg 50 mg 200 mg
Size
Size
Size
25
EGFR
P
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Afatinib
CI-1033
Gefitinib
BMS-599626
PD153035 HCl
AG-490
CP-724714
WZ3146
WZ4002
CUDC-101
Pelitinib
AEE788
Lapatinib
S1011
S1019
S1025
S1028
S1056
S1079
S1143
S1167
S1170
S1173
S1194
S1392
S1486
S2111
++++
+++
++
++
++
++++
+++
++
+++
+++
+++
++
+++
++
0.5 nM [IC50]
1.5 nM [IC50]
37 nM [IC50]
10.8 nM [IC50]
20 nM [IC50]
29 pM [IC50]
0.1 M [IC50]
6.4 M [IC50]
2 nM [IC50]
2 nM [IC50]
2.4 M [IC50]
38.5 nM [IC50]
2 nM [IC50]
10.8 nM [IC50]
++
+++
+++
++
+
+++
++
+++
+++
14 nM [IC50]
9 nM [IC50]
9.2 nM [IC50]
30 nM [IC50]
13.5 M [IC50]
10 nM [IC50]
15.7 M [IC50]
6 nM [IC50]
9.2 nM [IC50]
Cat.No. Inhibitor Name ERBB1(EGFR) ERBB2(Her2) ERBB3(Her3) ERBB4(Her4) Other
HER2
HER2
HER2
HER2
J AK2
HER2
HER2
VEGFR2, HER2
HER2
EGFRselective
WHI-P154 is a potent JAK3 inhibitor with IC50
of 1.8 M, no activity against JAK1 or JAK2,
also inhibits EGFR, Src, Abl, VEGFR and
MAPK, prevents Stat3, but not Stat5
phosphorylation.
S2867 WHI-P154
N
N
O
O
HN OH
Br
WHI-P154 purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 50 mg
Size
AST-1306 purchased from
Selleck
AST-1306 is a novel irreversible inhibitor of
EGFR and ErbB2 with IC50 of 0.5 nM and 3
nM, also effective in mutation
EGFR(T790M/L858R), more potent to
ErbB2-overexpressing cells, 3000-fold
selective for ErbB family than other kinases.
S2185 AST-1306
Varlitinib purchased from
Selleck
ARRY334543 is a selective and potent
ErbB1(EGFR) and ErbB2(HER2) inhibitor
with IC50 of 7 nM and 2 nM, respectively.
Phase 2.
S2755 Varlitinib
AG-18 inhibits EGFR with IC50 of 35 M.
S8009 AG 18
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
Desmethyl Erlotinib (CP-473420) is a free
base of OSI-420, an active metabolite of
Erlotinib (EGFR inhibitor with IC50 of 2 nM).
S2826 Desmethyl Erlotinib (CP-473420, OSI-774) EGFRselective
EGFRselective
N
N
NH
O
O
O
HO
Size
26
Phone:+1-832-582-8158
www.selleckchem.com
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EGFR / PDGFR
AST-1306
AZD8931
OSI-420
Dacomitinib
AG-1478
Arry-380
TAK-285
Desmethyl Erlotinib
WHI-P154
Tyrphostin 9
Icotinib
AG 18
S2185
S2192
S2205
S2727
S2728
S2752
S2784
S2826
S2867
S2895
S2922
S8009
++++
+++
+++
+++
+++
+++
++
+++
+++
+
+++
+
0.5 nM [IC50]
4 nM [IC50]
2 nM [IC50]
6 nM [IC50]
3 nM [IC50]
4 nM [IC50]
23 nM [IC50]
2 nM [IC50]
4 nM [IC50]
460 M [IC50]
5 nM [IC50]
35 M [IC50]
+++
++
+++
++
3 nM [IC50]
45.7 nM [IC50]
8 nM [IC50]
17 nM [IC50]
+++
Cat.No. Inhibitor Name ERBB1(EGFR) ERBB2(Her2) ERBB3(Her3) ERBB4(Her4) Other
4 nM [IC50]
73.7 nM [IC50] +
HER2
HER2
HER2
SRC, JAK3
S1042 Sunitinib Malate
PDGFR Inhibitors
Imatinib is a multi-target inhibitor of v-Abl,
c-Kit and PDGFR with IC50 of 0.6 M, 0.1 M
and 0.1 M, respectively.
S2475 Imatinib
Product Citations:
Cell Stem Cell, 2012, 10(2): 210-7
Clin Cancer Res, 2013, ahead of print
Data from[ FASEB J, 2011,
25(10): 3661-73 ]
Imatinib purchased from
Selleck
Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor
targeting VEGFR2 (Flk-1) and PDGFR with IC50 of 80nM and2nM,
and also inhibits c-Kit.
10 mM/1 mL in DMSO
250 mg 500 mg
Size
Page 16
S2622 PP-121
PP-121is a multi-targetedinhibitor of PDGFR, Hck, mTOR, VEGFR2,
Src and Abl with IC50 of 2nM, 8nM, 10nM, 12nM, 14nM and18nM,
also inhibits DNA-PK with IC50 of 60 nM.
Page 9
S1040 Sorafenib
Crenolanib (CP-868596) is a potent and
selective inihibitor of PDGFR/ with Kd of 2.1
nM/3.2 nM nM, also potently inhibits FLT3,
sensitive to D842V mutation not V561D
mutation, >100-fold more selective for
PDGFR than c-Kit, VEGFR-2, TIE-2,
FGFR-2, EGFR, erbB2, and Src.
Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor
of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM,
respectively.
S2730 Crenolanib (CP-868596)
Page 16
CP 673451 is a highly selective PDGFR
inhibitor, equipotent to PDGFR-/ with IC50
of 10 nM/1 nM, >250-fold more selective for
PDGFR than c-Kit, VEGFR1/2, Tie-2,
FGFR-2.
S1536 CP 673451
N
O
O
N
N
N
NH2
Product Citations:
Leukemia, 2013, 27(4): 932-40
Oncogene, 2012, ahead of print
Imatinib Mesylate is an orally bioavailability
mesylate salt of Imatinib, which is a
multi-target inhibitor of v-Abl, c-Kit and
PDGFR with IC50 of 0.6 M, 0.1 M and 0.1 M,
respectively.
S1026 Imatinib Mesylate (STI571)
Data from[ J Invest
Dermatol, 2012, 132(7):
1850-9 ]
Imatinib Mesylate purchased
fromSelleck
10 mM/1 mL in DMSO
100 mg 250 mg
Size
Size
Size
new
Tyrphostin 9 is firstly designed as an EGFR
inhibitor with IC50 of 460 M, but is also found to
be more potent to PDGFR with IC50 of 0.5 M.
S2895 Tyrphostin 9 EGFRselective
Size
Icotinib is a potent and specific EGFR
inhibitor with IC50 of 5 nM, including the
EGFR, EGFR(L858R), EGFR(L861Q),
EGFR(T790M) and EGFR(T790M, L858R).
Phase 4.
S2922 Icotinib EGFRselective
10 mM/1 mL in DMSO 5mg 50 mg 200 mg
Size
Size
HO
N
N
HO
HO
N
N
HN
N
N O
O
O
O
PDGFR
P
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S1470 TSU-68 (SU6668) PDGFR selective
SU6668 has greatest potency against PDGFR autophosphorylation
with Ki of 8 nM, but also strongly inhibits Flk-1 and FGFR1
trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck,
Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
S1363 Ki8751 PDGFR selective
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9
nM, >40-fold selective for VEGFR2 than c-Kit, PDGFR and FGFR-2,
little activity to EGFR, HGFR and InsR.
S3012 Pazopanib
Pazopanib is a potent and selective multi-targeted receptor tyrosine
kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-/, and
c-Kit.
Page 18
Page 20
S2231 Telatinib PDGFR selective
Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and
PDGFR with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
Phase 2.
Page 19
S1557 KRN 633
KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of
170 nM/160 nM/125 nM, weakly inhibits PDGFR-/ and c-Kit, does
not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.
Page 20
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly
for class III (FLT3/c-Kit) with IC50 of 1nM/2nM, also potent to class IV
(FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less
potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase
4.
Page 17
Page 19
S1490 Ponatinib (AP24534) PDGFR selective
S1005 Axitinib PDGFR selective
Masitinib is a novel inhibitor for Kit and
PDGFR/ with IC50 of 200 nM and 540
nM/800 nM, weak inhibition to ABL and
c-Fms. Phase 2/3.
S1064 Masitinib (AB1010)
AP24534 is a novel, potent multi-target inhibitor of Abl, PDGFR,
VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2
nM and 5.4 nM, respectively.
Axitinib (AG-013736) is a multi-target inhibitor of VEGFR1, VEGFR2,
VEGFR3, PDGFR and c-Kit with IC50 of 0.1nM, 0.2nM, 0.1-0.3nM,
S1003 Linifanib (ABT-869) PDGFR selective
Linifanib (ABT-869) is a novel, potent ATP-competitive
VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFR with
IC50 of 4nM, 3nM, 3nM/4nM and66nM respectively, mostlyeffective
inmutant kinase-dependent cancer cells(i.e. FLT3). Phase3.
Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR
inhibitor for VEGFR1/2/3 with IC50 of 0.21 nM/0.16 nM/0.24 nM, and
also inhibits PDGFR and c-Kit, low activity observed against FGFR-1,
Flt3, c-Met EGFR and IGF-1R. Phase 3.
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive
inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively;
similar activity against Kit, ~10-fold more selective for VEGFR than
BIBF1120 (Vargatef) is a potent triple angiokinase inhibitor for
VEGFR1/2/3, FGFR1/2/3 and PDGFR/ with IC50 of 34 nM/13 nM
/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM. Phase 3.
Dovitinib Dilactic acid (TKI258 Dilactic acid) is a multitargeted RTK
inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also
potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50
of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1
and HER2. Phase 4.
Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel
multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR,
FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74
nM, 140 nM and 146 nM, respectively.
Licensed by Pfizer
Page 16
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Page 15
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Page 17
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28
Phone:+1-832-582-8158
www.selleckchem.com
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PDGFR / c-Met
Linifanib
BIBF1120
Dovitinib
Sunitinib Malate
Masitinib
Tivozanib
Ki8751
TSU-68
Ponatinib
CP 673451
KRN 633
Telatinib
Imatinib
Crenolanib
MK-2461
Pazopanib
TyrphostinAG 1296
S1003
S1010
S1018
S1042
S1064
S1207
S1363
S1470
S1490
S1536
S1557
S2231
S2475
S2730
S2774
S3012
S8024
+
+
+
+
+++
+
++
+
+++
+
+++
59 nM [IC50]
210 nM [IC50]
0.54 M [IC50]
67 nM [IC50]
1.1 nM [IC50]
0.965 M [IC50]
15 nM [IC50]
100 nM [IC50]
10 nM [IC50]
71 nM [IC50]
1 M [IC50]
+
+
++
+++
+
+++
+++
++++
+
+
++
+
+++
66 nM [IC50]
65 nM [IC50]
27 nM [IC50]
2 nM [IC50]
0.8 M [IC50]
1.72 nM [IC50]
8 nM [Ki]
1 nM [IC50]
9.85 M [IC50]
100 nM [IC50]
22 nM [IC50]
85 nM [IC50]
1 M [IC50]
Cat.No. Inhibitor Name PDGFR- PDGFR- Other
FLT1, FLT3, CSF-1R
FGFR-3, VEGFR3, VEGFR2, VEGFR1, FGFR-2, FGFR-1
FGFR-1, c-Kit, FGFR-3, VEGFR1, VEGFR3, FLT3, VEGFR2
VEGFR2
c-Kit
VEGFR1, c-Kit, VEGFR2, VEGFR3
FGFR-2, VEGFR2, c-Kit
FGFR-1
SRC, Abl, VEGFR2, FGFR-1
VEGFR2, VEGFR3, VEGFR1
VEGFR2, VEGFR3, c-Kit
c-Kit, Bcr-Abl
FGFR-3, FGFR-1, FGFR-2, c-Met
VEGFR2, FGFR-1, VEGFR1, VEGFR3, c-Kit
c-Kit
Tyrphostin AG 1296 (AG 1296) is an inhibitor of PDGFR with IC50 of 0.3-0.5 M, no activity to EGFR.
S8024 Tyrphostin AG 1296
N
N
O
O
Size
c-Met Inhibitors
PF-2341066 (Crizotinib) is a potent inhibitor
of c-Met and ALK with IC50 of 11 nM and 24
nM, respectivley.
S1068 Crizotinib (PF-02341066)
Product Citations:
Nature, 2012, 487(7408): 505-9
Cell, 2012, 151(5): 937-50
Cancer Cell, 2011, 19(5): 679-90
Data from[ [Nat Med, 2011,
17(9): 1116-20 ]
Crizotinib purchased from
Selleck
Licensed by Pfizer
S1111 Foretinib (GSK1363089)
Foretinib (GSK1363089, XL880) is an ATP-competitive inhibitor of
HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and
0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFR/ and Tie-2,
and little activity to FGFR1 and EGFR. Phase 2.
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
Page 17
PHA-665752 is a potent, selective and
ATP-competitive c-Met inhibitor with IC50 of 9
nM, >50-fold selectivity for c-Met than RTKs
or STKs.
S1070 PHA-665752
Product Citations:
Nat Genet, 2012, 44(8): 852-60
Stem Cells, 2012, 30(9): 1819-30
Data from[ Oncogene, 2013,
32(23): 2818-27 ]
PHA-665752 purchased from
Selleck
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
0.0
0.5
1.0
1.5
2.0
2.5
3.0
3.5
F
lu
c
/R
lu
c
ra
tio
(fo
ld
o
f c
o
n
tro
l o
f
e
a
c
h
c
e
ll lin
e
)
control TRAIL Cetuximab Erlotinib MS-275 PI-103 PHA665752
PDGFR selective
MP-470 (Amuvatinib) is a potent and
multi-targeted inhibitor of c-Kit, PDGFR and
Flt3 with IC50 of 10 nM, 40 nM and 81 nM,
respectively. Phase 2.
S1244 Amuvatinib (MP-470)
Product Citations:
Nat Genet, 2012, 44(8): 852-60
44(8): 852-60 ]
Amuvatinib purchased from
Selleck
10 mM/1 mL in DMSO
50 mg 2 mg 10 mg
Size
PDGFR selective
MK-2461 is a potent, multi-targeted inhibitor
for c-Met(WT/mutants) with IC50 of 0.4-2.5
nM, less potent to Ron, Flt1; 8- to 30-fold
greater selectivity of c-Met targets versus
FGFR1, FGFR2, FGFR3, PDGFR, KDR,
Flt3, Flt4, TrkA, andTrkB. Phase 1/2.
S2774 MK-2461
Size
Size
29
c-Met
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J NJ -38877605is anATP-competitive inhibitor
of c-Met with IC50 of 4 nM, 600-fold selective
for c-Met than 200 other tyrosine and
serine-threonine kinases. Phase 1.
S1114 JNJ-38877605
10 mM/1 mL in DMSO
100 mg 2 mg 10 mg
Size
Product Citations:
PLoS Biol, 2011, 9(9): e1001162
Neoplasia, 2011, 13(12): 1132-42
Data from[ PLoS Biol, 2011,
9(9): e1001162 ]
JNJ-38877605 purchased
fromSelleck
BMS-777607 is a Met-related inhibitor for
c-Met, Axl, Ron and Tyro3 with IC50 of 3.9nM,
1.1 nM, 1.8 nM and 4.3 nM, 40-fold more
selective for Met-related targets versus Lck,
VEGFR-2, and TrkA/B, and more than
500-fold greater selectivity versus all other
receptor and non receptor kinases. Phase
1/2.
S1561 BMS 777607
Medical University
BMS 777607 purchased from
Selleck
ARQ-197 is the first non-ATP-competitive
c-Met inhibitor with Ki of 0.355 M, little
activity to Ron, and no inhibition to EGFR,
InsR, PDGFR or FGFR1/4. Phase 3.
S2753 Tivantinib (ARQ 197)
S2201 BMS 794833
BMS794833 is a potent ATP competitive inhibitor of Met/VEGFR2
with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of
<3 nM; a prodrug of BMS-817378. Phase 1.
N
F F
N
N
N
N
N
N
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
Page 20
S2774 MK-2461
MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants)
with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater
selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFR
, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2.
Page 27
S2859 Golvatinib (E7050)
Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of
14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth
(up to 1000 nM). Phase 1/2.
Page 19
SU11274 is a selective Met inhibitor with IC50
of 10 nM, no effects on PGDFR, EGFR or
Tie2.
S1080 SU11274
10 mM/1 mL in DMSO
200 mg 2 mg 25 mg
Size
Product Citations:
Nat Med, 2012, 18(7): 1118-22
Oncogene, 2013, 32(10): 1252-65
Data from[ Oncogene, 2012,
31(25): 3039-50 ]
SU11274 purchased from
Selleck
Gefitinib
SU11274
150 c-Met
-tubulin
pMet Tyr1234/1235 150
50
kDa
TGF-EGFRWT;Ink2/3/;PTENlox
-
-
-
+ +
+
+
+
+ + +
+ -
-
- -
-
-
T4 T5 T6
SGX-523 is a selective Met inhibitor with IC50
of 4nM, no activityto BRAFV599E, c-Raf, Abl
and p38. Phase 1.
S1112 SGX-523
50 mg 5 mg 25 mg
Size
Product Citations:
Clin Cancer Res, 2013, 19(9): 2584-91
Data from[ Neuro Oncol,
2012, 15(2): 161-71 ]
SGX-523 purchased from
Selleck
PF-04217903 is a selective ATP-competitive
c-Met inhibitor with IC50 of 4.8nM, susceptible
to oncogenic mutations (no activity to
Y1230C mutant). Phase 1.
S1094 PF-04217903
10 mM/1 mL in DMSO
100 mg 5 mg 50 mg
Size
Product Citation:
Eur J Cancer, 2011, 47(8): 1231-43
Data from[ Eur J Cancer,
2011, 47(8): 1231-43 ]
Selleck
AMG-208 is a highly selective c-Met inhibitor
with IC50 of 9 nM. Phase 1.
S1316 AMG-208
S1119 XL-184 (Cabozantinib, BMS907351)
XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035
nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50
of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM,
respectively.
S1361 MGCD-265
MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of
c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM,
respectively; also inhibits Ron andTie2. Phase 1/2.
Page 15
Page 18
10 mg 50 mg 200 mg
Size
10 mg 50 mg 200 mg
Size
INCB28060 is a novel, ATP-competitive
inhibitor of c-MET with IC50 of 0.13 nM,
inactive against RON, as well as EGFR and
HER-3. Phase 1.
S2788 INCB28060
O
HN
N
N
N N
N
F
10 mg 50 mg 200 mg
Size
30
Phone:+1-832-582-8158
www.selleckchem.com
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c-Met / HER2
S1011 Afatinib (BIBW2992)
BIBW2992 irreversibly inhibits EGFR/HER2 including EGFR(wt),
EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM,
0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against
Gefitinib-resistant L858R-T790M EGFR mutant. Phase 3.
Page 22
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
Mubritinib (TAK 165) is a potent inhibitor of
HER2/ErbB2 with IC50 of 6 nM; no activity to
EGFR, FGFR, PDGFR, J AK1, Src and Blk.
S2216 Mubritinib (TAK 165)
S1019 Canertinib (CI-1033)
CI-1033 is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5
nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or
CDK1/2/4. Phase 3.
S1194 CUDC-101
CUDC-101 is a potent multi-target inhibitor targeting HDAC, EGFR
and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, inhibits both
class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2
nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1,
does not inhibit Ins-R, IGF-1R, PKC and CDK1/cyclin B. Phase 1/2.
Page 22
Page 23
Page 20
S2111 Lapatinib
Lapatinib, used in the formof Lapatinib Ditosylate, is a potent EGFR
and ErbB2 inhibitor with IC50 of 10.8 nM and 9.2 nM, respectively.
Page 24
S2752 Arry-380
ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM,
equipotent against truncated p95-HER2, 500-fold more selective for
HER2 versus EGFR. Phase 1.
Page 24
S2784 TAK-285
TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of
17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less
potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
Page 24
AMG 458 is a potent c-Met inhibitor with Ki of
1.2 nM, ~350-fold selectivity for c-Met than
VEGFR2 in cells.
S2747 AMG458
NVP-BVU972 is a selective and potent Met
inhibitor with IC50 of 14 nM.
S2761 NVP-BVU972
HER2 Inhibitors
S1028 Lapatinib Ditosylate (GW-572016)
Lapatinib Ditosylate (GW572016, GW2016, Tykerb, Tyverb) is a
potent EGFR and ErbB2 inhibitor with IC50 of 10.8 nM and 9.2 nM,
respectively.
S2150 Neratinib (HKI-272)
Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor
with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no
significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and
c-Met. Phase 3.
S1167 CP-724714
CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of
10 nM, >640-fold selectivity against EGFR, IR, IRG-1R, PDGFR,
VEGFR2, Abl, Src, c-Metetc. Phase2.
S2192 AZD8931
AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2
and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM, more potent than
Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for
the ErbB family than MNK1 and Flt. Phase 1/2.
S1056 AC480 (BMS-599626)
MS-599626 (AC480) is a selective and efficacious inhibitor of HER1
and HER2 with IC50 of 20nM and30nM, ~8-foldless potent to HER4,
>100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.
Page 23
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Size
Size
EMD 1214063is a potent andselective c-Met
inhibitor with IC50 of 3nM, >200-fold selective
for c-Met than IRAK4, TrkA, Axl, IRAK1, and
Mer. Phase 1.
S7067 EMD 1214063
N
N
O
NC
N
N
O
N
5 mg 50 mg
Size
Size
AG879 potently inhibits HER2/ErbB2 with
IC50 of 1 M, 100- and 500-fold higher
selective to ErbB2 than PDGFR and EGFR.
H2N
S
N
OH
Size
31
IGF-1R
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NVP-AEW541 is a potent inhibitor of IGF-1R
with IC50 of 86 nM, 27-fold greater selectivity
for IGF-1R than InsR.
S1034 NVP-AEW541
Product Citations:
J Clin Invest, 2011, 121(11): 4311-21
Cancer Res, 2011, 71(21): 6773-84
2011, 10(4): 697-707 ]
NVP-AEW541 purchased
fromSelleck
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
50 mg 2 mg 10 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
GSK1904529A is a selective inhibitor of
IGF-1R and IR with IC50 of 27 nM and 25 nM,
>100-fold more selective for IGF-1R/InsR
than Akt1/2, Aurora A/B, B-raf, CDK2, EGFR
etc.
S1093 GSK1904529A
Product Citation:
Cell Death Dis, 2012, 3: e336
Data from[ Cell Death Dis,
2012, 3: e336 ]
GSK1904529A purchased
fromSelleck
NVP-ADW742is anIGF-1R inhibitor withIC50
of 0.17 M, >16-fold more potent against
IGF-1R than InsR; little activity to HER2,
PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
S1088 NVP-ADW742
IGF-1R Inhibitors
OSI-906 (Linsitinib) is a selective inhibitor of
IGF-1R withIC50 of 35nM; modestlypotent to
InsR with IC50 of 75 nM, and no activity
towards Abl, ALK, BTK, EGFR, FGFR1/2,
PKA etc. Phase 3.
S1091 Linsitinib (OSI-906)
Product Citations:
Cancer Res, 2013, 73(2): 834-43
Cancer Res, 2011, 71(21): 6773-84
Data from[ Clin Cancer Res,
2013, 19(9): 2584-91 ]
Linsitinib purchased from
Selleck
0
500
1000
IC
50 [n
m
o
l/L
]
IC
50 [n
m
o
l/L
]
0
500
1000
0
500
1000
0
500
1000
0
500
1000
0
500
1000
H1195
(NRASQ61L)
H2347
(NRASQ61R)
SW1271
(NRASQ61R)
H1299
(NRASQ61K)
H2087
(NRASQ61K)
HCC15
(NRASQ61K)
BMS-536924 is an ATP-competitive IGF-1R
inhibitor with IC50 of 100 nM, modest activity
for Mek, Fak, and Lck with very little activity
for Akt1, MAPK1/2.
S1012 BMS-536924
200 mg 5 mg 50 mg
Size
Product Citations:
Clin Cancer Res, 2011, 17(8): 2237-49
Data from[ Breast Cancer
Res, 2011, 13(3): R52 ]
BMS-536924 purchased from
Selleck
PQ401 inhibits autophosphorylation of
IGF-1R domain with IC50 of <1 M.
S8003 PQ 401
GSK1838705A is a potent IGF-1R inhibitor
withIC50 of 2.0nM, modestlypotent to IR and
ALK with IC50 of 1.6 nM and 0.5 nM,
respectively, and little activity to other protein
kinases.
S2703 GSK1838705A
AG-1024 (Tyrphostin) inhibits IGF-1R
autophosphorylation with IC50 of 7 M, is less
potentto IR withIC50 of 57 M and specifically
distinguishes between InsR and IGF-1R (as
compared to other tyrphostins).
S1234 AG-1024
Product Citation:
Mol Endocrinol, 2011, 25(12): 2041-53
Data from[ Mol Endocrinol,
2011, 25(12): 2041-53 ]
AG-1024 purchased from
Selleck
BMS-754807 is a potent and reversible
inhibitor of IGF-1R/InsR with IC50 of 1.8 nM
/1.7 nM, less potent to Met, Aurora A/B,
TrkA/B and Ron, and shows little activity to
Flt3, Lck, MK2, PKA, PKC etc. Phase 1/2.
S1124 BMS-754807
10 mM/1 mL in DMSO
5 mg 10 mg
Size
Size
0
20
40
60
80
100
120
0.005
0.0002
Size
32
Phone:+1-832-582-8158
www.selleckchem.com
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FLT3
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
FLT3 Inhibitors
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
Quizartinib purchased from
Selleck
Quizartinib (AC220) is a second-generation
FLT3inhibitor for Flt3(ITD/WT) withIC50 of 1.1
nM/4.2 nM, 10-fold more selective for Flt3
than KIT, PDGFR, PDGFR, RET, and
CSF-1R. Phase 1/2.
S1526 Quizartinib (AC220)
Medical University
KW 2449 purchased from
Selleck
KW-2449 is a multiple-targeted inhibitor,
mostly for Flt3 with IC50 of 6.6 nM, modestly
potent to Flt3, Bcr-Abl and Aurora A; little
effect on PDGFR, IGF-1R, EGFR. Phase 1.
S2158 KW 2449
Tandutinib (MLN518, CT53518) is a potent
FLT3 antagonist with IC50 of 0.22 M, also
inhibits PDGFR and c-Kit, 15- to 20-fold
higher potency for FLT3 versus CSF-1R and
>100-fold selectivity for the same target
versus FGFR, EGFR and KDR. Phase 1/2.
S1043 Tandutinib (MLN518)
Product Citation:
Br J Cancer, 2012, 107(10): 1702-13
potent to class IV (FGFR1/3) andclass V (VEGFR1-4) RTKs withIC50
and HER2. Phase 4.
S1181 ENMD-2076
ENMD-2076has selective activityagainstAurora AandVEGFR(Flt3)
withIC50 of 14nM and1.86nM, 25-foldselective to Aurora B andless
potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and
PDGFR. Phase 2.
Page 19
Page 19
0.0
20.0
40.0
60.0
80.0
100.0
120.0
0 0.03 0.1 0.3 1 3 10 30
10 mM/1 mL in DMSO
200 mg 2 mg 10 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Product Citation:
Clin Cancer Res, 2013, 19(3): 586-97
2013, 19(3): 586-97 ]
R406 purchased fromSelleck
R406 is a potent Syk inhibitor with IC50 of 41
nM, strongly inhibits Syk but not Lyn, 5-fold
less potent to Flt3. Phase 1.
S2194 R406
by Claude HAAN Universit
du Luxembourg
TG101209 purchased from
Selleck
TG101209 is a selective J AK2 inhibitor with
IC50 of 6 nM, less potent to Flt3 and RET with
IC50 of 25 nM and 17 nM, ~30-fold selective
for J AK2 than J AK3, sensitive to J AK2V617F
and MPLW515L/K mutations.
S2692 TG101209
MP-470 (Amuvatinib) is a potent and multi-targeted inhibitor of c-Kit,
PDGFR and Flt3 with IC50 of 10nM, 40nM and81nM, respectively.
Phase 2.
XL184(Cabozantinib) is a potent VEGFR2inhibitor withIC50 of 0.035
nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, andAXL with IC50
respectively.
Page 15
Page 27
for class III (FLT3/c-Kit) withIC50 of 1nM/2nM, also potent to class IV
4.
Page 17
ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076,
selective activityagainstAurora AandVEGFR(Flt3) withIC50 of 14nM
and 1.86 nM, 25-fold more selective for Aurora A thanAurora B and
less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and
PDGFR. Phase 2.
Page 21
C
I 0.594
C
I 0
.5
6
0 C
I 0.551
C
I 0.586
0
20
40
60
80
100
- 2.5 5 - 2.5 5 - 2.5 5 - 2.5 5
- 5 - 5
Size
TCS 359is a potent FLT3inhibitor withIC50 of
42 nM.
S8023 TCS 359
S
O
NH2
NH
O
O
O
Size
Size
5 mg 50 mg 200 mg
Size
33
FLT3 / FGFR
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FGFR Inhibitors
S1264 PD173074 FGFR1selective
BGJ 398 (NVP-BGJ 398) is a potent and
selective FGFR inhibitor for FGFR1/2/3 with
IC50 of 0.9nM/1.4nM/1nM, >40-foldselective
for FGFR versus FGFR4 and VEGFR2, and
little activityto Abl, Fyn, Kit, Lck, LynandYes.
Phase 2.
S2183 BGJ398 (NVP-BGJ398)
AZD4547 is a novel selective FGFR inhibitor
targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5
nM/1.8 nM, weaker activity against FGFR4,
VEGFR2(KDR), and little activity observed
against IGFR, CDK2, and p38. Phase 1/2.
S2801 AZD4547
PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also
inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selectivity over
PDGFR and c-Src.
Dovitinib
Tandutinib
XL-184
ENMD-2076
Amuvatinib
Quizartinib
KW 2449
TG101209
Dovitinib Dilactic acid
TCS 359
S1018
S1043
S1119
S1181
S1244
S1526
S2158
S2692
S2769
S8023
++12 nM [IC50]
++++
+++
++
+++
+
+++
+++
++
++++
++
1 nM [IC50]
0.22 M [IC50]
11.3 nM [IC50]
1.86 nM [IC50]
81 nM [IC50]
1.1 nM [IC50]
6.6 nM [IC50]
25 nM [IC50]
1 nM [IC50]
42 nM [IC50]
+++
++
6 nM [IC50]
15.9 nM [IC50]
Cat.No. Inhibitor Name FLT1 FLT3 FLT4 Other
VEGFR2, FGFR-1, c-Kit, PDGFR-,
VEGFR3, FGFR-3, VEGFR1, PDGFR-
c-Kit, PDGFR-
Axl, c-Met, Tie-2, c-RET, c-Kit, VEGFR2
Aurora B, VEGFR2, Aurora A
Aurora A, c-Kit, J AK2, FGFR-1, Abl
J AK3, c-RET, J AK2
c-Kit
O
O
N HN
NH
O
N NH
Page 17
S1490 Ponatinib (AP24534) FGFR1selective
BIBF1120 (Vargatef) is a potent triple angiokinase inhibitor for
VEGFR1/2/3, FGFR1/2/3 and PDGFR/ with IC50 of 34 nM/13 nM
/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM. Phase 3.
Page 16
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34
Phone:+1-832-582-8158
www.selleckchem.com
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FGFR / c-Kit
BIBF1120
Dovitinib
Brivanib alaninate
PD173074
TSU-68
Ponatinib
BGJ 398
MK-2461
AZD4547
S1010
S1018
S1138
S1264
S1470
S1490
S2183
S2774
S2801
+
+++
+
++
++
+++
++++
+
++++
69 nM [IC50]
8 nM [IC50]
148 nM [IC50]
~25 nM [IC50]
1.2 M [Ki]
2.2 nM [IC50]
0.9 nM [IC50]
65 nM [IC50]
0.2 nM [IC50]
++
+++
++
+++
37 nM [IC50]
1.4 nM [IC50]
39 nM [IC50]
2.5 nM [IC50]
+
+++
++++
++
+++
108 nM [IC50]
9 nM [IC50]
1 nM [IC50]
50 nM [IC50]
1.8 nM [IC50]
Cat.No. Inhibitor Name FGFR-1 FGFR-2 FGFR-3 FGFR-4 Other
PDGFR-, VEGFR2,
VEGFR1, PDGFR-,
VEGFR3
PDGFR-, VEGFR3,
c-Kit, FLT3, PDGFR-,
VEGFR2, VEGFR1
VEGFR1,VEGFR2
VEGFR2
PDGFR-
PDGFR-, Abl,
SRC, VEGFR2
c-Met, PDGFR-
+ 60 nM [IC50]
FGFR1selective S1138 Brivanib alaninate (BMS-582664)
Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an
ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.
S2774 MK-2461
MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants)
with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater
selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFR
, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2.
TyrphostinAG 1296 (AG 1296) is an inhibitor of PDGFR with IC50 of
0.3-0.5 M, no activity to EGFR.
Page 20
Page 27
Page 28
c-Kit Inhibitors
S1220 OSI-930
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80
nM, 9nM and15nM, respectively; modest activityto Flt-1, c-Raf and
Lck, and low activity against PDGFR/, Flt-3 and Abl. Phase 1.
S1064 Masitinib (AB1010)
Masitinib is a novel inhibitor for Kit and PDGFR/ with IC50 of 200nM
and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 2/3.
Phase 2.
Page 27
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Page 20
S1084 Brivanib (BMS-540215)
Brivanib is anATP-competitive inhibitor against VEGFR2 with IC50 of
25 nM, moderate potency against VEGFR-1 and FGFR-1, but
>240-fold against PDGFR-. Phase 3.
4.
Page 18
Page 17
Dasatinib (BMS-354825, Sprycel) is a novel,
potent andmulti-targetedinhibitor that targets
Abl, Src and c-Kit, with IC50 of <1 nM, 0.5 nM
S1021 Dasatinib
Product Citations:
Cell Stem Cell, 2012, 10(2): 210-7
Blood, 2012, 119(21): 4981-91
Cell Res, 2011, 21(7): 1080-87
2012, 18(1): 127-39 ]
Dasatinib purchased from
Selleck
10 mM/1 mL in DMSO
100 mg 25 mg
Size
pSFK (Y416) lighter
C
om
bination (3)
C
om
bination (2)
C
om
bination (1)
IN
C
B
16562 (2)
IN
C
B
16562 (1)
D
asatinib (2)
D
asatinib (1)
C
ontrol (2)
C
ontrol (1)
pSFK (Y416) darker
pFAK (Y861)
pJ ak2 (Y221)
pJ ak2 (1007/1008)
pSTAT3 (Y705)
SOCS2
-Actin
pSFK/-Actin
pFAK/-Actin
1.0 1.0 0.3 0.3 0.6 1.0 0.5 0.1 0.5
1.3 0.7 0.1 0.6 0.5 2.0 1.7 0.9 0.4
Size
SSR128129E (SSR) is an allosteric inhibitor
of FGF/FGFR signaling, acting via binding to
the extracellular part of the FGFR.
S7167 SSR128129E (SSR)
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
Danusertib (PHA-739358) is an Aurora
kinase inhibitor for Aurora A/B/C with IC50 of
13 nM/79 nM/61 nM, modest potent to Abl,
TrkA, c-RET and FGFR1, less potent to Lck,
VEGFR2/3, c-Kit, CDK2 etc. Phase 2.
S1107 Danusertib (PHA-739358)
Product Citation:
Am J Transl Res, 2013, 5(3): 359-67
Data from[ Biochem
Pharmacol, 2012, 83(4):
452-61 ]
Danusertib purchased from
Selleck
new
N
O
O
ONa
O
NH2
and HER2. Phase 4.
Page 19
S1470 TSU-68 (SU6668) FGFR1selective
SU6668 has greatest potency against PDGFR autophosphorylation
with Ki of 8 nM, but also strongly inhibits Flk-1 and FGFR1
trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck,
Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
Page 18
10 mg 50 mg
Size
Size
35
c-Kit / ALK
P
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K
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10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
ALK Inhibitors
TAE684 is a potent and selective ALK
inhibitor with IC50 of 3 nM, 100-fold more
sensitive for ALK than InsR.
S1108 TAE684
Product Citations:
Nature, 2012, 487(7408): 505-9
Cell, 2012, 151(5): 937-50
2012, 18(17): 4570-9 ]
TAE684 purchased from
Selleck
S2703 GSK1838705A
GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM,
modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM,
respectively, and little activity to other protein kinases.
S1363 Ki8751
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9
nM, >40-fold selective for VEGFR2 than c-Kit, PDGFR and FGFR-2,
little activity to EGFR, HGFR and InsR.
S2231 Telatinib
Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and
PDGFR with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
Phase 2.
4.
S3012 Pazopanib
Pazopanib is a potent and selective multi-targeted receptor tyrosine
kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-/, and
c-Kit.
TyrphostinAG 1296 (AG 1296) is an inhibitor of PDGFR with IC50 of
0.3-0.5 M, no activity to EGFR.
Page 20
Page 19
Page 17
Page 19
Page 28
Page 31
Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib,
which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR withIC50 of
0.6 M, 0.1 M and 0.1 M, respectively.
S1042 Sunitinib Malate
Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor
targeting VEGFR2 (Flk-1) and PDGFR with IC50 of 80nM and2nM,
and also inhibits c-Kit.
Licensed by Pfizer
Licensed by Pfizer
respectively.
S1005 Axitinib
Axitinib (AG-013736) is a multi-target inhibitor of VEGFR1, VEGFR2,
VEGFR3, PDGFR and c-Kit with IC50 of 0.1nM, 0.2nM, 0.1-0.3nM,
Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel
multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR,
FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74
nM, 140 nM and 146 nM, respectively.
S1178 Regorafenib (BAY 73-4506)
Regorafenib(BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor
for VEGFR1, VEGFR2, VEGFR3, PDGFR, Kit, RET and Raf-1 with
IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM,
respectively.
S1101 Vatalanib (PTK787) 2HCl
Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37
nM, less potent against VEGFR1/Flt-1, 18-fold against
VEGFR3/Flt-4. Phase 1/2.
and HER2. Phase 4.
Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR
inhibitor for VEGFR1/2/3 with IC50 of 0.21 nM/0.16 nM/0.24 nM, and
also inhibits PDGFR andc-Kit, lowactivityobservedagainst FGFR-1,
Flt3, c-Met EGFR and IGF-1R. Phase 3.
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive
inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively;
similar activity against Kit, ~10-fold more selective for VEGFR than
Page 26
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36
Phone:+1-832-582-8158
www.selleckchem.com
P
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ALK / Tie-2 / c-RET / Trk Receptor / Ephrin Receptor
Trk Receptor Inhibitors
Ephrin Receptor Inhibitor
TrkAselective
GW 441756 is a potent, selective inhibitor of
TrkA with IC50 of 2 nM, with very little activity
to c-Raf1 and CDK2.
S2891 GW441756
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora
A/B/C with IC50 of 13 nM/79 nM/61 nM, modest potent to Abl, TrkA,
c-RET and FGFR1, less potent to Lck, VEGFR2/3, c-Kit, CDK2 etc.
Phase 2.
Phase 2.
TG101209 is a selective J AK2 inhibitor with IC50 of 6 nM, less potent
to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for
J AK2 than J AK3, sensitive to J AK2V617F and MPLW515L/K
mutations.
S2692 TG101209
BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with
IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and
Ron, andshows little activityto Flt3, Lck, MK2, PKA, PKC etc. Phase
1/2.
S1124 BMS-754807
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that
discriminates between VEGFR and EphB4 inhibition; also shows
activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 M, 1.266
M and 1.667 M, respectively.
S2202 NVP-BHG712
c-RET Inhibitors
S1361 MGCD-265
MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of
c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM,
respectively; also inhibits Ron andTie2. Phase 1/2.
N
N
H
N
O
Page 18
Page 33
Page 27
Page 32
Page 31
Page 19
CH5424802is a potentALK inhibitor withIC50
of 1.9 nM, sensitive to L1196M mutation and
higher selectivity for ALK than PF-02341066,
NVP-TAE684 and PHA-E429. Phase 1/2.
S2762 CH5424802
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
AP26113 is a potentALK inhibitor with IC50 of
0.62 nM, demonstrated ability overcome
Crizotinib resistance mediated by a L1196M
mutation. Phase 1/2.
S7000 AP26113
LDK378is potent againstALK with IC50 of 0.2
nM, selectivityagainstIGF-1R andInsR is 40-
and 35-fold, respectively. Phase 2.
S7083 LDK378
Tie-2 Inhibitors
Tie2 kinase inhibitor is an optimized
compound of SB-203580, selective to Tie2
with IC50 of 0.25 M, 200-fold more potent
than p38.
S1577 Tie2 kinase inhibitor
Product Citation:
Neoplasia, 2012, 14(2): 131-40
Data from[ Neoplasia, 2012,
14(2): 131-40 ]
Tie2 kinase inhibitor
S1068 Crizotinib (PF-02341066)
PF-2341066 (Crizotinib) is a potent inhibitor of c-Met and ALK with
IC50 of 11 nM and 24 nM, respectivley.
Licensed by Pfizer
new
respectively.
N
H
Cl
N
N
S O
O
N
H
O
NH
N
N
N
H
NH
P
O
O
N
N
Cl
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
Size
Size
Page 28
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Size
5 mg 50 mg
Size
37
Axl / CSF-1R
P
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38
Phone:+1-832-582-8158
www.selleckchem.com
A
n
g
i
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s
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s
VEGFR / J AK / EGFR / PDGFR / HER2 / FLT3 / FGFR / ALK
Angiogenesis
TGF
Pathway
MAPK
Pathway
PI3K/Akt
Pathway
Angiogenesis
G-protein
eNOS
NO
CAS
ALK
S1P
Ras
PI3K
S1P
TGF-
c-Src
Raf
HIF protein
S1PR
VEGFR TGF-R
Flt/KDR
Pan-VEGFR inhibitors
Pan-VEGFR inhibitors
BIBF1120
Pazopani b
Axi ti ni b
ZM 306416(VEGFR1)
XL-184(VEGFR2)
Vandetani b(VEGFR2)
SAR131675(VEGFR3)
ALK inhibitors
TAE684
CH5424802
GSK1838705A
Cri zoti ni b
Src inhibitors
Dasati ni b
Saracati ni b
Bosuti ni b
KX2-391
NVP-BHG712
Pan-Raf inhibitors
Vemurafeni b
Sorafeni b
HIF inhibitors
FG-4592
IOX2
2-Methoxyestradi ol
PLX-4720
Selective Raf inhibitors
GDC-0879(B-Raf)
GW5074(C-Raf)
Pan-PI3K inhibitors
BEZ235
LY294002
GDC-0941
BYL719(p110)
GSK2636771(p110)
TGX-221(p110)
AS-252424(p110)
CAL-101(p110)
IPI-145(p110)
VEGFR Inhibitors
Detailed product information is on page 15-21
EGFR Inhibitors
PDGFR Inhibitors
HER2 Inhibitors
Detailed product information is on page 30
FLT3 Inhibitors
FGFR Inhibitors
ALK Inhibitors
JAK Inhibitors
CEP-32496 is a highly potent inhibitor of
BRAF(V600E/WT) and c-Raf with Kd of 14
nM/36 nM and 39 nM, modest potent to
Abl-1, c-Kit, Ret, PDGFR and VEGFR2,
respectively; insignificantaffinityfor MEK-1,
MEK-2, ERK-1 and ERK-2. Phase 1/2.
S8015 CEP-32496
NH
O
NH
O N
F
F
F
O
N
N
O
O
Axl Inhibitors
CSF-1R Inhibitors
GW2580 is a selective CSF-1R inhibitor for
c-FMS with IC50 of 30 nM, 150- to 500-fold
selective compared to b-Raf, CDK4, c-KIT,
c-SRC, EGFR, ERBB2/4, ERK2, FLT-3,
GSK3, ITK, J AK2 etc.
S8042 GW2580
R428 is an inhibitor of Axl with IC50 of 14 nM,
>100-foldselective forAxl versus Abl, 50- and
>100-foldover Mer andTyro3, >100-foldover
InsR, EGFR, HER2, and PDGFR.
S2841 R428 (BGB324)
respectively.
S1561 BMS 777607
BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3
withIC50 of 3.9nM, 1.1nM, 1.8nM and4.3nM, 40-foldmore selective
for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more
than 500-fold greater selectivity versus all other receptor and non
receptor kinases. Phase 1/2.
S4001 Cabozantinib malate (XL184)
Cabozantinibmalate is the malate of Cabozantinib, a potent VEGFR2
inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit,
Flt-1/3/4, Tie2, andAXL withIC50 of 1.3nM, 4nM, 4.6nM, 12nM/11.3
nM/6 nM, 14.3 nM and 7 nM, respectively.
S1003 Linifanib (ABT-869)
Linifanib (ABT-869) is a novel, potent ATP-competitive
VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFR with
IC50 of 4nM, 3nM, 3nM/4nM and66nM respectively, mostlyeffective
inmutant kinase-dependent cancer cells(i.e. FLT3). Phase3.
S1220 OSI-930
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80
nM, 9nM and 15nM, respectively; modest activityto Flt-1, c-Raf and
Lck, and low activity against PDGFR/, Flt-3 and Abl. Phase 1.
N
N N
NH2 N
H
N
N
N
N
N
NH2
H2N
O
O
O
10 mM/1 mL in DMSO
Size
1 mg 50 mg 100 mg 5 mg
10 mM/1 mL in DMSO
Size
25 mg
Page 15
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Page 21
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39
HIF / VDA / Bcr-Abl
A
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s
i
s
HIF Inhibitors
2-Methoxyestradiol depolymerizes
microtubules and blocks HIF-1 nuclear
accumulation and HIF-transcriptional activity.
Phase 2.
S1233 2-Methoxyestradiol (2-MeOE2)
FG-4592 is an HIF prolyl hydroxylase
inhibitor, stabilizes HIF-2 and induces EPO
production. Phase 2/3.
S1007 FG-4592
IOX2 is a potent inhibitor of HIF-1 prolyl
hydroxylase-2 (PHD2) with IC50 of 21 nM
>100-fold selectivity over J MJ D2A, J MJ D2C,
J MJ D2E, J MJ D3, or the 2OG oxygenase FIH.
S2919 IOX2
VDA
DMXAA (ASA404) is a VDA and competitive
inhibitor of DT-diaphorase with Ki of 20 M
and IC50 of 62.5 M, respectively. Phase 3.
S1537 DMXAA (Vadimezan)
NPI-2358 is a VDA against tubulin-
depolymerizing with IC50 of 9.8~18 nM in
tumor cells. Phase 2.
S1176 Plinabulin (NPI-2358)
Bcr-Abl Inhibitors
Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib,
which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR withIC50 of
S1490 Ponatinib (AP24534)
N
H
O
OH
O
N O
OH
Page 26
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Size
Size
Size
Size
S1021 Dasatinib
Dasatinib (BMS-354825, Sprycel) is a novel, potent and
multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1
nM, 0.5 nM and 79 nM, respectively.
Nilotinib (AMN-107, Tasigna) is a Bcr-Abl
inhibitor with IC50 less than 30 nM.
S1033 Nilotinib (AMN-107)
Product Citations:
Leuk Res, 2013, 37(2): 183-9
Leuk Res, 2012, 36(10): 1311-4
Data from[ Leuk Res, 2013,
37(2): 183-9 ]
Nilotinib purchased from
Selleck
Bafetinib (INNO-406) is a potent and
selective dual Bcr-Abl/Lyn inhibitor with IC50
of 5.8 nM/19 nM, does not inhibit the
phosphorylation of the T315I mutant and is
less potent to PDGFR and c-Kit. Phase 2.
S1369 Bafetinib (INNO-406)
S2243 WP1130
GZD824is a novel orallybioavailable Bcr-Abl
inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I)
with IC50 of 0.34 nM and 0.68 nM,
respectively.
S7194 GZD824
WP1130 (Degrasyn) is a selective
deubiquitinase (DUB: USP5, UCH-L1,
USP9x, USP14, and UCH37) inhibitor and
also supresses Bcr/Abl, also a J AK2
transducer (without affecting 20S
proteasome) and activator of transcription
(STAT).
Product Citations:
Neoplasia, 2012, 14(10): 893-904
J Biol Chem, 2012, 288(4): 2721-33
Data from[ J Biol Chem,
2012, 288(4): 2721-33 ]
WP1130 purchased from
Selleck
new
HN
O CF3
N
N
N
N
HN
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
300 mg 25 mg 100 mg
Size
Page 34
100 102 104 100 102 104 100 102 104
Size
5 mg 50 mg 200 mg
Size
5 mg 25 mg 200 mg
Size
40
Phone:+1-832-582-8158
www.selleckchem.com
A
n
g
i
o
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e
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e
s
i
s
Bcr-Abl
Saracatinib
Imatinib Mesylate
Nilotinib
Danusertib
S1006
S1026
S1033
S1107
++
++
<30 nM [IC50]
25 nM [IC50]
++
+
30 nM [IC50]
0.6 M [IC50]
Cat.No. Inhibitor Name Bcr-Abl Abl Other
SRC
c-Kit
Aurora A, Aurora B, c-RET, Aurora C
AT9283
Bafetinib
Ponatinib
KW 2449
WP1130
GNF-2
S1134
S1369
S1490
S2158
S2243
S2899
+++
+
+
5.8 nM [IC50]
1.8 M [IC50]
138 nM [IC50]
+++
++++
+++
4 nM [IC50]
0.37 nM [IC50]
14 nM [IC50]
Aurora B, J AK2,Aurora A, J AK3
SRC, VEGFR2, FGFR-1, PDGFR-
Aurora A, J AK2, FGFR-1, FLT3, c-Kit
AT9283 is a potent J AK2/3 inhibitor with IC50
of 1.2 nM/1.1 nM; also potent to Aurora A/B,
Abl(T315I). Phase 1/2.
S1134 AT9283
10 mM/1 mL in DMSO
2 mg 100 mg 10 mg
Size
Product Citations:
Cell Stem Cell, 2012, 11(2): 179-94
J Cell Mol Med, 2013, 17(2): 265-76
by Dr. Claude Haan and
Catherine Rolvering of
Universite du Luxembourg
Selleck
S2158 KW 2449
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of
6.6 nM, modestly potent to Flt3, Bcr-Abl andAurora A; little effect on
PDGFR, IGF-1R, EGFR. Phase 1.
GNF-2 is a highly selective non-ATP
competitive inhibitor of Bcr-Abl, shows no
activity to Flt3-ITD, Tel-PDGFR, TPR-MET
andTel-J AK1 transformed tumor cells.
S2899 GNF-2
O
H2N
N
N
HN O
F
F
F
DCC-2036is a conformational control Bcr-Abl
inhibitor for Abl1(WT) and Abl1(T315I) with
IC50 of 0.8 nM and 4 nM, also inhibits SRC,
LYN, FGR, HCK, KDR, FLT3, and Tie-2, and
lowactivity to seen towards c-Kit. Phase 1/2.
S2634 DCC-2036 (Rebastinib)
Page 32
S2202 NVP-BHG712
Page 19
FTY720 (Fingolimod, Gilenya) is a S1P
antagonist with IC50 of 0.033 nM.
S5002 Fingolimod (FTY720, fingolimod hydrochloride)
Product Citations:
Blood, 2012, 119(9): 2176-7
PLoS One, 2012, 7(2): e32211
Data from[ PLoS One,
2012, 7(5): e36429 ]
Fingolimod purchased from
Selleck
Saracatinib (AZD0530) is a potent Src
inhibitor with IC50 of 2.7 nM, and potent to
c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active
forAbl andEGFR (L858R andL861Q). Phase
1/2.
S1006 Saracatinib (AZD0530)
Product Citations:
Cancer Res, 2011, 71(24): 7547-57
Int J Cancer, 2013, 132(1): 224-35
Data from[ Mol Endocrinol,
2010, 24(6): 1151-64 ]
Saracatinib purchased from
Selleck
10 mM/1 mL in DMSO
200 mg 10 mg 25 mg
Size
10 mM/1 mL in DMSO
100 mg 200 mg
Size
Phase 2.
Page 33
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Size
41
Src / Syk
A
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s
i
s
Src Inhibitors
KX2-391 (KX01), the first clinical Src inhibitor
(peptidomimetic class) that targets the
peptide substrate site of Src, withGI50 of 9-60
nM in cancer cell lines. Phase 1/2.
S2700 KX2-391
S2202 NVP-BHG712
S1021 Dasatinib
Dasatinib (BMS-354825, Sprycel) is a novel, potent and
multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1
nM, 0.5 nM and 79 nM, respectively.
S1006 Saracatinib (AZD0530)
Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM,
andpotentto c-Yes, Fyn, Lyn, Blk, Fgr andLck; less active forAbl and
EGFR (L858R and L861Q). Phase 1/2.
Bosutinib (SKI-606) is a novel, dual Src/Abl
inhibitor with IC50 of 1.2 nM and 1 nM,
respectively.
S1014 Bosutinib (SKI-606)
Product Citations:
Blood, 2011, 118(7): 1885-98
Cancer Res, 2010, 70(19): 7489-99
Data from[ Blood, 2011,
118(7): 1885-98 ]
Bosutinib purchased from
Selleck
Licensed by Pfizer
PP1 is a potent and selective Src inhibitor for
Lck/Fyn with IC50 of 5 nM/6 nM.
S7060 PP1 new
PP2 is an Src family kinase inhibitor, potently
inhibits Lck/Fyn with IC50 of 4 nM/5 nM,
~100-fold less potent to EGFR, inactive for
ZAP-70, J AK2 and PKA.
S7008 PP2 new
N
N N
N
NH2
N
N N
N
NH2
Cl
10 mM/1 mL in DMSO
10 mg 50 mg
Size
Page 34
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Page 19
R788 (Fostamatinib) disodium, a prodrug of
the active metabolite R406, is a Syk inhibitor
with IC50 of 41 nM, strongly inhibits Syk but
not Lyn, 5-fold less potent to Flt3. Phase 2.
S2206 R788 (Fostamatinib) disodium
Syk Inhibitors
S2194 R406
R406is a potent Syk inhibitor withIC50 of 41nM, stronglyinhibits Syk
but not Lyn, 5-fold less potent to Flt3. Phase 1.
R788 (Fostamatinib), a prodrug of the active
metabolite R406, is a Sykinhibitor withIC50 of
41 nM, strongly inhibits Syk but not Lyn,
5-fold less potent to Flt3. Phase 2.
S2625 Fostamatinib (R788)
Piceatannol, a natural stilbene, is a selective
Syk inhibitor and ~10-fold selectivity versus
Lyn.
S3026 Piceatannol
R406(free base) is a potent Sykinhibitor with
IC50 of 41 nM, strongly inhibits Syk but not
Lyn, 5-fold less potent to Flt3. Phase 2.
S1533 R406 (free base)
Product Citation:
Clin Cancer Res, 2013, 19(3): 586-97
Data from[ Clin Cancer
Res, 2013, 19(3): 586-97 ]
R406 (free base)
10 mg 50 mg 200 mg
Size
PRT062607(P505-15) HCl is a novel, highly
selective Syk inhibitor with IC50 of 1 nM,
>80-fold selective for Syk than Fgr, Lyn, FAK,
Pyk2 and Zap70.
S8032 PRT062607 (P505-15, PRT2607, BIIB057) HCl new
OH
OH
HO
HO
O
O
O
H
N
N
N
F
H
N N
O
N
O
P
O
HO OH
O
N
N
NH2
O
NH NH
N
N N
NH2
HCl
Page 32
C
I 0.594
C
I 0
.5
6
0 C
I 0.551
C
I 0.586
0
20
40
60
80
100
- 2.5 5 - 2.5 5 - 2.5 5 - 2.5 5
- 5 - 5
Size
Size
Size
Size
Size
10 mg 25 mg
Size
5 mg 50 mg 200 mg
Size
42
Phone:+1-832-582-8158
www.selleckchem.com
A
n
g
i
o
g
e
n
e
s
i
s
FAK / BTK
FAK Inhibitors
PF-00562271 is the benzenesulfonate salt of
PF-562271, which is a potent, ATP-
competitive, reversible inhibitor of FAK with
IC50 of 1.5 nM, ~10-fold less potent for Pyk2
than FAK and >100-fold selectivity against
other proteinkinases, except for some CDKs.
Phase 1.
S2676 PF-00562271
Product Citation:
Mol Ther, 2012, 20(5): 972-83
Data from[ Mol Ther, 2012,
20(5): 972-83 ]
PF-00562271 purchased
fromSelleck
5 mg 50 mg 200 mg
Size
PF-562271 is a potent, ATP-competitive,
reversible inhibitor of FAK withIC50 of 1.5nM,
~10-fold less potent for Pyk2 than FAK and
>100-fold selectivity against other protein
kinases, except for some CDKs.
S2890 PF-562271
NVP-TAE226 is a potent FAK inhibitor with
IC50 of 5.5 nM and modestly potent to Pyk2,
~10- to 100-fold less potent against InsR,
IGF-1R, ALK, and c-Met.
S2820 NVP-TAE226 (TAE226)
PF 573228 is anATP-competitive inhibitor of
FAK with IC50 of 4 nM, ~50- to 250-fold
selective for FAK than Pyk2, CDK1/7 and
GSK-3.
S2013 PF 573228
PF-03814735 is a novel, potent and
reversible inhibitor of Aurora A/B with IC50 of
0.8 nM/5 nM, less potent to Flt3, FAK, TrkA,
little active to Met and FGFR1. Phase 1.
S2725 PF-03814735
S2680
BTK Inhibitors
PCI-32765 (Ibrutinib) is a potent and highly
selective Btk inhibitor with IC50 of 0.5 nM,
modestly potent to Bmx, CSK, FGR, BRK,
HCK, less potent to EGFR, Yes, ErbB2,
J AK3, etc. Phase 3.
PCI-32765 (Ibrutinib)
Product Citations:
Cancer Cell, 2012, 22(5): 656-67
Blood, 2012, 120(19): 3978-85
Data from[ Cell Signal,
2013, 25(1): 106-12 ]
PCI-32765 purchased from
Selleck
GDC-0834 is a novel potent and selective
BTK inhibitor with IC50 of 5.9 nM.
S7022 GDC-0834
AVL-292 is a covalent inhibitor of Bruton's
tyrosine kinase (Btk) with IC50 of <0.5 nM.
S7173 AVL-292 new
CGI1746 is a potent and selective Bruton's
tyrosine kinase (Btk) inhibitor with IC50 of 1.9
nM.
S7051 CGI1746 new
N
N
S
O
O
H
N
N
N
F
F
F
H
N
N
H
O
O
N
H
N
N
Cl
N
H
N
H
O
N
O
NH
O
HN
N
N
F
F
F
HN
S
O
O
S
O
HN
N
N
O
NH
N N
O
N
N
F
HN
N
H
N
H
O
O
O
O
N
H
N
N
O
H
N
O
N
O
10 mM/1 mL in DMSO
5 mg 200 mg
Size
R
e
la
tiv
e
lig
h
t u
n
its
( )
1
0
3
0
20
50
75
100
125
No inhibitor
FAK inhibitor
Mn++
+ -
Size
Size
Size
5 mg 10 mg 50 mg
Size
5 mg 50 mg 200 mg
Size
10 mg 50 mg
Size
10 mg 50 mg
Size
43
c-RET / Bcl-2
Caspase activators
PAC-1
Survivin inhibitor
YM155
Caspase activators
PAC-1
Caspase inhibitor
Z-VAD-FMK
Apoptosi s Acti vator 2
Bi ri napant
TNF-alpha inhibitors
Lenal i domi de
Pomal i domi de
Necrostati n-1
Apoptosi s Acti vator 2
IAP inhibitors
AT-406
YM155
Mdm2 inhibitors
Nutl i n-3
NSC-207895
p53 activators
JNJ 26854165
p53 inhibitor
Pifithrin-
RITA
Tenovi n-1
Bi ri napant
Caspase inhibitor
Z-VAD-FMK
TNF- Cytokine
Caspase-8
Caspase-9
Caspase-3
Caspase-3
NIK
IKK
NF-B
cIAP
MDM2
p53
ATM
Survivin
Caspase-9 Apaf1
J AK STAT PKC
Ras
Raf
J NK
c-J un
ERK1/2
PI3K
Src
Bcl-xL
Bcl-2
CytC
Bad
p70S6K
mTOR
Akt
GSK-3
Bcl-xL
Bcl-2
Akt
GSK-3
DNA-PK
Apoptosis
DNA Damage
Bcl-2 inhibitors
TW-37
AT101
ABT-263
ABT-737
Obatocl ax
Apoptosis
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL,
Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3
nM and 197.8 nM, respectively; no inhibition
observedagainst Mcl-1, Bcl-B or Bfl-1. Phase
2.
S1002 ABT-737
Product Citations:
Nat Biotechnol, 2011, 29(6): 542-6
J Clin Invest, 2011, 121(3): 1053-63
Mol Cell, 2012, 46(5): 573-83
117(26): 7145-54 ]
ABT-737 purchased from
Selleck
Bcl-2 Inhibitors
ABT-263 (Navitoclax) is a potent inhibitor of
Bcl-xL, Bcl-2 and Bcl-wwith Ki of 0.5 nM,
1 nM and 1 nM, but binds more weakly to
Mcl-1 andA1. Phase 1/2.
S1001 ABT-263 (Navitoclax)
Product Citations:
Blood, 2011, 117(26): 7145-54
Blood, 2013, 121(10): 1850-7
Data from[ Cancer Res,
2012, 72(12): 2949-56 ]
ABT-263 purchased from
Selleck
A
p
o
p
t
o
s
i
s
c-RET Inhibitors
10 mM/1 mL in DMSO
5 mg 25 mg
Size
10 mM/1 mL in DMSO
5 mg 50 mg
Size
44
Phone:+1-832-582-8158
www.selleckchem.com
A
p
o
p
t
o
s
i
s
Bcl-2
ABT-263
ABT-737
Obatoclax mesylate
HA14-1
TW-37
ABT-199
S1001
S1002
S1057
S1071
S1121
S8048
++++
++++
+++
++
+++
++++
1 nM [Ki]
30.3 nM [EC50]
0.22 M [Ki]
~9 M [IC50]
0.29 M [Ki]
<0.01 nM [Ki]
++++
++++
++
0.5 nM [Ki]
78.7 nM [EC50]
1.11 M [Ki]
++++
+++
1 nM [Ki]
197.8 nM [EC50]
Cat.No. Inhibitor Name Bcl-2 Bcl-xL Bcl-w
new
Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor,
including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with
IC50 of 0.31 M, 0.32 M, 0.20 M and 0.62
M, respectively.
S8061 Sabutoclax
new
Apogossypolone (ApoG2) is a pan Bcl-2
inhibitor for Bcl-2, Bcl-XL and Mcl-1 with IC50
of 35 nM, 660 nM and 25 nM, respectively.
S7200 Apogossypolone (ApoG2)
5 mg 25 mg
Size
new
BAM7 is a direct and selective activator of
proapoptotic Bax with EC50 of 3.3 M.
S7105 BAM7
HO
HO
O
O
O
O
OH
OH
HO
HO
HN O
OH
OH
OH
OH
O
H
N
O
N
H
N
N
N
O
S
N
Size
new
ABT-199 is a Bcl-2-selective inhibitor with Ki
of <0.01 nM, >4800-fold more selective
versus Bcl-xL and Bcl-w, and no activity to
Mcl-1. Phase 2.
S8048 ABT-199 (GDC-0199)
AT-101, the R-(-) enantiomer of Gossypol
acetic acid, binds withBcl-2, Bcl-xL andMcl-1
with Ki of 0.32 M, 0.48 M and 0.18 M;
does not inhibit BIR3domainandBID. Phase
1/2.
S2812 AT101
BM-1074 is a potent and efficacious
Bcl-2/Bcl-xL inhibitor withKi of <1nM, inactive
to Mcl-1.
S7034 BM-1074
10 mg 50 mg
Size
O
O OH
HO
OH
HO
O
HO
OH
HO
N N
N
H
O
S
O
O
Cl
N
H
N S O O
NO2
NH
S
N
Cl
N
N
O NH
O
N N
H
S
O
O
NO2 H
N
O
Size
new
Obatoclax (GX15-070) is an antagonist of
Bcl-2 with Ki of 0.22 M, can assist in
overcoming MCL-1 mediated resistance to
apoptosis. Phase 1/2.
S1057 Obatoclax mesylate (GX15-070)
Product Citations:
Cancer Res, 2011, 71(13): 4494-505
Cancer Res, 2012, 72(11): 2814-21
2012, 3: e351 ]
Obatoclax mesylate
HA14-1 is a non-peptidic ligand of a Bcl-2
surface pocket with IC50 of ~9 M.
S1071 HA14-1
TW-37 is a novel nonpeptide inhibitor to
recombinant Bcl-2, Bcl-xL andMcl-1withKi of
S1121 TW-37
Product Citation:
2013, 8(2): e56603 ]
TW-37 purchased from
Selleck
WEHI-539 is the first potent and selective
BCL-XL inhibitor with IC50 of 1.1 nM.
S7100 WEHI-539
O
Br
NH2
O
O
CN
O
O
H
N
HN
N S
S
N
OH
O
O
NH2
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mg 50 mg
Size
10 mg 50 mg
Size
5 mg 50 mg
Size
Size
100 mg
100 mg
45
Caspase / p53 / TNF-alpha
A
p
o
p
t
o
s
i
s
Caspase Inhibitors & Activators
PAC-1is a potent procaspase-3activator with
EC50 of 0.22 M and the first small molecule
known to directly activate procaspase-3 to
caspase-3.
S2738 PAC-1
Apoptosis Activator 2 strongly induces
caspase-3 activation, PARP cleavage, and
DNA fragmentation which leads to the
destruction of cells (Apaf-1 dependent) with
IC50 of ~4 M, inactive to HMEC, PREC, or
MCF-10A cells.
S2927 Apoptosis Activator 2
Z-VAD-FMK is a cell-permeable, irreversible
pan-caspase inhibitor, blocks all features of
apoptosis.
S7023 Z-VAD-FMK
5 mg
Size
p53 Inhibitors & Activators
J NJ -26854165 acts as a HDM2 ubiquitin
ligase antagonist and also induces early
apoptosis in p53 wild-type cells, inhibits
cellular proliferation followed by delayed
apoptosis in the absence of functional p53.
Phase 1.
S1172 JNJ 26854165 (Serdemetan)
Size
Size
5 mg 10 mM/1 mL in DMSO
Size
RITA (NSC 652287) induces both
DNA-protein and DNA-DNA cross-links with
no detectable DNA single-strand breaks, and
also inhibits MDM2-p53 interaction by
targeting p53.
S2781 RITA (NSC 652287)
Pifithrin- is an inhibitor of p53, inhibiting
p53-dependent transactivation of
p53-responsive genes.
S2929 Pifithrin- (PFT)
new
NSC319726 is a potent p53(R175) mutant
reactivator with EC50 of ~8 nM.
S7149 NSC319726
5 mg
Size
N O
O
Cl
Cl
HN
O
H
N
O
O
O
F
NH
O
O
O
O
S
HO
S
OH
S
N
NH
O
HBr
N
N
H
N N
S
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
10 mM/1 mL in DMSO
46
Phone:+1-832-582-8158
www.selleckchem.com
A
p
o
p
t
o
s
i
s
TNF-alpha / Mdm2 / Survivin / IAP
Size
QNZ (EVP4593) shows potent inhibitory
activity toward both NF-B activation and
TNF- production with IC50 of 11 nM and 7
nM, respectively.
S4902 QNZ (EVP4593)
5 mg 25 mg
Size
Thalidomide was introduced as a sedative
drug, immunomodulatory agent and also is
investigated for treating symptoms of many
cancers. Thalidomide inhibits an E3 ubiquitin
ligase which is a CRBN-DDB1-Cul4A
complex.
S1193 Thalidomide
Survivin Inhibitor
YM155 is a potent Survivin suppressant by
inhibiting Survivin promoter activity with IC50
of 0.54nM; does not significantlyinhibit SV40
promoter activity, but is observed to slightly
inhibit the interaction of Survivin with XIAP.
Phase 1/2.
S1130 YM155
Product Citations:
Leukemia, 2012, 26(4): 623-32
Data from[ Proc Natl Acad
Sci U S A, 2012, 109(2):
600-5 ]
YM155 purchased from
Selleck
N
O
O
HN
O
O
N N
H
N
NH2
O
GDC-0152 is a potent antagonist of
XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and
cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM
and43nM, respectively; less affinityshownto
cIAP1-BIR2 and cIAP2-BIR2. Phase 1.
S7010 GDC-0152
10 mg 100 mg
Size
T-3256336 is a selective antagonist of IAP,
mostly for cIAP-1 and cIAP-2 with IC50 of 1.3
nM and 2.2 nM, respectively; ~100-fold less
potent to XIAP, also activates TNF--
dependent extrinsic apoptosis.
S7017 T-3256336
5 mg 50 mg
Size
10 mg 50 mg
Size
new
LCL161 is an oral small molecule antagonist
of Inhibitor of Apoptosis Proteins (IAPs).
S7009 LCL161
Size
Birinapant (TL32711) is a SMAC mimetic
antagonist, mostly to cIAP1 with Kd of <1 nM,
less potent to XIAP. Phase 1/2.
S7015 Birinapant
5 mg 50 mg
Size
IAP Antagonists
AT-406 is a potent Smac mimetic and an
antagonist of IAP (inhibitor of apoptosis
protein via E3 ubiquitin ligase), binding to
XIAP, cIAP1andcIAP2withKi of 66.4nM, 1.9
nM, and 5.1 nM, 50- to 100-fold higher
affinities thantheSmacAVPI peptide. Phase1.
S2754 AT406 (SM-406, ARRY-334543)
H
N
N
H
O
N
O
OH
NH
HN
F
F
N
O H
N
HO
O
N
H
S
N N
NH
O
N
O
H
N
O
N
H
N
H
O
H
N
F F
N
O
N
O
N
H
O
O
H
N
N
O N
S
O
F
O
N
H
10 mM/1 mL in DMSO
5 mg 25 mg 100 mg
Size
Mdm2 Chemicals
Nutlin-3 is a potent and selective Mdm2
(RING finger-dependent ubiquitin protein
ligase for itself and p53) antagonist with IC50
of 90 nM; stabilizes p73 in p53-deficient cells.
S1061 Nutlin-3
Product Citations:
2012, 3: e294 ]
Nutlin-3 purchased from
Selleck
S2678 NSC 207895
NSC-207895 suppresses MDMX with IC50 of 2.5 M, leading to
enhanced p53 stabilization/activation and DNA damage, and also
regulates MDM2, an E3 ligase.
10 mM/1 mL in DMSO
5 mg 25 mg 100 mg
Size
Page 45
Tenovin-1 protects against MDM2-mediated
p53 degradation, which involves
ubiquitination, and acts through inhibition of
protein-deacetylating activities of SirT1 and
SirT2.
S8000 Tenovin-1
NSC-207895 suppresses MDMX with IC50 of
2.5 M, leading to enhanced p53 stabilization
/activation and DNA damage, and also
S2678 NSC 207895
5 mg 50 mg 200 mg
Size
N
H
N
H
O S
H
N
O
Size
TNF-alpha Inhibitors
Lenalidomide (Revlimid, CC-5013) is a TNF-
secretion inhibitor with IC50 of 13 nM.
S1029 Lenalidomide (CC-5013)
Product Citations:
Blood, 2012, 119(9): 2074-82
Clin Cancer Res, 2011, 17(16): 5311-21
Data from[ Clin Cancer
Res, 2011, 17: 3259-71 ]
Lenalidomide purchased
fromSelleck
Pomalidomide inhibits LPS-induced TNF-
release with IC50 of 13 nM.
S1567 Pomalidomide
Product Citation:
Blood, 2011, 118(18): 4771-9
118(18): 4771-9 ]
Pomalidomide purchased
fromSelleck
Necrostatin-1 is a specific RIP1 inhibitor and
inhibits TNF--induced necroptosis with EC50
of 490 nM.
S8037 Necrostatin-1
N
H
N
H
N
O
S
10 mM/1 mL in DMSO
50 mg 500 mg
Size
10 mM/1 mL in DMSO
5 mg 50 mg 200 mg
Size
10 mg 50 mg
Size
10 mM/1 mL in DMSO
47
EGFR / J AK
J
A
K
/
S
T
A
T
JAK/STAT Pathway
Growth Factor
Tyk Tyk J AK J AK
c-Myc
CDK
Pim1
Bcl2
Src
STAT
STAT
STAT
DNA
STAT STAT
STAT SOCS
STAT
p21
Ras
Rac
MLK
p38
J NK
ERK1/2
MKK1/2
Raf
PI3K
Akt
mTOR
Cytokine
ISRE/GAS
Cell Growth, Survival,
Differentiation and Oncogenesis
Pan-PI3K inhibitors
BEZ235
LY294002
GDC-0941
BYL719(p110)
GSK2636771(p110)
TGX-221(p110)
AS-252424(p110)
CAL-101(p110)
IPI-145(p110)
Pan-Akt inhibitors
MK-2206
GSK690693
GDC-0068
A-674563(Akt1)
CCT128930(Akt2)
Pan-mTOR inhibitors
AZD8055
INK 128
Rapamyci n
PF-04691502(mTORC1)
Pan-JAK inhibitors
Selective JAK inhibitors
Ruxol i ti ni b
AZD1480
Cyt387
TG101348(JAK2)
Tofaci ti ni b ci trate(JAK3)
Pan-Pim inhibitor
SGI-1776
Selective Pim inhibitor
SMI-4a(Pi m1)
Selective STAT inhibitors
Fl udarabi ne(STAT1)
NSC 74859(STAT3)
Ni cl osami de(STAT3)
EGFR Inhibitors
JAK Inhibitors
INCB018424 is the first potent, selective,
J AK1/2 inhibitor to enter the clinic with IC50 of
3.3 nM/2.8 nM, >130-fold selectivity for
J AK1/2 versus J AK3. Phase 3.
S1378 Ruxolitinib (INCB018424)
Tofacitinib citrate (CP-690550 citrate) is a
novel inhibitor of J AK3 with IC50 of 1 nM, 20-
to 100-fold less potent versus J AK2 and
J AK1. Phase 3.
S5001 Tofacitinib citrate
(CP-690550 citrate)
Product Citations:
J Exp Med, 2012, 209(2): 259-73
Blood, 2011, 118(14): 3911-21
Data from[ J Immunol,
2012, 189(6): 2784-92 ]
Tofacitinib citrate
J AK3selective Licensed by Pfizer
Product Citations:
Genes Dev, 2012, 26(19): 2144-53
J Immunol, 2012, 189(6): 2784-92
2012, 287(41): 34825-35 ]
Ruxolitinib purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 100 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg
Size
48
Phone:+1-832-582-8158
www.selleckchem.com
J
A
K
/
S
T
A
T
J AK
AZD1480 is a novel ATP-competitive J AK2
inhibitor with IC50 of 0.26 nM, selectivity
against J AK3 and Tyk2, and to a smaller
extent against J AK1. Phase 1/2.
S2162 AZD1480
Product Citation:
Leukemia, 2012, 26(4): 708-15
by M.Sc. Karoline Gaebler
and Dr. Claude Haan of
Universit du Luxembourg
Selleck
CYT387 is an ATP-competitive inhibitor of
J AK1/J AK2 with IC50 of 11 nM/18 nM,
~10-fold selectivity versus J AK3. Phase 1/2.
S2219 Cyt387
Product Citation:
Blood, 2012, 120(19): 4093-103
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mM/1 mL in DMSO
5 mg 50 mg 200 mg
Size
S1134 AT9283
AT9283 is a potent J AK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also
potent to Aurora A/B, Abl(T315I). Phase 1/2.
Page 40
S2692 TG101209
TG101209 is a selective J AK2 inhibitor with IC50 of 6 nM, less potent
to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for
J AK2 than J AK3, sensitive to J AK2V617F and MPLW515L/K
mutations.
J AK2selective
S1143 AG-490
AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 M,
135-fold more selective for EGFR versus ErbB2, also inhibits J AK2
with no activity to Lck, Lyn, Btk, Syk and Src.
J AK2selective
J AK2selective
5 mg 100 mg
Size
BMS-911543 is a potent and selective
inhibitor of J AK2 with IC50 of 1.1 nM, ~350-,
75- and 65-fold selective to J AK1, J AK3 and
TYK2, respectively. Phase 1/2.
S7144 BMS-911543 new
N N
N
O
N
N
N
H
N N
Page 22
Page 32
J AK2selective
LY2784544 is a potent J AK2 inhibitor with
IC50 of 3 nM, effective in J AK2V617F, 8- and
20-fold selective versus J AK1 and J AK3.
Phase 2.
S2179 LY2784544
by M.Sc. Karoline Gaebler
Selleck
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
J AK2selective
NVP-BSK805 is a potent and selective
ATP-competitive J AK2 inhibitor with IC50 of
0.5 nM, >20-fold selectivity towards J AK1,
J AK3 andTYK2.
S2686 NVP-BSK805 2HCl
Product Citation:
PLoS One, 2013, 8(5): e63301
by Dr. Catherine Rolvering
NVP-BSK805 2HCl
J AK2selective
AZ 960 is a novel ATP competitive J AK2
inhibitor with IC50 and Ki of <3 nM and 0.45
nM, 3-fold selectivity of AZ960 for J AK2 over
J AK3.
S2214 AZ 960
du Luxembourg
AZ 960 purchased from
Selleck
J AK2selective
TG-101348 (SAR302503) is a selective
inhibitor of J AK2 with IC50 of 3 nM, 35- and
334-fold more selective for J AK2 versus
J AK1 and J AK3. Phase 1/2.
S2736 TG101348 (SAR302503)
du Luxembourg
TG101348 purchased from
Selleck
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
10 mM/1 mL in DMSO
5 mg 10 mg 50 mg
Size
Tofacitinib is a novel inhibitor of J AK3 with
IC50 of 1 nM, 20- to 100-fold less potent
versus J AK2 and J AK1. Phase 3.
S2789 Tofacitinib
(CP-690550, Tasocitinib)
Product Citations:
Genes Dev, 2012, 26(19): 2144-53
Blood, 2012, 120(4): 709-19
Data from[ J Infect Dis,
2012, 205(11): 1705-8 ]
Tofacitinib purchased from
Selleck
J AK3selective
Licensed by Pfizer
N
N N
H
N
N
O
CN
10 mM/1 mL in DMSO
5 mg 50 mg 100 mg
Size
49
J AK
TG101348
Tofacitinib
WP1066
CEP33779
Baricitinib
WHI-P154
Tofacitinib citrate
ZM 39923 HCl
S2736
S2789
S2796
S2806
S2851
S2867
S5001
S8004
+++
++
5.9 nM [IC50]
4.4 M [IC50]
+++
++
+++
+++
3 nM [IC50]
2.3 M [IC50]
1.8 nM [IC50]
5.7 nM [IC50]
++++
++
++++
++
1 nM [IC50]
1.8 M [IC50]
1 nM [IC50]
7.1 M [IC50]
STAT3
SRC, ERBB1(EGFR)
AT9283
AG-490
AZD1480
LY2784544
AZ960
TG101209
S1134
S1143
S2162
S2179
S2214
S2692
+++1.3 nM [IC50]
+++
++
++++
+
+++
+++
1.2 nM [IC50]
10 M [IC50]
0.26 nM [IC50]
55 nM [IC50]
3 nM [IC50]
6 nM [IC50
Cat.No. Inhibitor Name JAK1 JAK2
+++
+
1.1 nM [IC50]
169 nM [IC50]
JAK3 Other
Abl, Aurora A, Aurora B
ERBB1(EGFR), ERBB2(Her2)
FLT3, c-RET
J
A
K
/
S
T
A
T
5 mg 200 mg 50 mg
Size
Baricitinib is a selective J AK1 and J AK2
inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70
and~10-foldselective versus J AK3andTyk2,
no inhibition to c-Met and Chk2. Phase 3.
S2851 Baricitinib (LY3009104, INCB028050)
WP1066 is a novel inhibitor of J AK2 and
STAT3 with IC50 of 2.30 M and 2.43 M in
HEL cells; shows activity to J AK2, STAT3,
STAT5, and ERK1/2 not J AK1 and J AK3.
S2796 WP1066
CEP33779 is a selective J AK2 inhibitor with
IC50 of 1.8 nM, >40- and >800-fold versus
J AK1 andTYK2.
S2806 CEP33779 J AK2selective
N N
N N
N
N
H
N
S
O
O
O
H
N (S) (S)
N
N Br
N
HN
N
N
N N
S
O
O
100 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 10 mg 25 mg
Size
10 mM/1 mL in DMSO
S2867 WHI-P154
WHI-P154 is a potent J AK3 inhibitor with IC50 of 1.8 M, no activity
against J AK1 or J AK2, also inhibits EGFR, Src, Abl, VEGFR and
MAPK, prevents Stat3, but not Stat5 phosphorylation.
Page 25
S-Ruxolitinib is the chirality of INCB018424,
which is the first potent, selective, J AK1/2
inhibitor to enter the clinic with IC50 of 3.3
nM/2.8 nM, >130-fold selectivity for J AK1/2
versus J AK3. Phase 3.
S2902 S-Ruxolitinib (INCB018424)
Product Citation:
Genes Dev, 2012, 26(19): 2144-53
Data from[ Genes Dev,
2012, 26(19): 2144-53 ]
S-Ruxolitinib purchased
fromSelleck
ZM39923 is an J AK1/3 inhibitor with pIC50 of
4.4/7.1, almost no activity to J AK2 and
modestly potent to EGFR; also found to be
sensitive to transglutaminase.
S8004 ZM 39923 HCl
O
N
HCl
10 mM/1 mL in DMSO
100 mg 5 mg 50 mg
Size
10 mg 50 mg
Size
10 mM/1 mL in DMSO
50
Phone:+1-832-582-8158
www.selleckchem.com
STAT / Pim
STAT Inhibitors
NSC 74859(S3I-201) shows potent inhibition
of STAT3 DNA-binding activity with IC50 of 86
M, and low activity towards STAT1 and
STAT5.
S1155 S3I-201
Product Citations:
Cancer Discov, 2013, 3(2): 158-67
Int J Cancer, 2012, 131(12): 2774-84
2013, 3(2): 158-67 ]
S3I-201 purchased from
Selleck
STAT3selective
Pim Inhibitors
SMI-4a is a potent inhibitor of Pim1 with IC50
of 17 nM, modest potent to Pim-2, does not
significantly inhibit other serine/threonine- or
tyrosine-kinases.
S8005 SMI-4a Pim1selective
Fludarabine (Fludara, F-ara-A, NSC 118218)
is a STAT1 activation inhibitor and a DNA
synthesis inhibitor.
S1491 Fludarabine STAT1selective
Stattic, the first nonpeptidic small molecule,
potentlyinhibits STAT3activationandnuclear
translocation with IC50 of 5.1 M, highly
selectivity over STAT1.
S7024 Stattic STAT3selective
Niclosamide can inhibit DNA replication and
inhibit STAT with IC50 of 0.7 M.
S3030 Niclosamide
50 mg
Size
STAT3selective
SGI-1776 is a novel ATP competitive inhibitor
of Pim1 with IC50 of 7 nM, 50- and 10-fold
selective versus Pim2 and Pim3, also potent
to Flt3 and haspin. Phase 1.
S2198 SGI-1776 free base
Product Citation:
Data from[ Pharmacol Res,
2013, 70(1): 90-101 ]
SGI-1776 free base
CX-6258 is a potent, selective, and orally
efficacious Pim1, Pim2 and Pim3 inhibitor
with IC50 of 5 nM, 25 nM and 6 nM,
respectively.
S7041 CX-6258 new
J
A
K
/
S
T
A
T
O
NH
HO
N+
O
-O
Cl
Cl
S
O
O
O2N
S
HN
O
O
F
F
F
N
H
O
Cl
O
O
N N
100 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
25 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mM/1 mL in DMSO
5 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
2 mg 10 mg 50 mg
Size
Pim1selective
N
N
N
OCF3
N
H
N
10 mg 50 mg
Size
51
MEK
M
A
P
K
MAPK Pathway
MEK Inhibitors
AZD6244 (Selumetinib, ARRY-142886) is a
potent, highly selective MEK1 inhibitor with
IC50 of 14 nM, also inhibits ERK1/2
phosphorylation with IC50 of 10 nM, no
inhibition to p38, MKK6, EGFR, ErbB2,
ERK2, B-Raf, etc. Phase 1/2.
S1008 Selumetinib (AZD6244)
Product Citations:
Nature, 2012, 487(7408): 505-9
Nature, 2010, 468(7326): 973-7
Nature, 2010, 468(7326): 968-72
Sci U S A, 2009, 106(48):
20411-6 ]
Selumetinib purchased from
Selleck
MEK1selective
10 mM/1 mL in DMSO
50 mg 500 mg
Size
PD0325901(PD325901) is selective andnon
ATP-competitive MEK inhibitor with IC50 of
0.33 nM, roughly 500-fold more potent than
CI-1040 on phosphorylation of ERK1 and
ERK2. Phase 1/2.
S1036 PD0325901
Product Citations:
Cell, 2012, 151(5): 937-50
Cell Stem Cell, 2012, 10(2): 210-7
Data from[ Nat Methods,
2011, 8(6): 487-93 ]
Selleck
Licensed by Pfizer
10 mM/1 mL in DMSO
5 mg 25 mg 100 mg
Size
52
Phone:+1-832-582-8158
www.selleckchem.com
M
A
P
K
MEK
GSK1120212 (J TP-74057, trametinib) is a
highly specific and potent MEK1/2 inhibitor
with IC50 of 0.92 nM/1.8 nM, no inhibition of
the kinase activities of c-Raf, B-Raf, ERK1/2.
Phase 3.
S2673 Trametinib (GSK1120212)
Product Citation:
Sci U S A, 2012, 109(31):
E2127-33 ]
Trametinib purchased from
Selleck
CH5126766 (RO5126766) is a novel
allosteric MEK inhibitor for MEK1 and MEK2
with Kd of 2.9 nM and 13 nM, respectively.
S7170 CH5126766 (RO5126766) new
PD 198306 is a cell-permeable and highly
selective MEK inhibitor with IC50 of 8 nM.
S7210 PD 198306 new
PD98059 is a non-ATP competitive MEK
inhibitor with IC50 of 2 M, specifically inhibits
MEK-1-mediated activation of MAPK; does
not directly inhibit ERK1 or ERK2.
S1177 PD98059
Product Citations:
J Natl Cancer Inst, 2012, 104(21): 1673-9
Sci Signal, 2011, 4(192): ra62
Data from[ J Natl Cancer
Inst, 2012, 104(21): 1673-9 ]
Selleck
U0126-EtOH is a highly selective inhibitor of
MEK1/2 with IC50 of 0.07 M/0.06 M,
100-fold higher affinity for N3-S218E/S222D
MEK than PD098059.
S1102 U0126-EtOH
Product Citations:
Nat Genet, 2011, 44(2): 133-9
Data from[ J Invest
Dermatol, 2012, 132(12):
2780-90 ]
U0126-EtOH purchased
fromSelleck
CI-1040 (PD 184352) is an ATP non-
competitive MEK1/2 inhibitor with IC50 of 17
nM, 100-fold more selective for MEK1/2 than
MEK5. Phase 2.
S1020 CI-1040 (PD184352)
Product Citations:
Nat Genet, 2011, 44(2): 133-9
Science, 2011, 331(6019): 912-6
Data from[ J Exp Med,
2011, 208(9): 1889-900 ]
CI-1040 purchased from
Selleck
MEK1selective
BIX02189is a selective inhibitor of MEK5with
IC50 of 1.5 nM, also inhibits ERK5 catalytic
activity with IC50 of 810 nM, does not inhibit
closely related kinases MEK1, MEK2, ERK2,
and J NK2.
S1531 BIX 02189
Product Citation:
J Biol Chem, 2012, 287(48): 40722-31
2012, 287(48): 40722-31 ]
BIX 02189 purchased from
Selleck
MEK5selective
AS703026 is a highly selective, potent, ATP
non-competitive allosteric inhibitor of MEK1/2
with IC50 of 0.005-2 M in MM cell lines.
Phase 1/2.
S1475 AS703026 (Pimasertib)
Data independently
produced by Dr. Zhang of
Tianjin Medical University
AS703026 purchased from
Selleck
N
N O O
N
N
H
S
N
H
O O
F
O
O
N
H
HN
I
F
F
F O
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
5 mg 25 mg 200 mg
Size
10 mM/1 mL in DMSO
25 mg 100 mg 300 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg 200 mg
Size
10 mM/1 mL in DMSO
5 mg 100 mg
Size
D
M
S
O
U
0
1
2
6
C
I-1
0
4
0
G
D
C
-0
8
7
9
P
D
8
9
0
5
9
D
M
S
O
U
0
1
2
6
C
I-1
0
4
0
G
D
C
-0
8
7
9
P
D
8
9
0
5
9
D
M
S
O
U
0
1
2
6
C
I-1
0
4
0
G
D
C
-0
8
7
9
P
D
8
9
0
5
9
c-J un
P-Erk1/2
Erk1/2
GAPDH
10 mg 50 mg
Size
10 mg
Size IP3 Ca2+
Lin-1
RSK
SOS
ER81
GSK3
BAD
IkB
CREB
ATF4
c-Fos
c-J un
MNK
MNK1
MSK
Histone H3
AKT
ATF1
STAT3
p65
Paxillin
ASK1
TAO1,2
MLK2
MLK3
MLK1 DLK
Bax
Bid
DUSP1
Bcl2
MEKK1-4
MKK4,7
MEKK1-4
J NK1,2,3
MKK3,6
p38MAPK,
p38MAPK,
TAK1
Vinexin
MEF2
ATF1/2/6
SAP-1
ELK-1
c-J un
STAT4
J unD
HSF-1
ATF2
ETS-1
NFK3 p53
p53
J NK
14-3-3
CREB
eEF2K
MK2,3
MEK1,2
MAPK
MAP2K
Neurofilament
eIF4E
ERK1,2
ERK1,2
PKC Ras
CaMK PLC
A-Raf
B-Raf
Raf-1
Cytokines UV
Inflammatory
Stress,LPS
GPCR
MAP3K
LPS
CDC40
TNFRII
TCR
TAK1
Pan-Raf inhibitors
Vemurafeni b
Sorafeni b
PLX-4720
GDC-0879(B-Raf)
GW5074(C-Raf)
Pan-MEK inhibitors
Selective MEK inhibitors
PD0325901
GSK1120212
U0126-EtOH
AZD6244(MEK1)
BIX 02189(MEK5
Pan-p38 inhibitors
Selective p38 inhibitors
SB 203580
SB 202190
VX-745
BIRB 796(p38)
LY2228820(p38)
VX-702(p38)
JNK inhibitors
SP600125
JNK-IN-8
53
MEK
M
A
P
K
5 mg 50 mg 200 mg
Size
SL327 is a selective inhibitor for MEK1/2 with
IC50 of 0.18 M/0.22 M, no activity towards
Erk1, MKK3, MKK4, c-J UN, PKC, PKA, or
CamKII; capable of transport through the
blood-brain barrier.
S1066 SL327
BIX02188is a selective inhibitor of MEK5with
IC50 of 4.3 nM, also inhibits ERK5 catalytic
activity with IC50 of 810 nM, does not inhibit
closely related kinases MEK1, MEK2, ERK2,
and J NK2.
S1530 BIX 02188 MEK5selective
Product Citation:
Exp Neurol, 2012, 238(2): 209-17
PD318088 is a non-ATP competitive
allosteric MEK1/2 inhibitor, binds
simultaneously with ATP in a region of the
MEK1 active site that is adjacent to the
ATP-binding site.
S1568 PD318088
Data independently
Selleck
AZD8330 (ARRY-424704) is a novel,
selective, non-ATP competitive MEK 1/2
inhibitor with IC50 of 7 nM. Phase 1.
S2134 AZD8330
Product Citation:
Data independently
Selleck
TAK-733 is a potent and selective MEK
allosteric site inhibitor for MEK1 with IC50 of
3.2 nM, inactive to Abl1, AKT3, c-RAF,
CamK1, CDK2/cyclinA, c-Met, etc. Phase 1.
S2617 TAK-733
Data independently
produced by J onas Nilsson,
PhDfromUniversity of
Gothenburg
TAK-733 purchased from
Selleck
S2310 Honokiol
Honokiol is the active principle of magnolia extract that inhibits
Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase3.
CI-1040
SL327
U0126-EtOH
PD98059
AS703026
BIX 02188
BIX 02189
AZD8330
TAK-733
S1020
S1066
S1102
S1177
S1475
S1530
S1531
S2134
S2617
+++
++
+++
++
+++
+++
+++
17 nM [IC50]
0.18 M [IC50]
70 nM [IC50]
2 M [IC50]
5-11 nM [IC50]
7 nM [IC50]
3.2 nM [IC50]
+++
++
+++
+++
+++
+++
17 nM [IC50]
0.22 M [IC50]
60 nM [IC50]
5-11 nM [IC50]
7 nM [IC50]
3.2 nM [IC50]
Cat.No. Inhibitor Name MEK1 MEK2 MEK5
+++
+++
4.3 nM [IC50]
1.5 nM [IC50]
F F
F
CN
S
NH2
NH2
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Page 10
54
Phone:+1-832-582-8158
www.selleckchem.com
M
A
P
K
Raf
MLN-2480 (BIIB-024) is a pan-Raf inhibitor.
S7121 MLN2480
PLX4032 (Vemurafenib, RG7204, Zelboraf,
RO5185426) is a novel andpotent inhibitor of
B-Raf(V600E) with IC50 of 31 nM.
S1267 Vemurafenib (PLX4032, RG7204)
Product Citations:
Nature, 2012, 483(7387): 100-3
Cell, 2012, 151(5): 937-50
Nat Med, 2012, ahead of print
Sci U S A, 2012, 109(31):
E2127-33 ]
Vemurafenib purchased
fromSelleck
5 mg 50 mg
Size
SB590885 is a potent B-Raf inhibitor with Ki
of 0.16 nM, 11-fold greater selectivity for
B-Raf over c-Raf, no inhibitionto other human
kinases.
S2220 SB590885
S1040 Sorafenib
Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor
of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM,
respectively.
B-Raf selective
ZM 336372 is a potent and selective c-Raf
inhibitor with IC50 of 70 nM, 10-fold selectivity
over B-RAF, no inhibition to PKA/B/C, AMPK,
p70S6, etc.
S2720 ZM 336372 C-Raf selective
Dabrafenib (GSK2118436) is a mutant
BRAFV600 specific inhibitor with IC50 of 0.8
nM, with 4- and 6-fold less potency against
B-Raf(wt) and c-Raf, respectively. Phase 3.
S2807 Dabrafenib (GSK2118436)
S2161 RAF265 (CHIR-265)
RAF265 (CHIR-265) is a potent selective inhibitor of
C-Raf/B-Raf/B-Raf
V600E
with IC50 of 3-60 nM, and exhibits potent
inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.
C-Raf selective S2202 NVP-BHG712
C-Raf selective S1178 Regorafenib (BAY 73-4506)
Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target
inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFR, Kit, RET and
Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5
nM, respectively.
Raf Inhibitors
PLX4720 is a potent and selective inhibitor of
B-Raf(V600E) with IC50 of 13 nM, modest
potent to c-Raf-1(Y340D and Y341D
mutations), 10-fold selectivity against
wild-type B-Raf.
S1152 PLX-4720
Product Citations:
Nature, 2013, 498(7452): 109-12
Nature, 2012, 483(7387): 100-3
Genes Dev, 2012, 26(10): 1055-69
Sci U S A, 2011, 108(15):
6067-72 ]
PLX-4720 purchased from
Selleck
GDC-0879 is a novel, potent, and selective
B-Raf inhibitor with IC50 of 0.13 nM with
activity against c-Raf as well; no inhibition
known to other protein kinases.
S1104 GDC-0879
Product Citations:
2011, 6(8): e23235 ]
Selleck
10 mM/1 mL in DMSO
2 mg 10 mg 25 mg
Size
10 mM/1 mL in DMSO
5 mg 25 mg 50 mg
Size
AZ628 is a new pan-Raf inhibitor for BRAF,
BRAF(V600E), and c-Raf-1 with IC50 of 105
nM, 34nM and29nM, also inhibits VEGFR2,
DDR2, Lyn, Flt1, FMS, etc.
S2746 AZ628
2013, 3(3): 350-62 ]
AZ628 purchased from
Selleck
Product Citation:
Cancer Discov, 2013, 3(3): 350-62
N
N NH2
Cl
O HN
N
S
HN
O
N
Cl
CF3
S
O
O
H
N
F
F
F
S N
N
N
NH2
100 mg 5 mg 20 mg
Size
10 mM/1 mL in DMSO
10 mM/1 mL in DMSO
100 mg 10 mg 25 mg
Size
10 mM/1 mL in DMSO
50 mg 200 mg
Size
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
Page 16
Page 17
Page 17
Page 19
0
20
40
60
80
100
120
140
0
20
40
60
80
100
120
140
0 5 25 50 100
1000 5000 0 5 25 50 100 1000 5000
32P 32P 32P 32P
D
M
S
O
D
M
S
O
In
d
iru
b
in
S
B
2
0
3
5
8
0
S
P
6
0
0
1
2
5
D
M
S
O
D
M
S
O
S
ta
u
ro
s
p
o
rin
e
K
U
5
5
9
3
3
N
U
7
0
2
6
IC
8
6
6
2
1
A
Z
D
7
7
6
8
V
X
-6
8
0
P
L
X
-4
7
2
0
G
D
C
-0
8
7
9
IC
2
6
1
P
P
1
P
D
9
8
0
5
9
M
e
th
a
n
o
l
T
D
Z
D
-8
T
D
Z
D
-2
0
R
o
s
c
o
v
itin
e
R
O
-3
1
-8
2
2
0
C
d
k
1
In
h
ib
ito
r
O
x
in
d
o
le
l
H3
GST-VRK2A
H3
GST-VRK2A
H3
GST-VRK2A
H3
GST-VRK2A
GST-VRK2A
H3
GST-VRK2A
H3
Coomassie Coomassie Coomassie Coomassie
55
Raf / p38 MAPK
M
A
P
K
GDC-0879
PLX-4720
Regorafenib
SB590885
ZM 336372
AZ628
Dabrafenib
GW5074
CEP-32496
S1104
S1152
S1178
S2220
S2720
S2746
S2807
S2872
S8015
+++ 2.5 nM [IC50]
++++
++
++++
+
++++
0.13 nM [IC50]
13 nM [IC50]
0.16 nM [Ki]
100 nM [IC50]
0.8 nM [IC50]
Cat.No. Inhibitor Name B-Raf C-Raf Other
+++
+
++
+++
+++
++
6.7 nM [IC50]
70 nM [IC50]
29 nM [IC50]
5 nM [IC50]
9 nM [IC50]
39 nM [IC50]
PDGFR-, VEGFR1, c-RET, VEGFR3, VEGFR2, c-Kit
CSF-1R
CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and
c-Raf with Kd of 14 nM/36 nM and 39 nM, modest potent to Abl-1,
c-Kit, Ret, PDGFR and VEGFR2, respectively; insignificant affinity
for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
S8015 CEP-32496
10 mM/1 mL in DMSO
5 mg 50 mg 200 mg
Size
BIRB 796 (Doramapimod) is a highly
selective p38 MAPK inhibitor with Kd of 0.1
nM, 330-fold greater selectivity versus J NK2,
weak inhibition for c-RAF, Fyn and Lck,
insignificant inhibition of ERK-1, SYK, IKK2,
ZAP-70, EGFR, HER2, PKA, PKC, PKC//.
S1574 BIRB 796 (Doramapimod)
Product Citations:
Blood, 2012, 119(26): 6255-8
Biochem J, 2013, 449(2): 497-506
2013, 8(1): e54181 ]
BIRB 796 purchased from
Selleck
p38 MAPK selective
PF-04880594 is a RAF inhibitor for
BRAF/BRAF(V599E) and c-RAF with IC50 of
0.19 nM/0.13 nM and 0.39 nM, >100-fold
selectivity over CSNK1, J NK2/3 and p38.
S7001 PF-04880594
10 mg 50 mg
Size
N N
H
N N
N
N
N
H
F
F
N
Page 37
10mM/1mLinDMSO
5mg 25mg
Size
S2200 Raf265 derivative
A derivative of Raf265, however, the effects of this derivative are not
known.
Product Citation:
GW5074 is a potent and selective c-Raf
inhibitor with IC50 of 9 nM, no effect on the
activities of J NK1/2/3, MEK1, MKK6/7,
CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms
is noted.
S2872 GW5074
Data from[ Mol Cell
745-57 ]
GW5074 purchased from
Selleck
C-Raf selective
H
N
O
I
OH
Br
Br
Page 20
W
T
2
7
oC
3
7
oC
D
M
S
O
T
C
S
2
3
1
2
P
D
0
3
2
5
9
0
1
S
U
6
6
6
8
R
D
E
A
1 1
9
P
11
0
3
S
K
F
8
6
0
0
2
A
Z
D
0
5
3
0
C
8
8
6
3
G
W
5
0
7
4
A
lste
rp
a
u
llo
n
e
band C
band B
actin
kDa
170
130
anti actin
Blot:
anti
CFTR
56
Phone:+1-832-582-8158
www.selleckchem.com
M
A
P
K
p38 MAPK
SB 202190 (FHPI) is a potent p38 MAPK
inhibitor targeting p38/ with IC50 of 50 nM
/100 nM, sometimes used instead of SB
203580 to investigate potential roles for
SAPK2a/p38 in vivo.
S1077 SB 202190
Product Citation:
J Biol Chem, 2010, 285: 32824-33
2010, 285: 32824-33 ]
SB 202190 purchased from
Selleck
LY2228820 is a novel and potent inhibitor of
p38 MAPK with IC50 of 7 nM, does not alter
p38 MAPK activation. Phase 1/2.
S1494 LY2228820
Product Citation:
Blood, 2012, 119(26): 6255-8
10 mg 50 mg
Size
10 mg 50 mg
Size
Vinorelbine (Navelbine) is an anti-mitotic
agent which inhibits the proliferation of Hela
cells with IC50 of 1.25 nM.
S1527 Vinorelbine
10 mg 50 mg 200 mg
Size
VX-745 is a potent and selective inhibitor of
p38 with IC50 of 10 nM, 22-fold greater
selectivity versus p38 and no inhibition to
p38.
S1458 VX-745 p38 MAPK selective
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
TAK 715 is a p38 MAPK inhibitor for p38
with IC50 of 7.1 nM, 28-fold more selective for
p38 over p38, no inhibition to p38/,
JNK1, ERK1, IKK, MEKK1 or TAK1. Phase 2.
S2928 TAK 715 p38 MAPK selective
2011, 10(12): 2244-56 ]
Selleck
VX-702 is a highly selective inhibitor of p38
MAPK, 14-fold higher potency against the
p38 versus p38. Phase 2.
S6005 VX-702
Data independently
produced by Lee lay hoon
fromNational University of
Singapore
VX-702 purchased from
Selleck
p38 MAPK selective
Skepinone-L is anATP-competitive p38
MAPK inhibitor with IC50 of 5 nM.
S7214 Skepinone-L new
PH-797804 is a novel pyridinone inhibitor of
p38 with IC50 of 26nM; 4-foldmore selective
versus p38 and does not inhibit JNK2.
Phase 2.
S2726 PH-797804
PH-797804 purchased from
Selleck
O O
HO
OH
H
N
F
F
O
NH
N
S
N
10 mM/1 mL in DMSO
5 mg 50 mg 200 mg
Size
10 mg 50 mg
Size
10 mM/1 mL in DMSO
10 mM/1 mL in DMSO
25 mg 100 mg
Size
10 mM/1 mL in DMSO
5 mg 50 mg 200 mg
Size
10 mM/1 mL in DMSO
10 mg 100 mg 200 mg
Size
p38 MAPK selective
SB202190 (p38-MAPK Inhibitor)
Concentration
T
=
0
T
=
1
2
0
1 M 5 M 10 M
T
=
2
4
0
T
=
0
T
=
1
2
0
T
=
2
4
0
T
=
0
T
=
1
2
0
T
=
2
4
0
SRP72 (72 kDa)
SRP54 (54 kDa)
GAPDH (37 kDa)
Time (minutes)
Lane No 1 2 3 4 5 6 7 8 9
0
10
20
30
40
50
60
70
80
90
100
%
o
f d
is
trib
u
tio
n
G1/G0
G2/M
S
rapa
LY2228820
%apoptotic cells
U87EV
2.9 4.6 3.0 5.5 3.0 2.9 4.6 11.7
U87PTEN
-
- - - -
+ - + - - + +
+ + + +
p-p38
p38
p-J NK1/2
J NK1/2
-actin
TNF- (1 nM)
PH-797804 (M)
-
0 0 0.01 0.1 1 10
+ + + + +
SB 203580
SB 202190
VX-745
LY2228820
BIRB 796
PH-797804
TAK 715
VX-702
S1076
S1077
S1458
S1494
S1574
S2726
S2928
S6005
+
++
+++
+++
++++
++
+++
+++
0.5 M [IC50]
50 nM [IC50]
10 nM [IC50]
7 nM [IC50]
0.1 nM [Kd]
26 nM [IC50]
7.1 nM [IC50]
4-20 nM [IC50]
+
++
+
0.5 M [IC50]
100 nM [IC50]
220 nM [IC50]
Cat.No. Inhibitor Name p38- p38-
Notes:
1."+" indicates inhibitory effect. The more "+" are,
the stronger inhibition is.
2.Black "+" corresponds to IC50 or Ki values in nMs,
gray "+" refers to values in Ms.
SB203580 is a p38 MAPK inhibitor with IC50
of 0.3-0.5 M, 10-fold less sensitive to
SAPK3(106T) and SAPK4(106T) and blocks
PKB phosphorylation with IC50 of 3-5 M.
S1076 SB 203580
Product Citations:
J Biol Chem, 2010, 285: 32824-33
Biochim Biophys Acta, 2012, 1823(5): 987-96
Data from[ Cancer Lett,
2013, 332(1): 35-45 ]
Selleck
p38 MAPK Inhibitors
10 mM/1 mL in DMSO
25 mg 100 mg 200 mg
Size
57
J NK / ERK
M
A
P
K
J NK-IN-8 is the first irreversible J NK inhibitor
for J NK1, J NK2andJ NK4withIC50 of 4.7nM,
18.7 nM and 1 nM, >10-fold selectivity
against MNK2, Fms and no inhibition to c-Kit,
Met, PDGFR.
S4901 JNK-IN-8
5 mg
Size
JNK Inhibitors
Product Citations:
Biochim Biophys Acta, 2012, 1823(5): 987-96
Mol Cancer, 2011, 10: 66
SP600125 is a broad-spectrumJ NK inhibitor
for J NK1, J NK2 and J NK3 with IC50 of 40 nM,
40 nM and 90 nM, respectively; 10-fold
greater selectivity against MKK4, 25-fold
greater selectivity against MKK3, MKK6,
PKB, and PKC, and 100-fold selectivity
against ERK2, p38, Chk1, EGFR etc.
S1460 SP600125
Data independently
produced by Lee lay hoon
fromNational University of
Singapore
SP600125 purchased from
Selleck
O
HN NH
N
N
N
NH
O
N
SCH772984 is a novel, specific inhibitor of
ERK1/2 with IC50 of 4 nM and 1 nM,
respectively.
S7101 SCH772984
5 mg 50 mg
Size
ERK Inhibitor
HN
N NH
O
N N
O
N
N
N
10 mM/1 mL in DMSO
10 mg 50 mg 200 mg
Size
58
Phone:+1-832-582-8158
www.selleckchem.com
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S
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Akt / Bcr-Abl / FAK / Wnt/beta-catenin
Size
Skepinone-L is an ATP-competitive p38
MAPK inhibitor with IC50 of 5 nM.
S7214 Skepinone-L new Focal
adhesion
assembly
MLC
MLCK
MBS
Profilin
Cofilin
Cofilin
LIMK1,2
APC
NMDA
F2R/CD14
Integrin
F2
G12,13
Rac1GEF
Growth Factor
RhoGEF Calcineurin
ADF/Cofilin
Rho
Insulin
G
Sos
Ras
Raf
MEK
ERK
Rac
ROCK1,2
PI3K
Src
FAK
Cas
Y421 Y456 Y482 CrkII
Dock180
Cortactin
Cortactin
FN1
FGD1/3
Cdc42
IQGAP
Adherens
junction
NHE1
PI4P5K
PAK
ADF
LIMK
CFN
ACTN
Focal complex
assembly
Stabilization
of actin
Protein
synthesis
Vav
RAP1
GRLF1
Cortactin
Integrin
clustering
Actin polymerization
stress fiber
PIP3
PIP2
VCL
GIT1
PXN
PIP2
PIX
PI4P5K mDia
p27
p21
PFN
ERM
F-Actin Arp2/3
NWASP
Asef
F-Actin
eEF1A
eEF1B,
Actin
polymerization
PFN TMSB4
Arp2/3
PIR121
Nap125
Abi2
IRSp53
HSPC300
WAVE1
WAVE2
F-Actin
MyosinII
GPCR
Ca
2+
+P
Src inhibitors
Dasati ni b
Saracati ni b
Bosuti ni b
KX2-391
NVP-BHG712
FAK inhibitors
PF-00562271
PF-562271
NVP-TAE226
PF 573228
APC inhibitor
TAME
Pan-Raf inhibitors
Vemurafeni b
Sorafeni b
PLX-4720
GDC-0879(B-Raf)
GW5074(C-Raf)
Pan-MEK inhibitors
PD0325901
GSK1120212
U0126-EtOH
AZD6244(MEK1)
BIX 02189(MEK5)
Pan-ROCK inhibitors
Thi azovi vi n
GSK429286A
Selective ROCK inhibitors
Y-27632(ROCK1)
Fasudi l (ROCK2)
Pan-PI3K inhibitors
BEZ235
LY294002
GDC-0941
BYL719(p110)
GSK2636771(p110)
TGX-221(p110)
AS-252424(p110)
CAL-101(p110)
IPI-145(p110)
P
CDK
assembly
Cytoskeletal Signaling
Akt Inhibitors
Wnt/beta-catenin Inhibitors
Bcr-Abl Inhibitors
FAK Inhibitors
59
PKC
C
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Enzastaurin S1055 ++
39 nM [IC50] 6 nM [IC50]
+
83 nM [IC50]
+
110 nM [IC50]
Sotrastaurin S2791
Go 6983 S2911
++++
+++
++++
0.95 nM [Ki]
7 nM [IC50]
+++
7 nM [IC50]
+++
6 nM [IC50]
+++
10 nM [IC50]
+++
60 nM [IC50]
0.64 nM [Ki]
+++
2.1 nM [Ki]
+++ +++ ++++
3.2 nM [Ki] 1.8 nM [Ki] 0.22 nM [Ki]
Cat.No. Inhibitor Name PKC PKC PKC PKC PKC PKC PKC PKC
PKC Inhibitors
Staurosporine (AM-2282) is a potent PKC
inhibitor for PKC, PKC and PKC with IC50
of 2 nM, 5 nM and 4 nM, less potent to PKC
(20 nM), PKC (73 nM) and PKC (1086 nM).
Phase 3.
S1421 Staurosporine
Product Citation:
PLoS One, 2012, 7(6): e39679
2012, 7(6): e39679 ]
Staurosporine purchased
fromSelleck
2mg 10 mg 100 mg
Size
Enzastaurin (LY317615) is a potent PKC
selective inhibitor with IC50 of 6 nM, 6- to
20-fold selectivity against PKC, PKC and
PKC. Phase 3.
S1055 Enzastaurin (LY317615)
Product Citations:
Cell, 2012, 149(3): 656-70
Arthritis Rheum, 2013, 65(4): 1022-31
Data from[ Arthritis Rheum,
2013, 65(4): 1022-31 ]
Enzastaurin purchased from
Selleck
PKC selective
A potent nitrogen-containing
bisphosphonates. It inhibited proliferation of
human foetal osteoblastic cell line (hFOB)
with an IC50 of 40 M.
S1314 Zoledronic Acid
25 mg 100 mg
Size
Sotrastaurin (AEB071) is a potent selective
pan-PKC inhibitor, mostly for PKC with Ki of
0.22 nM, inactive to PKC. Phase 1/2.
S2791 Sotrastaurin
Product Citation:
Am J Physiol Cell Physiol, 2013, 304(9): C895-904
Go 6983 is a pan-PKC inhibitor against for
PKC, PKC, PKC and PKC with IC50 of 7
nM, 7nM, 6nM and10nM, respectively; less
potent to PKC and inactive to PKC.
S2911 Go 6983
Dequalinium Chloride is a PKC inhibitor with
IC50 of 7-18 M, and also a selective blocker
of apamin-sensitive K
+
channels with IC50 of
1.1 M.
S4066 Dequalinium Chloride
50 mg
Size
Midostaurin (PKC412) is a multi-targeted
kinase inhibitor, including PKC//, Syk,
Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3,
PDFR and VEGFR1/2 with IC50 ranging
from80 nM to 500 nM.
S8064 Midostaurin (PKC412)
1 mg 5 mg
Size
new
FTY720 (Fingolimod, Gilenya) is a S1P antagonist with IC50 of 0.033
nM.
+++
N
NH
N
O
O
N
N
N
N
OH
PO3H2
PO3H2
O
N N
H
N O
H3CO
NHCH 3
HN
O
O N
N N
N
NH
N N
N
H
O H
O
N
O
O
O
N
N
H
N O O
N
H
N+
H2N
N+
NH2
Cl -
Cl -
Size
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
Page 40
S
le
1
S
le
3
.
P
K
C
/
S
le
1
S
le
3
B
6
Anti-lgG2b Anti-lgG2c
B
6
S
le
1
S
le
3
P
K
C
/
S
le
1
S
le
3
.
P
K
C
/
S
le
1
S
le
3
.
P
K
C
/
S
le
1
S
le
3
B
6
Anti-lgG2b Anti-lgG2c
B
6
S
le
1
S
le
3
P
K
C
/
S
le
1
S
le
3
.
P
K
C
/
60
Phone:+1-832-582-8158
www.selleckchem.com
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Rac / HSP (e.g. HSP90)
Rac Inhibitor
HSP (e.g. HSP90) Inhibitors
NSC 23766 is an inhibitor of Rac GTPase
targeting Rac activation by guanine
nucleotide exchange factors (GEFs) with IC50
of ~50 M; does not inhibit the closely related
targets Cdc42 or RhoA.
S8031 NSC23766
Elesclomol (STA-4783) is a novel potent
oxidative stress inducer that illicits
pro-apoptosis events among tumor cells.
S1052 Elesclomol (STA-4783)
NVP-HSP990 (HSP990) is an orally
bioavailable HSP90 inhibitor for HSP90,
HSP90 and GRP94 with IC50 of 0.6 nM, 0.8
S7097 NVP-HSP990 (HSP990)
1 mg 5 mg
Size
new
VER 155008 is a novel adenosine-derived
inhibitor of HSP70 with IC50 of 0.5 M.
S7150 VER 155008
10 mg 50 mg
Size
new
IPI-504 (Retaspimycin) is a potent inhibitor
of HSP90 with EC50 of 63 nM.
S7112 IPI-504
10 mg 50 mg
Size
new
17-AAG (Tanespimycin) is a potent HSP90
inhibitor with IC50 of 5 nM, having a 100-fold
higher bindingaffinityfor HSP90derivedfrom
tumour cells than HSP90 fromnormal cells
S1141 17-AAG
Product Citations:
J Exp Med, 2012, 209(2): 259-73
Sci U S A, 2011, 108(18):
7535-40 ]
17-AAG purchased from
Selleck
17-DMAG (Alvespimycin) is a potent,
water-soluble HSP90 inhibitor with IC50 of 62
nM.
S1142 17-DMAG HCl
Product Citation:
Hepatology, 2013, 57(1): 70-80
Data from[ J Thorac Oncol,
2012, 7(7): 1078-85 ]
17-DMAG HCl purchased
fromSelleck
NVP-AUY922 (VER-52296) is a highly potent
HSP90 inhibitor for HSP90/ with IC50 of 13
nM/21 nM, weaker potency against the
HSP90familymembers GRP94andTRAP-1,
exhibits the tightest binding of any
small-molecule HSP90 ligand. Phase 1/2.
S1069 AUY922 (NVP-AUY922)
Product Citations:
PLoS Pathog, 2012, 8(11): e1003048
Br J Haematol, 2013, 160(4): 465-76
Data from[ Br J Haematol,
2013, 160(4): 465-76 ]
AUY922 purchased from
Selleck
BIIB021(CNF2024) is an orally available,
fully synthetic small-molecule inhibitor of
HSP90 with Ki and EC50 of 1.7 nM and 38
nM, respectively.
S1175 BIIB021
Product Citations:
PLoS Pathog, 2012, 8(11): e1003048
Arthritis Rheum, 2013, ahead of print
Data from[ PLoS Pathog,
2012, 8(11): e1003048 ]
BIIB021 purchased from
Selleck
5mg 25mg 50mg
Size
N
NH2
N
H
N N
NH
N
3HCl
N
N
NH
H2N
O
F
N O
CN
O
N N
N
N
NH
H2N
Cl
Cl
O
HO
OH
HO
OH
HN NH
O
OH
O
O
O
O
NH2
HCl
Size
Size
10 mM/1 mL in DMSO
200 mg 25 mg 100 mg
Size
10 mM/1 mL in DMSO
200 mg 25 mg 100 mg
Size
10 mM/1 mL in DMSO
200 mg 25 mg 100 mg
Size
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triptolide
NVP-AUY922
HSP90
HSP90
HSP72
HSP73
HSP40
HSP40-4
HSP27
a-tubulin
-
- -
- -
- -
- + +
+ +
+ +
+ +
INA-6 MM1.S
p-EGFR
PC-9 Ma-1 Ma-1/Vec Ma-1/HGF
EGFR
p-Met
Met
p-Akt
Akt
p-ERK1/2
ERK1/2
-actin
C
o
n
tro
l
E
rlo
tin
ib
1
7
-D
M
A
G
C
o
n
tro
l
E
rlo
tin
ib
1
7
-D
M
A
G
C
o
n
tro
l
E
rlo
tin
ib
1
7
-D
M
A
G
C
o
n
tro
l
E
rlo
tin
ib
1
7
-D
M
A
G
C
o
n
tro
l
E
rlo
tin
ib
1
7
-D
M
A
G
C
o
n
tro
l
E
rlo
tin
ib
1
7
-D
M
A
G
C
o
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tro
l
E
rlo
tin
ib
1
7
-D
M
A
G
HGF Control HGF Control HGF Control
61
HSP (e.g. HSP90)
NVP-BEP800 is a novel, fully synthetic
HSP90 inhibitor with IC50 of 58 nM, exhibits
>70-fold selectivity against Hsp90 family
members Grp94 andTrap-1.
S1498 NVP-BEP800
Product Citation:
PLoS Pathog, 2012, 8(11): e1003048
Data from[ PLoS Pathog,
2012, 8(11): e1003048 ]
NVP-BEP800 purchased
fromSelleck
5 mg 50 mg 200 mg
Size
HSP90 selective
SNX-2112 selectively binds to the ATP
pocket of HSP90 and HSP90 with Ka of 30
nM and 30 nM, uniformly more potent than
17-AAG.
S2639 SNX-2112 (PF-04928473)
Size
Ganetespib is an HSP90 inhibitor with IC50 of
4 nM in OSA 8 cells, induces apoptosis of
OSA cells while normal osteoblasts are not
affected; active metabolite of STA-1474.
S1159 Ganetespib (STA-9090)
Geldanamycin is a natural existing HSP90
inhibitor with Kd of 1.2 M, specifically
disrupts glucocorticoid receptor (GR)/HSP
association.
S2713 Geldanamycin
Product Citation:
Antimicrob Agents Chemother, 2013, 57(2): 1035-9 AT13387 is a selective potent Hsp90
inhibitor with IC50 of 18 nM in A375 cells,
displays a long duration of anti-tumor activity.
S1163 AT13387
Product Citation:
PLoS One, 2013, 8(4): e59315
KW-2478 is a nonansamycin HSP90
inhibitor with IC50 of 3.8 nM. Phase 1/2.
S2685 KW-2478
XL888 is an ATP-competitive inhibitor of
HSP90 with IC50 of 24 nM.
S7122 XL888
5 mg 50 mg
Size
new
AUY922
17-DMAG HCl
BIIB021
NVP-BEP800
SNX-2112
KW-2478
S1069
S1142
S1175
S1498
S2639
S2685
++
+
+++
++
+++
13 nM [IC50]
62 nM [IC50]
1.7 nM [IC50]
30 nM [Ka]
3.8 nM [IC50]
++
+
+
++
21 nM [IC50]
62 nM [IC50]
58 nM [IC50]
30 nM [Ka]
p110, p110, p110, p110
Cat.No. Inhibitor Name Hsp90- Hsp90- Other
PF-04929113 (SNX-5422) is a potent and
selective HSP90 inhibitor with Kd of 41 nM
and induces Her-2 degradation with IC50 of
37 nM. Phase 1/2.
S2656 PF-04929113 (SNX-5422)
N
N
O
HN
O
HN
H2N
O
Size
Size
Size
Size
Size
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62
Phone:+1-832-582-8158
www.selleckchem.com
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Kinesin / Microtubule Associated
ABT-751(E7010) binds to the colchicine site
on -tubulin and inhibits polymerization of
microtubules, not a substrate for the MDR
transporter and is active against cell lines
resistant to vincristine, doxorubicin, and
cisplatin. Phase 1/2.
S1165 ABT-751 (E7010)
Size
Docetaxel, an analog of taxol, is an inhibitor
of depolymerisation of microtubules through
binding to stabilized microtubules.
S1148 Docetaxel
Kinesin Inhibitors
Microtubule Associated Inhibitors
& Chemicals
Ispinesib (SB-715992, CK0238273) is a
potent, specific and reversible inhibitor of
kinesin spindle protein (KSP) with Ki
app
of 1.7
nM, no inhibitionto CENP-E, RabK6, MCAK,
MKLP1, KHC or Kif1A. Phase 1/2.
S1452 Ispinesib (SB-715992)
SB 743921is a kinesinspindle protein(KSP)
inhibitor with Ki of 0.1 nM, almost no affinity
to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and
CENP-E. Phase 1/2.
S2182 SB 743921
AZ3146 is a selective Mps1 inhibitor with IC50
of ~35 nM, contributes to recruitment of
CENP-E (kinesin-relatedmotor protein), less
potent to FAK, J NK1, J NK2, and Kit.
S2731 AZ 3146
GSK923295 is a first-in-class, specific
allosteric inhibitor of CENP-E kinesin motor
ATPase with Ki of 3.2 nM, and less potent to
mutant I182 andT183. Phase 1.
S7090 GSK923295
Paclitaxel (Taxol, Onxol, Nov-Onxol) is a
microtubule polymer stabilizer with IC50 of 0.1
pM in human endothelial cells.
S1150 Paclitaxel
Product Citations:
Am J Physiol Heart Circ Physiol, 2012, 302(11): H2211-9
BMC Cancer, 2012, 12: 541
Data from[ RSC Adv, 2011,
1: 884-92 ]
Paclitaxel purchased from
Selleck
Vincristine is an inhibitor of polymerization of
microtubules by binding to tubulin with IC50 of
32 M.
S1241 Vincristine
Product Citation:
Int J Mol Sci, 2012, 13(9): 10736-49
Product Citation:
Bioorg Med Chem, 2012, 21(4): 922-31
Fosbretabulin disodium(Combretastatin A-4
phosphate disodium, CA4P disodium) is the
water-soluble prodrug of combretastatin A4
(CA4), which is a microtubule-targeting
agent that can depolymerize tubulin with IC50
of 2.4 M.
S7204 Fosbretabulin (Combretastatin A4 Phosphate (CA4P))
Disodium
Data from[ Int J Mol Sci,
2012, 13(9): 10736-49 ]
Vincristine purchased from
Selleck
Epothilone B is a Taxol-like microtubule-
stabilizing agent with EC0.01 of 1.8 M. Phase
2.
S1364 Epothilone B (EPO906, Patupilone)
Data independently
produced by Dr. Helen Sadik
of J ohns Hopkins University
Epothilone B purchased
fromSelleck
new
O
HN
O
N
N
OH HN
N O
Cl
O
O
P
O
-O
O-
O
O
O
Na+ Na+
Size
Size
Size
10 mg 50 mg
Size
10 mg 25 mg
Size
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
25 mg 2 mg 10 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg
Size
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Microtubule Associated / PAK / Dynamin / Integrin
CYT997 is a potent microtubule
polymerization inhibitor with IC50 of 10-100
nM in cancer cell lines. Phase 1/2.
S2195 CYT997
5 mg 50 mg 200 mg
Size
Vinblastine inhibits microtubule formation
and supresses nAChR activity with IC50 of
8.9 M.
S1248 Vinblastine
Vinflunine is a new vinca alkaloid uniquely
fluorinated with the properties of mitotic-
arresting and tubulin-interacting activity.
Phase 2/3.
S2209 Vinflunine Tartrate
Nocodazole is a rapidly-reversible inhibitor of
microtubule polymerization, also inhibits Abl,
Abl(E255K) and Abl(T315I) with IC50 of 0.21
M, 0.53 M and 0.64 M, respectively.
S2775 Nocodazole
10 mg 50 mg
Size
Griseofulvin, a production fromsome strains
of the mold Penicillium griseofulvumam, is
able to inhibit cell mitosis by interfering with
microtubule function.
S4071 Griseofulvin
25 mg
Size
Epothilone A is a Taxol-like microtubule-
stabilizing agent with EC0.01 of 2 M.
S1297 Epothilone A
PAK Inhibitor
IPA-3 is a selective non-ATP competitive
Pak1 inhibitor with IC50 of 2.5 M, no inhibition
to group II PAKs (PAKs 4-6).
S7093 IPA-3
5mg 50mg
Size
Dynamin Inhibitors
Dynasore is a cell-permeable, reversible
non-competitive dynamininhibitor of GTPase
activity of dynamin 1/2, with IC50 of 15 M,
also inhibits the mitochondrial dynamin Drp1,
with no effect against other small GTPase.
S8047 Dynasore
Mdivi-1 is a selective cell-permeable inhibitor
of mitochondrial division DRP1 (dynamin-
related GTPase) and mitochondrial division
Dynamin I (Dnm1).
S7162 Mdivi-1 new
Integrin Inhibitors
RGD (Arg-Gly-Asp) Peptides is a cell
adhesion motif which can mimic cell adhesion
proteins and bind to integrins.
S8008 RGD (Arg-Gly-Asp) Peptides
10mg
Size
Cilengitide (EMD 121974, NSC 707544) is a
potent integrin inhibitor for v3 receptor and
v5 receptor with IC50 of 4.1 nM and 79 nM,
respectively; ~10-fold selectivity against
gpIIbIIIa. Phase 2.
S7077 Cilengitide
N
H Et
OAc
OH
O O
NH
O
O
N
H
N OH
Et
H
O O
O
O
O
Cl
O O
O
S
S
HO
OH
HO
HO
N
N
H
O
HO
N
N
O
O
Cl
Cl
SH
N
H
OH
O
O OH
O
H
N
O
H2N
NH
H2N NH
N
NH HN
NH HN
O
O
HN
O
O
O
O
NH
NH2
HO
Size
Size
Size
Size
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S
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10 mg 50 mg
Size
10 mg 50 mg
Size
64
Phone:+1-832-582-8158
www.selleckchem.com
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Rac / CDK
Cell Cycle
CDK Inhibitors
PD 0332991 is a highly selective inhibitor of
CDK4/6 with IC50 of 11 nM/16 nM. It shows no
activity against CDK1/2/5, EGFR, FGFR,
PDGFR, InsR, etc. Phase 2/3.
PD 0332991 HCl
Product Citations:
Pigment Cell Melanoma Res, 2013, 26(2): 236-46
Data from
[ Pharmacogenomics J,
2013, 13(1): 94-104 ]
PD 0332991 HCl purchased
fromSelleck
Rac Inhibitor
S1116
N
N N
O
O N
H
N
N
HN
HCl
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
P
P
P
P
Pan-CDK inhibitors
PD 0332991(CDK4 & CDK6)
Di naci cl i b(CDK1,2,5 &9)
AT7519(CDK1,2,3,4,5 & 6
Selective CDK inhibitor
BS-181(CDK7)
ATM/ATR inhibitors
KU-55933
KU-60019
VE-821
CP-466722
BEZ235
Wortmanni n
Pan-CDK inhibitors
PD 0332991(CDK4 & CDK6)
Di naci cl i b(CDK1,2,5 &9)
AT7519(CDK1,2,3,4,5 & 6)
Selective CDK inhibitor
BS-181(CDK7)
p53 activators
JNJ 26854165
RITA
Tenovi n-1
p53 inhibitor
Pifithrin-
PLK inhibitors
BI 2536
BI6727
Ri goserti b
GSK461364
HMN-214
MLN0905
Pan-Chk inhibitors
AZD7762
PF 477736
Selective Chk inhibitors
LY2603618(Chk1)
CHIR-124(Chk1)
SCH 900776(Chk1)
Pan-Aurora inhibitors
VX-680
Danuserti b
ZM-447439
Selective Aurora inhibitors
MLN8237(Aurora A)
Baraserti b(Aurora B)
Wee1 inhibitor
MK-1775
P P
P P
Growth Factor
Receptor Activation
TGF-
DNA
Damage
Akt
FoxO1/3
p27 Kip1
ATM/
ATR
p53
p21 Cip1
Chk1/2
Cyclin-A
Cyclin-A
Cyclin-H
E2F
Rb
Rb
CDC25A
Raf1
p21
Myc
Myc
cdc25A
Smad3
Smad4
Growth Factor
Withdrawal
GSK-3
CDK4/6
Wee1
Rb FoxO1 Bim
FasL
TRAIL
Apoptosis
E2F/DP Target Genes:
Cyclin E/A, E2F-1/2/3,
cdc2, c-Myc, p107,
RanGAP, TK, DHFR,
PCNA, H2A, etc.
S
- P
H
A
S
E
M- P HAS E G2- P HAS E
DBE
Abl E2F Rb Suv39H1
E2F
OFF ON
TopoII
14-3-3 GADD45 p21
Cip1 CDK7 PLK1
Wee1
Nuclear Exclusion
MDM2
p53
p53
Chk1
BRCA1
cdc25
Chk2
MDM4
Nuclear Export,
Ubiquitination
HIPK2
DNA-PK DNA
Repair
ATM/ATR
c-Abl
Rad52
Rad51
FANCD2
AurA
Bora
Cyclin B
cdc2
Cyclin D
DP-1 DP-1
Critically Short
Telomeres
UV IR
G1- PHASE
TRF2 POT1
Cyclin E
p27 Kip1
CDK2
CDK7
CDK2
HDAC
CDK2
65
CDK
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Roscovitine(Seliciclib, CYC202) is apotentand
selective CDK inhibitor for Cdc2, CDK2 and
CDK5 with IC50 of 0.65 M, 0.7 M and 0.16
M. It shows little effect on CDK4/6. Phase 2.
S1153 Roscovitine (Seliciclib,CYC202)
Product Citations:
J Neurosci, 2012, 32(32): 11050-66
Sci U S A, 2011, 108(20):
8414-9 ]
Roscovitine purchased from
Selleck
SNS-032 has firstly been described as a
selective inhibitor of CDK2 with IC50 of 48 nM
and is 10- and 20-fold selective over
CDK1/CDK4. It is also found to be sensitive to
CDK9 with IC50 of 4 nM and greater than
15-fold more selective for CDK2 than CDK5
and 7, with little effect on CDK6. Phase 1.
S1145 SNS-032 (BMS-387032)
Product Citation:
Mol Cancer Ther, 2011, 10(9): 1624-34
Data independently
produced byYolanda
Sanchez fromGeisel School
of Medicine at Dartmouth
SNS-032 purchased from
Selleck
10 mM/1 mLin DMSO
5mg 50mg 200mg
Size
Flavopiridol competes with ATP to inhibit
CDKs including CDK1, CDK2, CDK4 and
CDK6 with IC50 of ~40 nM. It is 7.5-fold more
selective for CDK1, 2, 4, 6 versus CDK7.
Flavopiridol is initially found to inhibit EGFR
and PKA. Phase 1/2.
S1230 Flavopiridol (Alvocidib)
Product Citations:
Mol Cancer Ther, 2012, 11(11): 2321-30
2012, 11(11): 2321-30 ]
Flavopiridol purchased from
Selleck
10mg 50mg 200mg
Size
AT7519 is a multi-CDK inhibitor for CDK1, 2,
4, 6 and 9 with IC50 of 10-210 nM. It is less
potent to CDK3 and little active to CDK7.
Phase 1.
S1524 AT7519
Product Citation:
J Biol Chem, 2012, 287(52): 43639-50
2011, 6(9): e25683 ]
Selleck
LY2835219 is a potent and selective inhibitor
of CDK4 and CDK6 with IC50 of 2 nM and 10
nM, respectively.
S7158 LY2835219
5 mg 200 mg
Size
10 mg 200 mg
Size
NU6027 is a potent ATR/CDK inhibitor,
inhibits CDK1/2, ATR and DNA-PK with Ki of
2.5 M/1.3 M, 0.4 M and 2.2 M, enter
cells more readily than the 6-aminopurine-
based inhibitors.
S7114 NU6027 new
5 mg 50 mg
Size
p276-00 is a novel CDK1, CDK4 and CDK9
inhibitor with IC50 of 79nM, 63nM and20nM,
respectively.
S8058 P276-00 new
new
JNJ-7706621 is pan-CDK inhibitor with the
highest potency on CDK1/2 with IC50 of 9 nM
/4 nM and showing >6-fold selectivity for
CDK1/2 than CDK3/4/6. It also potently
inhibits Aurora A/B and has no activity on Plk1
and Wee1.
S1249 JNJ-7706621
Data independently
fromSelleck
N
N
N
N
N
H
HO
HN
N
O
S
N
S
H
N
O
NH
O
O OH
HO
N
H
HO
Cl
Cl Cl
NH O
HN N
O
N
H
NH
N
N
H
N
N
F
N
N
N
N
F
S
O
O
OH
O
N
N H2N
N
NH2
O
Cl
O OH
OH O
N
OH
HCl
10 mM/1 mL in DMSO
100 mg 5 mg 25 mg
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
100 mg 2 mg 10 mg
Size
66
Phone:+1-832-582-8158
www.selleckchem.com
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CDK
Flavopiridol (Alvocidib) HCl competes with
ATP to inhibit CDKs including CDK1, CDK2,
CDK4 and CDK6 with IC50 of ~40 nM. It is
7.5-fold more selective for CDK1/2/4/6 than
CDK7. Flavopiridol is initially found to inhibit
EGFR and PKA. Phase 1/2.
S2679 Flavopiridol HCl
Product Citations:
Mol Cancer Ther, 2011, 10(9): 1624-34
Sci U S A, 2011, 108(20):
8414-9 ]
Flavopiridol HCl purchased
fromSelleck
BS-181 is a highly selective CDK7 inhibitor
with IC50 of 21 nM. It is more than 40-fold
selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
S1572 BS-181 HCl
Data independently
produced by Dr. Vladimir
Krystof of Palacky University
BS-181 HCl purchased from
Selleck
Product Citation:
Anticancer Agents Med Chem, 2011, 11(5): 418-26
AZD5438 is a potent inhibitor of CDK1/2/9
with IC50 of 16 nM/6 nM/20 nM. It is less
potent to CDK5/6 and also inhibits GSK3.
Phase 1.
S2621 AZD5438
PHA-793887is a novel andpotent inhibitor of
CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5
nM and 10 nM. It is greater than 6-fold more
selective for CDK2, 5, and 7 than CDK1, 4,
and 9. Phase 1.
S1487 PHA-793887
S2670 A-674563
A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA
and >30-fold selective for Akt1 over PKC.
Dinaciclib(SCH727965) is a novel andpotent
CDK inhibitor for CDK2, CDK5, CDK1 and
CDK9 with IC50 of 1nM, 1nM, 3nM and4nM,
respectively. It also blocks thymidine (dThd)
DNA incorporation. Phase 3.
S2768 Dinaciclib (SCH727965)
Dinaciclib purchased from
Selleck
SCH 900776 is a selective Chk1 inhibitor with
IC50 of 3 nM. It shows 50-fold selectivity
against Chk2. Phase 2.
S2735 MK-8776 (SCH 900776)
PHA-848125 is a potent, ATP-competitive
CDK inhibitor for CDK2 with IC50 of 45 nM. It
is >3-fold more selective for CDK2 than
CDK1, 2, 4, 5, and 7. Phase 2.
S2751 PHA-848125
BMS265246 is a potent and selective CDK1/2
inhibitor with IC50 of 6 nM/9 nM. It is 25-fold
more selective for CDK1/2 than CDK4.
S2014 BMS-265246
R547 is a potent ATP-competitive inhibitor of
CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less
potent to CDK7 and GSK3/, while inactive
to other kinases.
S2688 R547
PHA-767491 is a potent ATP-competitive
dual Cdc7/CDK9 inhibitor with IC50 of 10 nM
and 34 nM, respectively. It displays ~20-fold
selectivity against CDK1/2 and GSK3-,
50-fold selectivity against MK2 and CDK5,
100-fold selectivity against PLK1 and CHK2.
S2742 PHA-767491
O
O OH
HO
N
H
HO
Cl
HCl
H
N
N
N
S
O
O
N
N
H
N
N
N
N
O
HN
O
N
OH
N
N
N
HN
N+
O-
N
N
HN
NH2
Br
N
N
N
N
N
NH2
O
F
F
O HN
N
S O
O
N
N
H
NH
O
N
N N
NH
O
N
HN
N
N
O F
F N
N
N
H
O
10 mM/1 mL in DMSO
10 mg 50 mg
Size
Size
Size
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Page 10
67
CDK
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10 mg 50 mg
Size
BAY 1000394 is an orally bioavailable
pan-CDK inhibitor for CDK1/2/3/4/7/9 with
IC50 of 5-25nM. It also potentlyinhibits Aurora
A, Clk2, ARK5, FGFR1, Flt3, and JAK2/3.
Phase 1/2.
S7047 BAY 1000394
10 mg 50 mg
Size
PD 0332991 is a highly selective inhibitor of
CDK4 and 6 with IC50 of 11 nM and 16 nM,
respectively. It shows no activity to CDK1, 2,
or 5, and none towards EGFR, FGFR,
PDGFR, or InsR. Phase 2/3.
S1579 Palbociclib (PD0332991)
Isethionate
PD 0332991
HCl
S1116
11nM [IC50] 16nM [IC50]
SNS-032 S1145 ++
38nM [IC50]
++ ++
+
62nM [IC50]
Cat.No. Inhibitor Name Cdk1 Cdk2 Cdk3 Cdk4 Cdk5 Cdk6 Cdk7 Cdk9 Other
+++
4nM [IC50]
S1153 Roscovitine
S1249 J NJ -7706621
S1487 PHA-793887
S1524 AT7519
S1572 BS-181HCl
S2014 BMS-265246
S2621 AZD5438
S2670 A-674563
S2688 R547
S2742 PHA-767491
S2751 PHA-848125
S2768 Dinaciclib
+
+++
0.7 M[IC50]
9nM [IC50]
+
210nM [IC50]
+++
6nM [IC50]
+++
16nM [IC50]
++++
1nM [IC50]
++++
1nM [IC50]
++++
1nM [IC50]
++++
4nM [IC50]
++++
1nM [IC50]
+++
3nM [IC50]
++
45nM [IC50]
+++
3nM [IC50]
+
0.16 M[IC50]
+
0.265 M[IC50]
+
0.15 M[IC50]
+++
6nM [IC50]
++
46nM [Ki]
++
20nM [IC50]
++
34nM [IC50]
+++
9nM [IC50]
+
0.23 M[IC50]
++
47nM [IC50]
+
360nM [IC50]
+
100nM [IC50]
+
13nM [IC50]
+
170nM [IC50]
+++
3nM [IC50]
+++
8nM [IC50]
+++
5nM [IC50]
+++
10nM [IC50]
++
21nM [IC50]
AuroraB,
AuroraA
PKA,
AKT1
+
0.16 M[IC50]
N N
HN
S
NH
O
O
F F
F
OH
N N O
N
HN
O
N
N
N
H
HO
S
OH
O
O
68
Phone:+1-832-582-8158
www.selleckchem.com
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Aurora Kinase
MLN8237 (Alisertib) is a selective Aurora A
inhibitor with IC50 of 1.2 nM. It has >200-fold
higher selectivity for Aurora A than Aurora B.
Phase 3.
S1133 Alisertib (MLN8237)
Product Citations:
Cell Stem Cell, 2012, 11(2): 179-94
J Cell Biol, 2010, 191(7): 1315-32
EMBO J, 2011, 30(5): 906-19
Data from[ J Cell Biol,
2010, 191(7): 1315-32 ]
Alisertib purchased from
Selleck
Aurora Kinase Inhibitors
Aurora A selective
VX-680 (MK-0457, Tozasertib) is a
pan-Aurora inhibitor, mostly against Aurora A
with Ki
app
of 0.6 nM, less potent towards
Aurora B/Aurora C and 100-fold more
selective for Aurora A than 55 other kinases.
Phase 2.
S1048 VX-680 (Tozasertib, MK-0457)
Product Citations:
Cell Stem Cell, 2012, 11(2): 179-94
Curr Biol, 2011, 21(16): 1356-65
Data from[ J Neurosci,
2012, 32(32): 11050-66 ]
Selleck
AZD1152-HQPA (Barasertib) is a highly
selective Aurora B inhibitor with IC50 of 0.37
nM, ~100 fold more selective for Aurora B
over Aurora A.
S1147 Barasertib (AZD1152-HQPA)
Data from[ J Pharmacol
Exp Ther, 2012, 343(3):
617-27 ]
Barasertib purchased from
Selleck
Product Citations:
Curr Biol, 2011, 21(16): 1356-65
Clin Cancer Res, 2010, 16(18): 4572-82
Aurora B selective
A
Z
D
1
1
5
2
A
B
T
-3
4
8
1 day
Tx1 Tx2
6 day 1 day 6 day
V
e
h
ic
le
pre-treatment
ZM447439is a selective andATP-competitive
inhibitor for Aurora Aand Aurora B with IC50 of
110 nM and 130 nM, respectively. It is more
than 8-fold selective for Aurora A/B than
MEK1, Src, Lck and has little effect against
CDK1/2/4, Plk1, Chk1, etc.
S1103 ZM-447439
Data from[ Mol Biol Cell,
2011, 22(22): 4227-35 ]
ZM-447439 purchased from
Selleck
Product Citations:
Mol Biol Cell, 2011, 22(22): 4227-35
Mol Cancer Ther, 2011, 10(5): 784-94
MLN8054is a potent andselective inhibitor of
Aurora A with IC50 of 4 nM. It is more than
40-fold selective for Aurora A than Aurora B.
Phase 1.
S1100 MLN8054
Data from[ Antiviral Res,
2013, 99(2): 139-48 ]
MLN8054 purchased from
Selleck
Product Citations:
Dev Cell, 2012, 22(1): 52-63
J Cell Biol, 2012, 198(4): 591-605
Phase 2.
Hesperadin potently inhibits Aurora B with
IC50 of 250 nM. It markedly reduces the
activity of AMPK, Lck, MKK1, MAPKAP-K1,
CHK1 and PHK while it does not inhibit MKK1
activity in vivo.
S1529 Hesperadin
Data from[ J Cell Biol,
2012, 199(2): 251-68 ]
Hesperadin purchased from
Selleck
Product Citations:
J Cell Biol, 2012, 199(2): 251-68
Curr Biol, 2011, 21(16): 1356-65
Aurora B selective
O
F
N
N
N Cl
HN
O
OH
O
N
N
H
N S
N
N
N
H
N
NH
O
O N
O
N
N
O
NH
HN
O
N Cl
F
F
N
N
HN
O
OH
N
H
O
H
N
S
O
O
NH
N
N
N
HN
H
N
N
NH
O
O
N
HO
F
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
250 mg 25 mg 100 mg
Size
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
Aurora A selective
Page 33
69
Aurora Kinase
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S1134 AT9283
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also
potent to Aurora A/B, Abl(T315I). Phase 1/2.
S1249 JNJ-7706621
JNJ-7706621 is pan-CDK inhibitor with the highest potency on
CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for
CDK1/2 than CDK3/4/6. It also potently inhibits Aurora A/B and has
no activity on Plk1 and Wee1.
S2158 KW 2449
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of
6.6 nM, modestly potent to Flt3, Bcr-Abl andAurora A; little effect on
PDGFR, IGF-1R, EGFR. Phase 1.
Aurora A Inhibitor I is a novel, potent, and
selective inhibitor of Aurora A with IC50 of 3.4
nM. It is 1000-foldmore selective forAurora A
thanAurora B.
S1451 Aurora A Inhibitor I
2012, 33(2): 285-93 ]
Aurora A Inhibitor I
Product Citations:
J Neurosci, 2012, 32(32): 11050-66
Carcinogenesis, 2012, 33(2): 285-93
Aurora A selective
Aurora A selective
S1181 ENMD-2076
ENMD-2076 has selective activity against Aurora A and VEGFR(Flt3)
with IC50 of 14nM and1.86nM, 25-foldselective to Aurora B andless
potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and
PDGFR. Phase 2.
DMSO
PT288
DAPI
Merge
S1451 1M S1451 2.5M
ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076,
selective activity against Aurora Aand VEGFR(Flt3) with IC50 of 14nM
and 1.86 nM, 25-fold more selective for Aurora A thanAurora B and
less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and
PDGFR. Phase 2.
SNS-314 Mesylate is a potent and selective
inhibitor of Aurora A, Aurora B and Aurora C
with IC50 of 9 nM, 31 nM, and 3 nM,
respectively. It is less potent to Trk A/B, Flt4,
Fms, Axl, c-Raf and DDR2. Phase 1.
S1154 SNS-314 Mesylate
Data independently
SNS-314 Mesylate
10 mM/1 mL in DMSO
5 mg 50 mg 200 mg
Size
Product Citation:
Exp Cell Res, 2012, 318(4): 336-49
S1171 CYC116
CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM,
less potent to VEGFR2 with Ki of 44 nM, with 50-fold more potent than
CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3/,
CK2, Plk1 and SAPK2A. Phase 1.
AMG 900 is a potent and highly selective
pan-Aurora kinases inhibitor for Aurora A/B/C
with IC50 of 5 nM/4 nM/1 nM. It is >10-fold
selective for Aurora kinases than p38, Tyk2,
J NK2, Met andTie2. Phase 1.
S2719 AMG 900
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
PHA-680632 is potent inhibitor of Aurora A,
Aurora B and Aurora C with IC50 of 27nM, 135
nM and 120 nM, respectively. It has 10- to
200-fold higher IC50 for FGFR1, FLT3, LCK,
PLK1, STLK2, and VEGFR2/3.
S1454 PHA-680632
Data independently
PHA-680632 purchased
fromSelleck
TAK-901 is a novel inhibitor of Aurora A/B with
IC50 of 21 nM/15 nM. It is not a potent inhibitor
of cellular J AK2, c-Src or Abl. Phase 1.
S2718 TAK-901
Product Citations:
Cancer Res, 2013, 73(10): 3168-80
Stem Cells, 2012, 30(9): 1819-30
S2725 PF-03814735
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B
with IC50 of 0.8 nM/5 nM, less potent to Flt3, FAK, TrkA, little active to
Met and FGFR1. Phase 1.
CCT129202 is an ATP-competitive pan-
Aurora inhibitor for Aurora A, Aurora B and
Aurora C with IC50 of 0.042 M, 0.198 M and
0.227 M, respectively. It is less potent to
FGFR3, GSK3, PDGFR, etc.
S1519 CCT129202
CCT129202 purchased from
Selleck
5 mg 50 mg 200 mg
Size
Product Citation:
Mol Pharm, 2012, ahead of print
N
N
N
O
H
N
N
N
S
H2N
N
H
N
O
S
O
O
N
H
N
N N
N
H F
N
H
O
Cl
NH
N
O
N
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Size
Size
Page 40
Page 65
Page 32
Page 19
Page 19
Page 42
Page 21
70
Phone:+1-832-582-8158
www.selleckchem.com
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Aurora Kinase
MK-5108 (VX-689) is a highly selective
Aurora A inhibitor with IC50 of 0.064nM andis
220- and190-foldmore selective for Aurora A
than Aurora B/C, while it inhibits TrkA with
less than 100-fold selectivity. Phase 1.
S2770 MK-5108 (VX-689)
Data independently
produced by Ken Ma Hong
Kong University of Science &
Technology
MK-5108 purchased from
Selleck
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
GSK1070916 is a reversible and
ATP-competitive inhibitor of Aurora B/C with
IC50 of 3.5 nM/6.5 nM. It displays >100-fold
selectivity against the closely related Aurora
A-TPX2 complex. Phase 1.
S2740 GSK1070916
Data independently
produced byAntonino Maria
Spart fromUniversity of
Bologna
GSK1070916 purchased
fromSelleck
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
CCT137690 is a highly selective inhibitor of
Aurora A, Aurora B and Aurora C with IC50 of
15nM, 25nM and19nM. It has little effect on
hERG ion-channel.
S2744 CCT137690
Data independently
produced by Dr. Antonino
Maria Sparta, PhDUniversity
of Bologna
CCT137690 purchased from
Selleck
10mg 50mg
Size
VX-680
MLN8054
ZM-447439
Danusertib
MLN8237
AT9283
Barasertib
CYC116
ENMD-2076
J NJ -7706621
Aurora A Inhibitor I
PHA-680632
CCT129202
Hesperadin
KW 2449
TAK-901
AMG 900
PF-03814735
GSK1070916
CCT137690
MK-5108
S1048
S1100
S1103
S1107
S1133
S1134
S1147
S1171
S1181
S1249
S1451
S1454
S1519
S1529
S2158
S2718
S2719
S2725
S2740
S2744
S2770
++++
+++
+
++
+++
+++
+++
+++
++
+++
++
++
++
++
+++
++++
++
++++
0.6 nM [Ki
app
]
4 nM [IC50]
110 nM [IC50]
13 nM [IC50]
1.2 nM [IC50]
3 nM [IC50]
8.0 nM [Ki]
14 nM [IC50]
11 nM [IC50]
3.4 nM [IC50]
27 nM [IC50]
0.042 M [IC50]
48 nM [IC50]
21 nM [IC50]
5 nM [IC50]
0.8 nM [IC50]
15 nM [IC50]
0.064 nM [IC50]
++
+
+
+++
++++
+++
+
++
+
+
+
+
++
+++
+++
+++
++
+++
+
++
+
+
++++
+++
++
18 nM [Ki
app
]
130 nM [IC50]
79 nM [IC50]
3 nM [IC50]
0.37 nM [IC50]
9.2 nM [Ki]
350 nM [IC50]
15 nM [IC50]
3.4 M [IC50]
135 nM [IC50]
0.198 M [IC50]
250 nM [IC50]
15 nM [IC50]
4 nM [IC50]
5 nM [IC50]
3.5 nM [IC50]
25 nM [IC50]
Cat.No. Inhibitor Name Aurora A Aurora B Aurora C Other
4.6 nM [Ki
app
]
61 nM [IC50]
0.432 M [IC50]
120 nM [IC50]
0.227 M [IC50]
1 nM [IC50]
6.5 nM [IC50]
19 nM [IC50]
Bcr-Abl,c-RET
Abl,J AK3,J AK2
VEGFR2
FLT3,FLT4,VEGFR2
Cdk2,Cdk1
p38-
FAK,FLT1
Abl,FLT3,c-Kit,
J AK2,FGFR-1
N
H
O N
H
O
OH
N N
H
N Br
N
N
N N
O
N
N N
H
N
N N
N
H
N
O
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Aurora A selective
71
Chk / ROCK
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AZD7762is a potent andselective inhibitor of
Chk1 with IC50 of 5 nM. It is equally potent
against Chk2 and less potent against CAM,
Yes, Fyn, Lyn, Hck and Lck. Phase 1.
S1532 AZD7762
2012, 2(6): 524-39 ]
Selleck
Data from[ Dev Biol, 2012,
370(1): 33-41 ]
Y-27632 2HCl purchased
fromSelleck
Product Citations:
Nat Biotechnol, 2011, 29(6): 542-6
Cancer Discov, 2012, 2(6): 524-39
LY2603618 (IC-83) is a selective Chk1
inhibitor with potential anti-tumor activity.
S2626 LY2603618
AZD7762
LY2603618
CHIR-124
MK-8776
PF 477736
S1532
S2626
S2683
S2735
S2904
+++
+++
++++
+++
++++
5 nM [IC50]
7 nM [IC50]
0.3 nM [IC50]
3 nM [IC50]
0.49 nM [Ki]
+++
++
<10 nM [IC50]
47 nM [Ki]
Cat.No. Inhibitor Name CHK1 CHK2 Other
VEGFR2
Chk Inhibitors
Y-27632 2HCl is a selective ROCK1
(p160ROCK) inhibitor with Ki of 140 nM,
exhibits >200-fold selectivity over other
kinases, including PKC, cAMP-dependent
protein kinase, MLCK and PAK.
S1049 Y-27632 2HCl
Product Citation:
Dev Biol, 2012, 370(1): 33-41
ROCK Inhibitors
Chk1 selective
ROCK1 selective
S2735 MK-8776 (SCH 900776)
SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows
50-fold selectivity against Chk2. Phase 2.
PF 477736 is a selective, potent and ATP-
competitive Chk1 inhibitor with Ki of 0.49 nM
and also inhibits VEGFR2, Aurora-A, FGFR3,
Flt3, Fms (CSF1R), Ret and Yes. It shows
~100-fold selectivity for Chk1 than Chk2.
Phase 1.
S2904 PF 477736
CHIR-124is a novel andpotentChk1inhibitor
with IC50 of 0.3 nM. It shows 2,000-fold
selectivity against Chk2, 500- to 5,000-fold
less activity against CDK2/4 and Cdc2.
S2683 CHIR-124 Chk1 selective
Chk1 selective
LY2606368 is a second generation Chk
inhibitor for Chk1 and Chk2 with IC50 of <1nM
and 4.7 nM, respectively.
S7178 LY2606368 new
Basal
Apical
1:36 0:00
F
S
NH
NH2
O
HN
O
N
H
Br
O
NH
O
H
N
H
N
O
N
N
H
N
N
NH
O
Cl
NH
N
O
HN N H2N
2HCl
N
H
N
H
O
NH2
N
N
N
H
N
O
O
O
NH2
HN
N N
H
N
N
CN
Thiazovivin (Tzv) is a novel ROCK inhibitor
with IC50 of 0.5 M, promotes hESC survival
after single-cell dissociation.
S1459 Thiazovivin
Fasudil is a potent inhibitor of ROCK-II, PKA,
PKG, PKC, and MLCK with Ki of 0.33 M, 1.6
M, 1.6 M, 3.3 M and 36 M, respectively.
S1573 Fasudil (HA-1077) HCl
Product Citation:
Cell Reprogram, 2012, 14(6): 485-96
ROCK2 selective
N
H
O
N
S
HN
N
N
NH
N N
N
S
N
O
N
N
S
O
O
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO
50 mg 2 mg 10 mg
Size
10 mM/1 mL in DMSO
100 mg 2 mg 25 mg
Size
Page 66
72
Phone:+1-832-582-8158
www.selleckchem.com
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ROCK / PLK
GSK429286A is a selective inhibitor of
ROCK1 and ROCK2 with IC50 of 14 nM and
63 nM, respectively.
S1474 GSK429286A
10 mg 50 mg
Size
RKI-1447 is a potent inhibitor of ROCK1 and
ROCK2 with IC50 of 14 nM and 6 nM,
respectively.
S7195 RKI-1447
Y-27632 2HCl
GSK429286A
Fasudil HCl
RKI-1447
S1049
S1474
S1573
S7195
+
+++
+++
140 nM [Ki]
14 nM [IC50]
14 nM [IC50]
++
+
+++
63 nM [IC50]
0.33 M [Ki]
6 nM [IC50]
Cat.No. Inhibitor Name ROCK1 ROCK2
ON-01910 is a non-ATP-competitive inhibitor
of PLK1 with IC50 of 9 nM. It shows 30-fold
greater selectivityagainst Plk2andno activity
to Plk3. Phase 3.
S1362 Rigosertib (ON-01910)
Data independently
produced by Dr. Antonino
Maria Sparta, PhDUniversity
of Bologna
Rigosertib purchased from
Selleck
Product Citation:
Stem Cells, 2013, 31(6): 1051-63
BI 2536 is a potent Plk1 inhibitor with IC50 of
0.83 nM. It shows 4- and 11-fold greater
selectivity against Plk2 and Plk3. Phase 2.
S1109 BI 2536
2010, 18(6): 641-54 ]
BI 2536 purchased from
Selleck
Product Citations:
Cell, 2011, 147(4): 853-67
Cancer Cell, 2010, 18(6): 641-54
Nat Cell Biol, 2011, 13(10): 1265-71
PLK Inhibitors
BI6727 (Volasertib) is a highly potent Plk1
inhibitor with IC50 of 0.87 nM. It shows 6- and
65-fold greater selectivity against Plk2 and
Plk3. Phase 2.
S2235 BI6727 (Volasertib)
Data independently
produced by Dr. Xiangbing
Meng from University of Iowa
BI6727 purchased from
Selleck
H
N O
H
N
O
F F
F
F N
H
N
O
N
H
HO
O
O
O
O
O OH
O O
O
O
O
OH
O
O O
S
O O
O
NH
ONa
O
N
N
S
N
H
N
H
O
OH
N
N N
N O
H
N
O
H
N
O
N
N
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
100 mg 5 mg 50 mg
Size
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
10 mg 50 mg
Size
73
PLK / APC / Wee1 / c-Myc
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GSK461364 inhibits purified Plk1 with Ki of 2
nM. It is more than 1000-fold selective
against Plk2/3. Phase 1.
S2193 GSK461364
2012, 287(21): 17088-99 ]
Selleck
Product Citation:
Br J Pharmacol, 2012, 166(3): 858-76
MLN0905 is a potent inhibitor of PLK1 with
IC50 of 2 nM.
S2898 MLN0905
2mg 5mg 25mg
Size
HMN-214 is a prodrug of HMN-176, which
alters the cellular spatial orientation of Plk1.
S1485 HMN-214
MK-1775 is a potent and selective Wee1
inhibitor with IC50 of 5.2 nM; hinders G2 DNA
damage checkpoint. Phase 2.
S1525 MK-1775
Data from[ Mol Cell Biol,
2012, 32(20): 4226-36 ]
MK-1775 purchased from
Selleck
Product Citations:
Mol Cell Biol, 2012, 32(20): 4226-36
Mol Cancer Ther, 2011, 11(1): 174-82
Tosyl-L-Arginine Methyl Ester (TAME) is an
APC inhibitor.
S2225 TAME
APC Inhibitor
25 mg
Size
10058-F4is a c-Myc inhibitor that specificallly
inhibits the c-Myc-Max interaction and
prevents transactivation of c-Myc target gene
expression.
S7153 10058-F4
c-Myc Inhibitor
Wee1 Inhibitor
N
N
N
N
S
O
NH2
O
F
F F
N+ N
S
O O O
O
O-
N
OH
N N
N
N
O
N
H
N
N
N
H
N
N
NH
F3C
S
N
N
S
N
H
O O
O
O
NH
HN NH2
NH
S
O
S
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
Size
Size
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
74
Phone:+1-832-582-8158
www.selleckchem.com
T
G
F
-
b
e
t
a
/
S
m
a
d
Bcr-Abl / PKC / ROCK / TGF-beta/Smad
TGF-beta/Smad Pathway
Bcr-Abl Inhibitors
PKC Inhibitors
ROCK Inhibitors
Transcription
Actin Polymerization
Stress Fibers
Cell Adhesion
Tumor
Suppression Cell Growth
S
B
E
TGF
ROCK
LIMK
PI3K/Akt
Pathway
MAPK
Pathway
CDC42
PAK
c-Abl
PKC
Smad3
Smad3
Smad4
Smad4
Smad2
Smad3/4 Smad2/4
Ras
MEKs
ERK1/2
Smad7
Smad6
Apoptosis
Angiogenesis P300
CBP
LDN193189(ALK2 & ALK3)
LY2109761(TRI & TRII)
SB-505124(ALK4 & ALK5)
Selective TGF-beta/Smad inhibitors
SB 431542(TRI/ALK5)
LY2157299(TRI/ALK5)
SB 525334(TRI/ALK5)
Pan-TGF-beta/Smad inhibitors
SB-505124(ALK4 & ALK5)
SB 431542(TRI/ALK5)
LY2157299(TRI/ALK5)
SB 525334(TRI/ALK5)
PD0325901
GSK1120212
U0126-EtOH
AZD6244(MEK1)
BIX 02189(MEK5)
Pan-MEK inhibitors
Thi azovi vi n
GSK429286A
Selective ROCK inhibitors
Y-27632(ROCK1)
Fasudi l (ROCK2)
Pan-ROCK inhibitors
Ponati ni b
Imati ni b Mesyl ate
WP1130
Ni l oti ni b
Bafeti ni b
Dasati ni b
Bcr-Abl inhibitors
Staurospori ne
Sotrastauri n
Enzastauri n
Pan-PKC inhibitors
LDN193189 is a selective BMP signaling
inhibitor, inhibits the transcriptional activity of
the BMP type I receptors ALK2 and ALK3 with
IC50 of 5 nM and 30 nM, respectively, exhibits
200-fold selectivity for BMP versus TGF-.
S2618 LDN193189
Data from[ J Cell Sci, 2013,
126(Pt 1): 234-43 ]
LDN193189 purchased from
Selleck
Product Citation:
J Cell Sci, 2013, 126(Pt 1): 234-43
SB 431542 is a potent and selective inhibitor
of ALK5 with IC50 of 94 nM, 100-fold more
selective for ALK5 than p38 MAPK and other
kinases.
S1067 SB 431542
2013, 288(11): 7841-56 ]
Selleck
Product Citations:
J Biol Chem, 2013, 288(11): 7841-56
Mol Cancer, 2011, 10: 66
TGF-beta/Smad Inhibitors
ALK5 selective
N
N
H
N
O
NH2
O
O
N
HN
N
N N
N
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
25 mg 2 mg 5 mg
Size
75
TGF-beta/Smad
T
G
F
-
b
e
t
a
/
S
m
a
d
LY2157299 is a potent TGF receptor I (T
RI) inhibitor with IC50 of 56 nM. Phase 2.
S2230 LY2157299
Product Citation:
Lab Chip, 2013, 13(10): 1969-78
ALK5 selective
LY2109761 is a novel selective TGF-
receptor type I/II (TRI/II) dual inhibitor with Ki
of 38 nM and 300 nM, respectively; shown to
negatively affect the phosphorylation of
Smad2.
S2704 LY2109761
ALK5 selective
SB 525334 is a potent and selective inhibitor
of TGF receptor I (ALK5) with IC50 of 14.3
nM, is 4-fold less potent to ALK4 than ALK5
and inactive to ALK2, 3, and 6.
S1476 SB 525334
2013, 8(2): e56585 ]
Selleck
Product Citation:
PLoS One, 2013, 8(2): e56585
SB 431542
SB 525334
SB-505124
LY2157299
LDN193189
LY2109761
GW788388
S1067
S1476
S2186
S2230
S2618
S2704
S2750
+++ 5 nM [IC50] +++ 30 nM [IC50]
+ 129 nM [IC50]
+ 129 nM [IC50]
Cat.No. Inhibitor Name ALK2 ALK3 ALK4 ALK5 TRII
+
++
+
++
++
94 nM [IC50]
14.3 nM [IC50]
56 nM [IC50]
38 nM [Ki]
18 nM [IC50]
N
N N
N
O
NH2
N
N
N
HN N
N O
N
O
N N
N
LY364947 is a potent ATP-competitive
inhibitor of TGFR-I with IC50 of 59 nM, shows
7-fold selectivity over TGFR-II.
S2805 LY364947
10mg 25mg 50mg
Size
GW788388 is a potent and selective inhibitor
of ALK5 with IC50 of 18 nM, also inhibits other
TGF- type I and type II receptor kinase
activities, but does not inhibit BMP type II
receptor.
S2750 GW788388
Pirfenidone is an inhibitor for TGF-
production and TGF- stimulated collagen
production, also reduces production of TNF-
and IL-1, has anti-fibrotic and anti-
inflammatory properties. Phase 3.
S2907 Pirfenidone
SB505124 is a selective inhibitor of TGF
R-IALK4, ALK5 with IC50 of 129 nM and 47
nM, respectively, also inhibits ALK7, but does
not inhibitALK1, 2, 3, or 6.
S2186 SB-505124
N
N
H
N
O
O
O
N
H
O
N
H
N
N
N
N
O
N
H
N
N
N
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO
100 mg 5 mg 50 mg
Size
76
Phone:+1-832-582-8158
www.selleckchem.com
D
N
A

D
a
m
a
g
e
HDAC / ATM/ATR / DNA-PK / PARP
DNA Damage
HDAC Inhibitors
ATM/ATR Inhibitors
DNA-PK Inhibitors
ABT-888 (Veliparib, NSC 737664) is a potent
inhibitor of PARP1 and PARP2 with Ki of 5.2
nM and 2.9 nM, respectively. It is inactive to
SIRT2. Phase 1/2.
S1004 Veliparib (ABT-888)
2013, 34(4): 739-49 ]
Veliparib purchased from
Selleck
Product Citations:
Cancer Res, 2011, 71(14): 4944-54
Nucleic Acids Res, 2013, 41(7): 4080-92
Olaparib (AZD2281, KU0059436) is a
selective inhibitor of PARP1/2 with IC50 of 5
nM/1 nM, 300-times less effective against
tankyrase-1. Phase 1/2.
S1060 Olaparib (AZD2281, Ku-0059436)
Data from[ Nat Struct Mol
Biol, 2012, 19(4): 417-23 ]
Olaparib purchased from
Selleck
Product Citations:
Cell, 2011, 145(4): 529-42
Nat Chem Biol, 2012, 8(11): 905-12
PARP Inhibitors
NH
N
O
N
O
F
N O
H2N O
N
H
N
N
H
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
500 mg 10 mg 100 mg
Size
NT
CPT
(nM)
- 251001000 - 251001000 - 251001000 - 251001000 - 251001000
+Olaparib +Olaparib PARP1+/+
PARP1+/+
PARP1-/-
U2OS MEFS
R
e
la
tiv
e
D
S
B
in
d
u
c
tio
n
1
3
5
7
9
100 nM 1 M 25 nM 100 nM 1 M 25 nM CPT
Olaparib - - - - - - - - - + + + +
+/+ +/+ +/+ +/+ +/+ +/+ -/- -/- -/-
+ +
(PARP1)
U2OS MEFS
S
u
r
v
iv
in
g
fr
a
c
tio
n
0.0001
0.001
0.01
0.1
1
0 1 3 10
Cisplatin (M)
Control
5uM Veliparib
10uM Veliparib
50uM Veliparib
ERCC1-low PC9
NU7441
PI-103
PIK-75
NU7026
PP-121
DNA-PK inhibitors
KU-55933
KU-60019
CP-466722
VE-821
BEZ235
Wortmanni n
ATM/ATR inhibitors
Topotecan(Topoi somerase I)
Camptotheci n(Topoi somerase I)
Doxorubi ci n(Topoi somerase II)
IIri notecan(Topoi somerase I)
Etoposi de(Topoi somerase II)
Epi rubi ci n(Topoi somerase II)
Selective Topoisomerase inhibitors
AZD7762
PF 477736
Selective Chk inhibitors
LY2603618(Chk1)
CHIR-124(Chk1)
SCH 900776(Chk1)
Pan-Chk inhibitors
Ol apari b
ABT-888
A-966492
Selective PARP inhibitors
Rucapari b(PARP1)
Ini pari b(PARP1)
UPF 1069(PARP2)
Pan-PARP inhibitors
J AK
ATM
ATR
ATM
CHK1 TLK1/2
H2AX
BRCA1
c-Abl
p53
CHK2
PARP
CDK Wee1
Topoisomerase
CDC25
Aurora
Kinnase
PLK
DNA-PK
Double-strand breaks Alkylating agents Replication stress
Apoptosis
DNA Repair
Cell-cycle
Chromatin
remodelling
MDM2
JNJ 26854165
RITA
p53 inhibitor
Tenovi n-1
Pifithrin-
p53 activators
77
PARP
D
N
A

D
a
m
a
g
e
AG14361 is a potent inhibitor of PARP1 with
Ki of <5 nM. It is at least 1000-fold more
potent than the benzamides.
S2178 AG14361
Rucaparib (AG-014699, PF-01367338) is an
inhibitor of PARP with Ki of 1.4 nM with
binding affinity to nine PARP domains. Phase
1/2.
S1098 Rucaparib (AG-014699, PF-01367338)
2012, 287(47): 39824-33 ]
Rucaparib purchased from
Selleck
Product Citation:
Nature, 2011, 470(7334): 419-23
ABT-888
Iniparib
Rucaparib
AG14361
A-966492
MK-4827
BMN 673
UPF 1069
S1004
S1087
S1098
S2178
S2197
S2741
S7048
S8038
+++
+
+++
+++
++++
+++
++++
5.2 nM [Ki]
40 M [IC50]
1.4 nM [Ki]
<5 nM [Ki]
1 nM [Ki]
3.8 nM [IC50]
0.58 nM [IC50]
+++
+++
+++
++
2.9 nM [Ki]
1.5 nM [Ki]
2.1 nM [IC50]
0.3 M [IC50]
Cat.No. Inhibitor Name PARP1 PARP2
BSI-201 (Iniparib, SAR240550) is a PARP1
inhibitor with demonstrated effectiveness in
triple-negative breast cancer (TNBC). Phase
3.
S1087 Iniparib (BSI-201)
Data from[ Neuroscience,
2010, 171(4): 1256-64 ]
Iniparib purchased from
Selleck
Product Citation:
Neuroscience, 2010, 171(4): 1256-64
10 mM/1 mLin DMSO
5 mg 50 mg 200 mg
Size
PARP1 selective
PARP1 selective
Notes:
1."+" indicates inhibitory effect. The more "+" are,
the stronger inhibition is.
2.Black "+" corresponds to IC50 or Ki values in nMs,
gray "+" refers to values in Ms.
HN
NH
F
H
N
O
P OH
OH
O
HO
H2N O
I
NO2
N
HN
N
O
N
Size
AZD2461 is a novel PARP inhibitor with low
affinity for Pgp than Olaparib. Phase 1.
S7029 AZD2461 new
N
NH
F
O
N
O
O 10 mM/1 mL in DMSO 5 mg 25 mg
Size
UPF 1069 is a selective PARP2 inhibitor with
IC50 of 0.3 M. It is ~27-fold selective against
PARP1.
S8038 UPF 1069
BMN 673 is a novel PARP inhibitor with IC50 of
0.58 nM. It is also a potent inhibitor of
PARP-2, but does not inhibit PARG and is
highly sensitive to PTEN mutation. Phase 1.
S7048 BMN 673
10 mg 50 mg
Size
MK-4827 is a selective inhibitor of PARP1/2
with IC50 of 3.8 nM/2.1 nM, with great activity
in cancer cells with mutant BRCA-1 and
BRCA-2. It is >330-fold selective against
PARP3, V-PARP and Tank1. Phase 3.
S2741 MK-4827 (Niraparib)
PJ-34 is a PARP inhibitor with EC50 of 20 nM
and is equally potent to PARP1/2.
S2886 PJ34
5 mg 10 mg 50 mg
Size
A-966492 is a novel and potent inhibitor of
PARP1 and PARP2 with Ki of 1 nM and 1.5
nM, respectively.
S2197 A-966492
5 mg 50 mg 200 mg
Size
PARP2 selective
INO-1001 is a potent inhibitor of PARP with
IC50 of <50nM inCHO cells anda mediator of
oxidant-induced myocyte dysfunction during
reperfusion. Phase 2.
S1132 INO-1001
Size
NH2
O
NH2
H2N O
N
H
N
F
N
H
N
N
O H2N
NH
N
H
H
N
O
N
HCl
O
NH
O
O
O
N
H
N
H
N
F
O
N
N N
F
Size
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
78
Phone:+1-832-582-8158
www.selleckchem.com
D
N
A

D
a
m
a
g
e
DNA/RNA Synthesis
DNA/RNA Synthesis Inhibitors
Carboplatin is a DNA synthesis inhibitor by
binding to DNA and interfering with the cell's
repair mechanism.
S1215 Carboplatin
Adrucil (Fluorouracil) is an DNA/RNA
synthesis inhibitor, which interrupts
nucleotide synthetic by inhibiting thymidylate
synthase (TS).
S1209 Fluorouracil (5-Fluoracil, 5-FU)
Fludarabine Phosphate is an analogue of
adenosine and deoxyadenosine, which is
able to compete with dATP for incorporation
into DNA and inhibit DNA synthesis.
S1229 Fludarabine Phosphate
Pemetrexed disodium (Alimta) is a novel
antifolate and antimetabolite for TS, DHFR
and GARFT with Ki of 1.3 nM, 7.2 nM and 65
nM, respectively.
S1135 Pemetrexed
50 mg 100 mg 200 mg
Size
Gemcitabine Hydrochloride (Gemzar) is a
DNA synthesis inhibitor with IC50 of 50nM, 40
nM, 18 nM and 12 nM in PANC1, MIAPaCa2,
BxPC3 and Capan2 cells, respectively.
S1149 Gemcitabine HCl
Data from[ Cancer
Immunol Immunother,
2013, 62(2): 383-91 ]
Gemcitabine HCl purchased
fromSelleck
Product Citation:
Cancer Immunol Immunother, 2013, 62(2): 383-91
Product Citation:
PLoS One, 2013, 8(1): e54595
Bleomycin sulfate (Blenoxane) is a
glycopeptide antibiotic and an anticancer
agent for squamous cell carcinomas (SCC)
with IC50 of 4 nM in UT-SCC-19A cells.
S1214 Bleomycin Sulfate
Data from[ Mol Cell Biol,
2013, 33(8): 1632-44 ]
Bleomycin Sulfate
Product Citation:
Mol Cell Biol, 2013, 33(8): 1632-44
Product Citation:
PLoS One, 2013, 8(1): e54595
Capecitabine is a tumor-selective
fluoropyrimidine carbamate which achieves
higher intratumoral 5-FU level with lower
toxicity than 5-FU.
S1156 Capecitabine
Data independently
Capecitabine purchased
fromSelleck
10 mM/1 mL in DMSO
50 mg
Size
Oxaliplatin inhibits DNA synthesis by
conforming DNA adducts.
S1224 Oxaliplatin
Oxaliplatin purchased from
Selleck
S1491 Fludarabine
Fludarabine (Fludara, F-ara-A, NSC 118218) is a STAT1 activation
inhibitor and a DNA synthesis inhibitor.
Cisplatin is an inorganic and water-soluble
platinum complex, which is able to inhibit
DNA synthesis by conforming DNA adducts.
S1166 Cisplatin
2013, 8(1): e54595 ]
Cisplatin purchased from
Selleck
NH3
Pt
Cl
NH3 Cl
N
N
O
O
HO
HO F
F
NH2
HCl
Pt
O
O
O
O
H3N
H3N
N
N
H
O
NH
OH
NH O
NH
OH O
N S
N
S
HN
O
S+ S
O
O
OH -O
O
O
OH
OH
HO
O
H O
OH O
HO
HO
H2N
O
H
N
O
N N
H2N
H
N
NH2
NH2
O
H2N
O
N
H2
Pt
H2
N
O
O O
O
HN
H
N
F
O
O
N N
N
N
H2N
F
O
HO
OPO3H2
OH
N
H
O
ONa
O ONa
O
HN
N
HN
O
H2N
Size
Size
Size
10 mM/1 mL in DMSO
25 mg 100 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg
Size
10 mM/1 mL in DMSO
50 mg
Size
10 mM/1 mL in DMSO
10 mg 50 mg
Size
Page 50
Oxaliplatin effects on MiaPaCa-2 cell survival
after 72h in 1%FBS-containing media
C
e
ll v
ia
b
ility
(%
o
f c
o
n
tro
l)
0
20
40
60
80
100
120
0.1 1 10 100 1000
Drug dose, M
10 mg 50 mg
Size
79
DNA/RNA Synthesis
D
N
A

D
a
m
a
g
e
Clofarabine inhibits the enzymatic activities
of ribonucleotide reductase (IC50=65 nM)
and DNA polymerase.
S1218 Clofarabine
Mizoribine (Bredinin) is an imidazole
nucleoside andanimmunosuppressive agent
with an IC50 of approximately 100 M.
S1384 Mizoribine
10mg 50 mg
Size
Flupirtine maleate is the salt formof Flupirtine,
which is a centrally acting non-opioid analgesia,
is a selective neuronal potassium channel
opener thatalsohas NMDAreceptor antagonist
properties. Phase2.
S1334 Flupirtine maleate
CX-5461 is an inhibitor of rRNA synthesis,
selectively inhibits Pol I-driven transcription
of rRNAwith IC50 of 142nM, has no effect on
Pol II, and possesses 250- to 300-fold
selectivity for inhibition of rRNA transcription
versus DNA replication and protein
translation.
S2684 CX-5461
5 mg 50 mg 200 mg
Size
Nelarabine (Arranon, 506U78) is a purine
nucleoside analog and DNA synthesis
inhibitor with IC50 from 0.067-2.15 M in
tumor cells.
S1213 Nelarabine
This agent inhibited cell proliferation of
NCI-H727 with IC50 of 9.3 nM.
S1217 Cyclophosphamide
Cytarabine (Cytosine arabinoside, AraC) is
an antimetabolic agent and DNA synthesis
inhibitor with IC50 of 16 nM in wild-type
CCRF-CEM cells.
S1648 Cytarabine
50 mg
Size
Cladribine (Leustatin, Litak, 2CDA) is an
adenosine deaminase inhibitor for U266,
RPMI8226, and MM1.S cells with IC50 of
approximately 2.43 M, 0.75 M, and 0.18
M, respectively.
S1199 Cladribine
10 mM/1 mL in DMSO
50 mg
Size
Floxuridine (Fludara) is a prodrug of
floxuridine and an oncology agent with an
GI50 of 5.1 M for the inhibition of
MDCK/PEPT1.
S1299 Floxuridine
Mercaptopurine is a widely used antileukemic
agent and immunosuppressive drug that
inhibits de novo purine synthesis through
incorporation of thiopurine methyltransferase
metabolites into DNA and RNA.
S1305 Mercaptopurine (6-MP)
Ifosfamide is a nitrogen mustard alkylating
agent used in the treatment of cancer.
S1302 Ifosfamide
S2678 NSC 207895
Raltitrexed (Tomudex) is a thymidylate
synthase inhibitor with an IC50 of 9nM for the
inhibition of L1210 cell growth.
S1192 Raltitrexed
Raltitrexed purchased from
Selleck
Gemcitabine(Gemzar) belongs to the group
of medicines called antimetabolites.
S1714 Gemcitabine
Data independently
Gemcitabine purchased
fromSelleck
N N S
O
N
H
O
N
N
N
N
N N
N
N
NH2
O
O
HO OH
OH
O
P
NH
O
N
Cl Cl
N N
N
N
Cl
H2N
O
OH
OH
NH
N
O
N
S
NH
O
O
HO
O OH
N
N N
N
NH2
Cl
O
F
HO
OH
N
H
N NH2
NH
O O
F
O
OH HO
O
O
N
HO
HO
OH
N
OH
NH2
O
N
N
H
S
N
H
N
N
N O NH2
O
OH
HO
HO
O N
HO
HO
H
N
O
F
O
O
P
N
Cl
N
H
Cl
O
N N
H2N
O
O
OH
OH
F
F
Size
Size
Size
Size
Dacarbazine (DTIC-Dome) is an
antineoplastic chemotherapy drug used in
the treatment of various cancers.
S1221 Dacarbazine
N
NH
O H2N
N
N N
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO
50 mg 100 mg 10 mg
Size
Page 45
Raltitrexed
HEK/MRP5
HEK/P
T
o
ta
l D
N
A
/w
e
ll
(%
o
f c
o
n
tro
l)
RTX (log M)
-9 -8 -7 -6 -5
0
50
0
150
80
Phone:+1-832-582-8158
www.selleckchem.com
D
N
A

D
a
m
a
g
e
DNA/RNA Synthesis / Sirtuin / Topoisomerase
Carmofur (INN) is a pyrimidine analogue
used as an antineoplastic agent.
S1289 Carmofur
50 mg
Size
Doxorubicin (Adriamycin) is an antibiotic
agent that inhibits DNA topoisomerase II and
induces DNA damage and apoptosis.
S1208 Doxorubicin (Adriamycin)
Data from[ Mol Cancer
Ther, 2011, 10(10): 1846-56 ]
Doxorubicin purchased from
Selleck
Topoisomerase Inhibitors
Product Citation:
Mol Cancer Ther, 2011, 10(10): 1846-56
Topo II selective Licensed by Pfizer
Etoposide is a semisynthetic derivative of
podophyllotoxin, which inhibits DNA
synthesis via topoisomerase II inhibition
activity.
S1225 Etoposide
Data from[ Mol Cancer
Ther, 2011, 10(10): 1846-56 ]
Etoposide purchased from
Selleck
Product Citation:
Mol Cancer Ther, 2011, 10(10): 1846-56
Topo II selective
Topotecan (Hycamtin, NSC 609699) is a
topoisomerase I inhibitor for MCF-7 Luc cells
and DU-145 Luc cells with IC50 of 13 nM and
2 nM, respectively.
S1231 Topotecan HCl Topo I selective
O O
O
OH
OH
O
O H
OH
NH2
OH
O
OH
.HCl
O
O
O
O H
O
OH
O
H
O O
H
OH
OH
O
O
H
H
N
N
OH
N
O
O
O
HO
HCl
Irinotecan (Camptosar, Campto, CPT-11) is a
topoisomerase I inhibitor for LoVo cells and
HT-29 cells with IC50 of 15.8 M and 5.17 M,
respectively.
S1198 Irinotecan
Irinotecan purchased from
Selleck
N N
O
O N
N O
O
O
HO
N
H
N
F
O O
N
H
O
Sirtinol is a specific SIRT1 and SIRT2
inhibitor with IC50 of 131 M and 38 M,
respectively.
S2804 Sirtinol
SRT1720 is a selective SIRT1 activator with
EC50 of 0.16 M, but is >230-fold less potent
for SIRT2 and SIRT3.
S1129 SRT1720
Data from[ EMBO J, 2013,
32(6): 791-804 ]
SRT1720 purchased from
Selleck
5 mg 50 mg 200 mg
Size
Sirtuin Inhibitors & Chemicals
Product Citation:
EMBO J, 2013, 32(6): 791-804
SIRT1 selective
EX 527 is a potent and selective SIRT1
inhibitor with IC50 of 38nM, exhibits >200-fold
selectivity against SIRT2 and SIRT3.
S1541 EX 527
2013, 288(22): 15537-46 ]
EX 527 purchased from
Selleck
Product Citation:
J Biol Chem, 2013, 288(22): 15537-46
SIRT1 selective
Resveratrol is a phytoalexin produced
naturally by several plants with anti-cancer,
anti-inflammatory, blood-sugar-lowering and
other beneficial cardiovascular effects.
S1396 Resveratrol
Data independently
produced by Bai Bo
University of Hong Kong
Resveratrol purchased from
Selleck
100mg 200mg 500mg
Size
N
N
O
N
H
S
N
N
N
N
H
HCl
H
N
Cl
O
H2N
HO
OH
OH
O
H
N
N
OH
Size
Size
10 mM/1 mL in DMSO
100 mg 200 mg
Size
10 mM/1 mL in DMSO
25 mg 5 mg 10 mg
Size
10 mM/1 mL in DMSO
100 mg 10 mg 25 mg
Size
10 mM/1 mL in DMSO
100 mg 500 mg
Size
Topo I selective
81
Topoisomerase / Telomerase
D
N
A

D
a
m
a
g
e
Moxifloxacin(Avelox, Avalox) is a fourth
generation synthetic fluoroquinolone
antibacterial agent.
S1465 Moxifloxacin HCl
Irinotecan prevents DNA from unwinding by
inhibition of topoisomerase 1.
S2217 Irinotecan HCl Trihydrate Topo I selective
N
O
OH
O
O
F
N
HN
H
H
HCl
N N
O
O
N
N O
O
O
OH
H2O
H2O H2O HCl
Epirubicin HCl, a semisynthetic L-arabino
derivative of doxorubicin, is an antineoplastic
agent by inhibitingTopoisomerase.
S1223 Epirubicin HCl
Data independently
produced by Dr. Edita
Aksamitiene fromThomas
J efferson University
Epirubicin HCl purchased
fromSelleck
Product Citation:
J Biol Chem, 2013, 288(22): 15537-46
Topo II selective
Camptothecin (NSC100880) is a specific
inhibitor of DNA topoisomerase I (Topo I) with
IC50 of 0.68 M. Phase 2.
S1288 Camptothecin
50 mg
Size
Topo I selective
new
Idarubicin HCl (Idamycin, Zavedos,
4-demethoxydaunorubicin) is a hydrochloride
salt form of Idarubicin which is an
anthracycline antibiotic and a DNA
topoisomerase II (topo II) inhibitor for MCF-7
cells with IC50 of 3.3 ng/mL.
S1228 Idarubicin HCl
Data from[ J Phys Chem B,
2013, 117(23): 6868-73 ]
Idarubicin HCl purchased
fromSelleck
Product Citation:
J Phys Chem B, 2013, 117(23): 6868-73
O O
O
OH
OH
OH
O
OH
O
O H OH
NH2
HCl
O
O
OH
OH O
OH
O O
NH2
OH
HCl
O N
O
O
HO N
Genistein, a phytoestrogen found in soy
products, is a highly specific inhibitor of
protein tyrosine kinase (PTK) which blocks
the mitogenic effect mediated by EGF on
NIH-3T3 cells with IC50 of 12 M or by insulin
with IC50 of 19 M.
S1342 Genistein
Pirarubicin is an anthracycline agent.
S1393 Pirarubicin
10 mg 50 mg 200 mg
Size
Amonafide (NSC-308847) produces protein-
associated DNA-strand breaks through a
topoisomerase II-mediatedreaction, but does
not produce topoisomerase I-mediated DNA
cleavage. Phase 3.
S1367 Amonafide Topo II selective
N
NH2
O
N
O
O
O
OH
HO
OH
O O
NH2
O
O
HO
O
HO
H
OH
OH
O
O O
SN-38 is an active metabolite of CPT-11,
inhibits DNAtopoisomerase I with IC50 of 1 M,
inhibits DNA synthesis and causes frequent
DNA single-strand breaks.
S4908 SN-38
10 mg 50 mg
Size
Topo I selective
N
N
O
O
O
HO
HO
BIBR 1532 is a potent, selective, non-
competitive telomerase inhibitor with IC50 of
100 nM.
S1186 BIBR 1532
DaunorubicinHCl inhibits bothDNAandRNA
synthesis and inhibits DNA synthesis with Ki
of 0.02 M.
S3035 Daunorubicin HCl
Costunolide, a natural sesquiterpene
compound with multiple biological activities;
inhibits FPTase with IC50 of 20 M, also
inhibits telomerase with IC50 of 90 M and 65
M.
S1319 Costunolide
Telomerase Inhibitors
(E) N
H
O
COOH
O
O
O O
O
OH
OH
OH
O
O
O
H
OH
NH2
HCl
Size
Size
Size
10 mM/1 mL in DMSO
25 mg 5 mg 100 mg
Size
10 mM/1 mL in DMSO
10 mg 5 mg 50 mg
Size
Size
Size
400
500
600
700
800
1000 2000 3000 4000 5000 6000
0.2 a
b
s
o
rb
a
n
c
e
0.4
0.6
0.8
0
.2
0
.4
0
.6
0
.8
400
500
600
700
800
w
a
v
e
le
n
g
th
(n
m
)
Size
Size
82
Phone:+1-832-582-8158
www.selleckchem.com
PARP / Pim / Aurora Kinase / JAK / HIF / Sirtuin / HDAC
E
p
i
g
e
n
e
t
i
c
s
PARP Inhibitors
JAK Inhibitors
Pim Inhibitors
HIF Inhibitors
Aurora Kinase Inhibitors
Sirtuin Inhibitors & Chemicals
Vorinostat (suberoylanilide hydroxamic acid,
SAHA, Zolinza) is an HDAC inhibitor with IC50
of ~10 nM.
S1047 Vorinostat (SAHA, MK0683)
Data from[ J Exp Med,
2012, 209(1): 35-50 ]
Vorinostat purchased from
Selleck
HDAC Inhibitors
Epigenetics
Product Citations:
Nature, 2011, 471(7337): 235-9
Nat Biotechnol, 2011, 29(3): 255-65
H
N
O
N
H
O
OH
MS-275 strongly inhibits HDAC1 and HDAC3
with IC50 of 0.51 M and 1.7 M, compared
with HDACs 4, 6, 8, and 10. Phase 1/2.
S1053 Entinostat (MS-275)
Data from[ Brain, 2011,
134(Pt 8): 2408-21 ]
Entinostat purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 200 mg 50 mg
Size
Product Citations:
Nat Biotechnol, 2011, 29(3): 255-65
Circ Res, 2012, 110(5): 739-48
N
O
H
N
O
NH
O
NH2
LBH589 (Panobinostat) is a novel
broad-spectrum HDAC inhibitor with IC50 of 5
nM. Phase 3.
S1030 Panobinostat (LBH589)
Data from[ Acta
Neuropathol, 2011, 122(5):
637-50 ]
Panobinostat purchased
fromSelleck
Product Citations:
Nat Biotechnol, 2011, 29(3): 255-65
Blood, 2012, 119(6): 1450-8
Trichostatin A(TSA) is an HDAC inhibitor with
IC50 of ~1.8 nM. HDAC8 is the only known
member of the HDAC-family that is not
affected byTSA. Phase 3.
S1045 Trichostatin A (TSA)
Data from[ Epigenetics,
2012, 7(10): 1161-72 ]
Trichostatin A purchased
fromSelleck
Product Citation:
Plant J, 2013, 74(5): 815-28
N
H
HN
O
H
N
OH
N
N
H
O O
OH
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
10 mM/1 mL in DMSO
50 mg 5 mg 10 mg
Size
10 mM/1 mL in DMSO
200 mg 500 mg
Size
MS-275
Ac-H3K18
Ac-H3K14
Ac-H4K12
P35
P25
Septin 7
OPA1
Actin
0d 5d 10d
Injection 0d 5d10dDays
1
5
10
4h Dissection
Vehicle
MS-275
Post-injection
untreated DMSO 0.2% 0.01 M 0.1 M 1 M 10 M
untreated DMSO 0.1% 1 nM 10 nM 50 nM 100 nM
V
o
rin
o
s
ta
t
P
a
n
o
b
in
o
s
ta
t
Control Sb TSA TSA +Sb Saha Saha +Sb
P
-h
is
to
n
e

H
3
Ser10
p
-M
P
M
-2
D
A
P
I
M
e
rg
e
6
0
X
4
0
X
T
u
b
u
lin
/D
A
P
I
HDAC
E
p
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g
e
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i
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s
83
MGCD0103 (Mocetinostat) is a potent HDAC
inhibitor with most potency for HDAC1 with
IC50 of 0.15 M, 2- to 10-fold selectivity
against HDAC2, 3, and 11, and no activity to
HDAC4, 5, 6, 7, and 8. Phase 1/2.
S1122 Mocetinostat (MGCD0103)
Data from[ Oncogene,
2011, 30(27): 3062-72 ]
Mocetinostat purchased
fromSelleck
Product Citations:
Nat Struct Mol Biol, 2013, 20(3): 317-25
Circ Res, 2012, 110(5): 739-48
N N
N
N
H H
N
O
NH2
10 mg 50 mg
Size
Resminostat (RAS2410) dose-dependently
and selectively inhibits HDAC1/3/6 with IC50
of 42.5 nM/50.1 nM/71.8 nM, less potent to
HDAC8 with IC50 of 877 nM.
S2693 Resminostat
Product Citation:
J Biol Chem, 2013, 288(20): 14400-7
new
Scriptaid is an inhibitor of HDAC. It shows a
greater effect on acetylated H4 than H3.
S8043 Scriptaid new
50 mg
Size
Tubastatin Ais a potent and selective HDAC6
inhibitor with IC50 of 15 nM. It is selective
against all the other isozymes (1000-fold)
except HDAC8 (57-fold).
S8049 Tubastatin A new
Belinostat (PXD101) is a novel HDAC
inhibitor with IC50 of 27 nM, with activity
demonstrated in cisplatin-resistant tumors.
Phase 1/2.
S1085 Belinostat (PXD101)
Data from[ Breast Cancer
Res Treat, 2011, 131(3):
777-89 ]
Belinostat purchased from
Selleck
10 mM/1 mLin DMSO
10 mg 50 mg 200 mg
Size
Product Citations:
Nat Biotechnol, 2011, 29(3): 255-65
Breast Cancer Res Treat, 2011, 131(3): 777-89
Sodium Phenylbutyrate is a transcriptional
regulators that act by altering chromatin
structure via the modulation of HDAC activity.
S4125 Sodium Phenylbutyrate new
S
N
H
N
H
O
OH
O O
MC1568 is a selective HDAC inhibitor for
HDAC1A with IC50 of 100 nM. It is 34-fold
more selective for HDAC1A than HDAC1B.
S1484 MC1568
2013, ahead of print ]
MC1568 purchased from
Selleck
Product Citation:
F
O
N
H
N
O
OH
200 mg
Tubastatin Ais a potent and selective HDAC6
inhibitor with IC50 of 15 nM. It is selective
(1000-fold more) against all other isozymes
except HDAC8 (57-fold more).
S2627 Tubastatin A HCl
LAQ824 (NVP-LAQ824) is a novel HDAC
inhibitor with IC50 of 32 nM and is known to
activate the p21 promoter.
S1095 LAQ824 (Dacinostat)
Data from[ Diabetologia,
2012, 55(9): 2421-31 ]
LAQ824 purchased from
Selleck
10 mg 50 mg
Size
Product Citations:
Nat Biotechnol, 2011, 29(3): 255-65
Diabetologia, 2012, 55(9): 2421-31
SB939 is a potent pan-HDAC inhibitor with
IC50 of 40-140 nM with exception for HDAC6.
It has no activity against the class III
isoenzyme SIRT I. Phase 2.
S1515 SB939 (Pracinostat)
Data from[ Antimicrob
Agents Chemother, 2012,
56(7): 3849-56 ]
SB939 purchased from
Selleck
Product Citation:
Antimicrob Agents Chemother, 2012, 56(7): 3849-56
S1194 CUDC-101
CUDC-101 is a potent multi-target inhibitor targeting HDAC, EGFR
and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, inhibits both
class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
N
HO
N
H
HN
O
HO
H
N
HO
O
N
N
HCl
N
N N
H
O
HO
N
N O O
NH
O
HO
H
N
HO
O
N
N
O
NaO
N
S
N
O
O
NH
O OH
10 mM/1 mL in DMSO
25 mg 10 mg
Size
10 mM/1 mL in DMSO
10 mg 5 mg 50 mg
Size
Size
Size
Size
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
Page 23
H3K4me2
Acety-H3
H3
H3K4me2
Acety-H3
H3
SAHA TSA MS-275 LBH-589 PXD-101
U
n
tre
a
te
d
0
.5

M
1

M
5

M
1
0

M
U
n
tre
a
te
d
0
.5

M
1

M
5

M
1
0

M
U
n
tre
a
te
d
0
.5

M
1

M
5

M
1
0

M
U
n
tre
a
te
d
0
.5

M
1

M
5

M
1
0

M
U
n
tre
a
te
d
0
.5

M
1

M
5

M
1
0

M
MDA-
MB-231
MDA-
MB-468
84
Phone:+1-832-582-8158
www.selleckchem.com
HDAC
E
p
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g
e
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t
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c
s
Droxinostat (CMH, 5809354) is a selective
inhibitor of HDAC, mostly for HDACs 6 and 8
with IC50 of 2.47 M and 1.46 M, greater
than 8-fold selective against HDAC3 and no
inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.
S1422 Droxinostat
Data independently
Droxinostat purchased from
Selleck
Product Citation:
Nat Struct Mol Biol, 2013, 20(3): 317-25
PCI-24781 (CRA-024781) is a novel
pan-HDAC inhibitor mostly targeting HDAC1
withKi of 7 nM, modest potent to HDACs 2, 3,
6, and 10 and greater than 40-fold selectivity
against HDAC8. Phase 1/2.
S1090 PCI-24781
2013, 8(5): e65369 ]
PCI-24781 purchased from
Selleck
10 mM/1 mL in DMSO
5 mg 50 mg
Size
Product Citation:
Nat Biotechnol, 2011, 29(3): 255-65
JNJ-26481585 is a novel second-generation
HDAC inhibitor with highest potency for
HDAC with IC50 of 0.11 nM, modest potent to
HDACs 2, 4, 10, and 11; greater than 30-fold
selectivity against HDACs 3, 5, 8, and 9 and
lowest potency to HDACs 6 and 7. Phase 2.
S1096 JNJ-26481585
Data independently
fromSelleck
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Romidepsin (FK228, FR901228,
depsipeptide, NSC 630176) is a potent
HDAC1 and HDAC2 inhibitor with IC50 of 36
S3020 Romidepsin (FK228, depsipeptide)
Data from[ Br J Haematol,
2013, 162(4): 559-62 ]
Romidepsin purchased from
Selleck
Product Citation:
J Neurosci, 2013, 33(17): 7535-47
O
N
O
HN
O
O
NH
OH
1mg 5mg
Size
Apicidin is a potent nonselective HDAC
inhibitor with IC50 of 0.7 nM.
S4909 Apicidin (OSI-2040)
Product Citation:
J Neurosci, 2013, 33(17): 7535-47
Size
Valproic acid sodium salt (Sodium valproate)
is an HDAC inhibitor with IC50 of 0.4 mM and
also inhibits GABA-transaminase or succinic
semialdehyde dehydrogenase.
S1168 Valproic acid sodium salt (Sodium valproate)
Rocilinostat (ACY-1215) is a selective
HDAC6 inhibitor with IC50 of 5 nM. It is
>10-fold more selective for HDAC6 than
HDAC1/2/3 (class I HDACs) with slight
activity against HDAC8, minimal activity
against HDAC4/5/7/9/11, Sirtuin1, and
Sirtuin2.
S8001 Rocilinostat (ACY-1215)
S2759 CUDC-907
CUDC-907 is a dual PI3K and HDAC inhibitor for PI3K and
HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM,
HDAC1selective
CI994 (Tacedinaline) is an anti-cancer drug
which inhibits HDAC1 with IC50 of 0.57 M
and causes G1 cell cycle arrest. Phase 3.
S2818 CI994 (Tacedinaline)
M344 is a potent HDAC inhibitor with IC50 of
100 nM and able to induce cell differentiation.
S2779 M344
AR-42 (OSU-HDAC42) is an HDAC inhibitor
with IC50 30 nM.
S2244 AR-42
PCI-34051 is a potent and specific HDAC8
inhibitor withIC50 of 10nM. It has greater than
200-fold selectivity over HDAC1 and 6, more
than 1000-fold selectivity over HDAC2, 3, and
10.
S2012 PCI-34051 HDAC8selective
N
H
O N
H
O
OH
N
O
HN
O
HO
ONa
O
HN
O
O
HN
H2N
N
H
N
O
H
N
O
OH
N
N
N
O
H
N NHOH
O
NH
N
N
H
O
O N
H
N
O
O
O O
S S
(S) (S)
NH
(S) (S) NH
(R) (R) O
O
O
(S) (S)
O
NH
NH
O
O
10 mM/1 mL in DMSO
10 mg 5 mg 25 mg
Size
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO
1 mg 5 mg
Size
Page 5
LBH589 50 nM
FK228 50 nM
ACY-1215 5 M
ACY-1215 10 M
ACY-738 5 M
ACY-738 10 M
ACY-775 5 M
ACY-775 10 M
CELL DEATH
PROPORTION
0-20%
20-40%
40-60%
60-80%
80-100%
1 2 3 4 5 6 7 8
HDAC / Histone Demethylases / Histone Acetyltransferase / Epigenetic Reader Domain / DNA Methyltransferase
E
p
i
g
e
n
e
t
i
c
s
85
RG108 is an inhibitor of DNA
methyltransferase with IC50 of 115 nM, does
not cause trapping of covalent enzymes.
S2821 RG108
SGI-110 (S-110) is a stable and potent
inhibitor for DNA methylation, inhibits DNMT1
when SGI-110 is activated by
phosphorylation and incorporated into DNA.
Phase 2.
S7013 SGI-110
10 mg 50 mg
Size
Cat.No. Inhibitor Name HDAC1 HDAC2 HDAC3 HDAC8 HDAC5 HDAC9 HDAC4 HDAC6 HDAC10 HDAC11
+++ ++ +++
+++ ++
17 nM[Ki] 24 nM[Ki]
++++ ++++ ++++
0.64 nM [IC50] 0.46 nM [IC50]
0.37
0.37 nM [IC50]
+
220 nM[IC50]
+ + ++
70 nM [IC50] 56 nM[IC50] 40 nM[IC50]
++
15 nM[IC50]
S1030 Panobinostat +++ ++ +++ +++ 13.2 nM
13.2 nM [IC50] 2.5 nM [IC50] 2.1 nM [IC50] 7.8 nM [IC50] 5.7 nM [IC50] 10.5 nM[IC50] 2.3 nM [IC50]
S1090 PCI-24781 +++ ++ +++ +
7 nM[Ki] 19 nM[Ki] 8.2 nM[Ki] 280 nM[Ki]
S1096 J NJ -26481585 ++++ ++++ 0.11 nM 0.33 nM
0.33 nM[IC50]
S1122 Mocetinostat 0.29
S1422 Droxinostat
S1484 MC1568
S1515 SB939 ++ ++ ++
49 nM[IC50] 43 nM[IC50]
47
47 nM [IC50]
S2012 PCI-34051 +++
10 nM[IC50]
S2170 ITF2357 ++ ++
16 nM[IC50] 10 nM[IC50]
S2627
Tubastatin A
Tubastatin A HCl +
854 nM[IC50]
S2818 CI994
+
2.47 M [IC50]
+ + +
0.15 M [IC50] 0.29 M [IC50] 1.66 M [IC50]
+ +
16.9 M [IC50] 1.46 M [IC50]
+
0.57 M[IC50]
0.11 nM[IC50]
GSK J4 HCl is a cell permeable prodrug of
GSK J1, which is the first selective inhibitor of
the H3K27 histone demethylase JMJD3 and
UTX with IC50 of 60 nM and inactive against a
panel of demethylases of the JMJ family.
S7070 GSK J4 HCl
Histone Demethylases Inhibitor
C646 is a selective p300/CREB-binding
protein (CBP) inhibitor with Ki of 400 nM.
S7152 C646
Histone Acetyltransferase Inhibitor
Decitabine is a potent inhibitor of DNA
methylation with IC50 of 438 nM and 4.38 nM
in HL-60 and KG1a cells, respectively.
S1200 Decitabine
DNA Methyltransferase Inhibitors
Azacitidine is a nucleoside analogue of
cytidine that specifically inhibits DNA
methylation by trapping DNA
methyltransferases.
S1782 Azacitidine
Thioguanine is a purine antimetabolite widely
used in the treatment of acute lymphoblastic
leukemia, autoimmune disorders (e.g.,
Crohn's disease, rheumatoid arthritis) and
organ transplant recipients.
S1774 Thioguanine
50 mg 500 mg
Size
10 mg 25 mg
Size
(+)-JQ1 is a BET bromodomain inhibitor, with
IC50 of 33 nM for BRD4(2), binding to all
bromodomains of the BET family, but not to
bromodomains outside the BET family.
S7110 (+)-JQ1
PFI-1 is a selective BET (bromodomain-
containing protein) inhibitor for BRD4 with
IC50 of 0.22 M.
S1216 PFI-1
Epigenetic Reader Domain Inhibitors
N
N
N N
NH
O
O
HCl
NO2
O
N
N O
OH
O
N
N
N
N
S
Cl
O
O
O
OH
OH
N
HO
N
N
O
NH2
N
N
H
N
H
N
H2N
S
(S) (S) N
O
O
NH
OH
O
H
N
O
O
P O
O
HO
ONa
NH
N
N
O
NH2 N
O
OH
N N
O
NH2
Size
Size
Size
Size
Size
86
Phone:+1-832-582-8158
www.selleckchem.com
DNA Methyltransferase / Histone Methyltransferase
E
p
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c
s
Zebularine is a DNA methylation inhibitor that
forms a covalent complex with DNA
methyltransferases, also inhibits
cytidinedeaminase with Ki of 2 M.
S7113 Zebularine
BIX01294 is an inhibitor of G9a histone
methyltransferase with IC50 of 2.7 M,
reduces H3K9me2 of bulk histones, also
weakly inhibits GLP (primarily H3K9me3), no
significant activity observed at other histone
methyltransferases.
S8006 BIX01294
Histone Methyltransferase Inhibitors
Entacapone inhibits
catechol-O-methyltransferase(COMT) with
IC50 of 151 nM.
S3147 Entacapone
EPZ-5676 is an S-adenosyl methionine
(SAM) competitive inhibitor of protein
methyltransferase DOT1L with Ki of 80 pM,
demonstrating >37,000-fold selectivity
against all other PMTs tested, inhibits H3K79
methylation in tumor. Phase 1.
S7062 EPZ-5676
10 mg 50 mg
Size
SGC 0946 is a highly potent and selective
DOT1L methyltransferase inhibitor with IC50
of 0.3 nM, is inactive against a panel of 12
PMTs and DNMT1.
S7079 SGC 0946
10 mg 50 mg
Size
10 mg 50 mg
Size
10 mg 50 mg
Size
new
UNC1999 is a SAM-competitive, potent and
selective inhibitor of EZH1 and EZH2 with
IC50 of 45 nM and <10 nM, respectively.
S7165 UNC1999 new
GSK343 is a potent, selective, cell-active
EZH2 inhibitor with IC50 of 4 nM.
S7164 GSK343 new
10 mg 50 mg
Size
UNC0224 is a selective histone lysine
methyltransferase (HMTase) inhibitor for G9a
and GLP with IC50 of 15 nM and 20 nM,
respectively.
S8070 UNC0224 new
5 mg 50 mg
Size
respectively, with excellent potency in a
variety of cell lines and excellent separation
of functional potency versus cell toxicity.
S8069 UNC0631 new
10 mg 50 mg
Size
and GLP with IC50 of <15 nM and 19 nM,
respectively, with excellent potency and
selectivity over a wide range of epigenetic
and non-epigenetic targets.
S8071 UNC0638 new
1 mg 5 mg
Size
3-deazaneplanocin A (DZNeP), an analog of
adenosine, is a competitive inhibitor of
S-adenosylhomocysteine hydrolase with Ki of
50 pM.
S7120 3-Deazaneplanocin A (DZNeP) new
5 mg 50 mg
Size
EPZ004777 is a potent, selective DOT1L
S7032 EPZ004777 new
5 mg 50 mg
Size
UNC0321 (trifluoroacetate salt) is a selective
histone lysine methyltransferase (HMTase)
inhibitor for G9a and GLP with IC50 of 6 nM
S7012 UNC0321 (Trifluoroacetate salt) new
10 mg 50 mg
Size
respectively, with excellent potency in a
variety of cell lines and excellent separation
of functional potency versus cell toxicity.
S7020 UNC0646 new
O
N
OH OH
HO
N
O
N
N
NH
N
O
O
N
N
3HCl
O
N
N+
O
-O
HO OH
N
N
O N
HO OH
N
N
N
NH2
N
HN
N
H
O
N
H
N
O
N
HO OH N N
Br
NH2
N N
N
N
N
O
H
N
H
N O
N
N
N
H
O NH
O
N
N
N
N
N
NH
N
O
N
N
O N
N
N
NH
N
O
N
N
O N
N
N
NH
N
O
O N
N N
N
NH2
OH
HO
HO
H
N H
N
O
N
O
N
OH
OH
N
N
NH2
N
N
NH
N
N
O
O
O
N
N
CF3COOH
CF3COOH
CF3COOH
N
N
NH
O N
O
N
N
N
Size
Size
Size
O
HO
HO
N
N
N
O
NH2
NH
N
O
HN
S
O
O O
10 mg 50 mg
Size
GSK-3 / JAK / STAT / TGF-beta/Smad / ROCK / Wnt/beta-catenin
S
t
e
m

C
e
l
l
s

a
n
d

W
n
t
Data from[ Toxicol Sci,
2013, 133(1): 42-53 ]
XAV-939 purchased from
Selleck
XAV-939 selectively inhibits Wnt/-catenin-
mediated transcription through tankyrase1/2
inhibition with IC50 of 11 nM/4 nM, regulates
axin levels and does not affect CRE, NF-B or
TGF-.
S1180 XAV-939
Product Citations:
J Mol Cell Cardiol, 2013, 62C: 203-13
Cancer Lett, 2013, 335(2): 332-42
Stem Cells and Wnt Pathway
Wnt/beta-catenin Inhibitors
GSK-3 Inhibitors
ROCK Inhibitors
JAK Inhibitors
STAT Inhibitors
TGF-beta/Smad Inhibitors
CF3
N
N
HO
S
10 mM/1 mL in DMSO
200 mg 10 mg 50 mg
Size
Vehicle TCDD DKK1 + DKK2 XAV-939
N
u
m
b
e
r o
f P
ro
s
ta
tic
B
u
d
s
0
5
10
15
20
25
30
88
Phone:+1-832-582-8158
www.selleckchem.com
Wnt/beta-catenin / Gamma-secretase
S
t
e
m

C
e
l
l
s

a
n
d

W
n
t
ICG-001 antagonizes Wnt/-catenin/TCF-
mediated transcription and specifically binds
to element-binding protein (CBP) with IC50 of
3 M, but is not the related transcriptional
coactivator p300.
S2662 ICG-001
IWP-2 is an inhibitor of Wnt processing and
secretion with IC50 of 27 nM, selective
blockage of Porcn-mediated Wnt
palmitoylation, does not affect Wnt/-catenin
in general and displays no effect against
Wnt-stimulated cellular responses.
S7085 IWP-2
5 mg 25 mg
Size
IWR-1 (endo-IWR 1) is a Wnt pathway
inhibitor with IC50 of 180 nM, induces Axin2
protein levels and promotes -catenin
phosphorylation by stabilizing Axin-scaffolded
destruction complexes.
S7086 IWR-1-endo
10 mg 25 mg
Size
Wnt-C59 (C59) is a PORCN inhibitor for
Wnt3A-mediated activation of a multimerized
TCF-binding site driving luciferase with IC50 of
74 pM.
S7037 Wnt-C59 (C59)
5 mg 50 mg
Size
new
5 mg 50 mg 200 mg
Size
BMS-708163 is a potent, selective, orally
bioavailable -secretase inhibitor of A40 and
A42 with IC50 of 0.3 nM and 0.27 nM,
demonstrating a 193-fold selectivity against
Notch. Phase 2.
S1262 BMS-708163 (Avagacestat)
KY02111 promotes differentiation of hPSCs
to cardiomyocytes by inhibiting Wnt signaling,
may act downstream of APC and GSK3.
S7096 KY02111
10 mg 50 mg
Size
new
new
MK-0752 is a moderately potent -secretase
inhibitor, which reduces A40 production with
IC50 of 5 nM. Phase 1/2.
S2660 MK-0752
5 mg 25 mg
Size
LY900009 is a potent Notch inhibitor with IC50
of 0.27 nM.
S7168 LY900009
new
5 mg 25 mg
Size
LY3039478 is a potent Notch inhibitor with
IC50 of 0.41 nM.
S7169 LY3039478
DAPT (GSI-IX) is a novel -secretase
inhibitor, which inhibits A production with
IC50 of 20 nM in HEK 293 cells.
S2215 DAPT (GSI-IX)
Gamma-secretase Inhibitors
RO4929097 is a secretase inhibitor with
IC50 of 4 nM, inhibiting cellular processing of
A40 and Notch with EC50 of 14 nM and 5 nM,
S1575 RO4929097
Product Citation:
Development, 2013, 140(7): 1402-11
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
Data from[ Development,
2013, 140(7): 1402-11]
RO4929097 purchased from
Selleck
Semagacestat (LY450139) is a -secretase
blocker for A42, A40 and A38 with IC50 of
10.9 nM, 12.1 nM and 12.0 nM, also inhibits
Notch signaling with IC50 of 14.1 nM. Phase 3.
S1594 Semagacestat (LY450139)
Product Citation:
J Biol Chem, 2012, 287(15): 11810-9
10 mM/1 mL in DMSO
200 mg 5 mg 50 mg
Size
2012, 287(15): 11810-9 ]
Semagacestat purchased
fromSelleck
H
N N
O
N
N
O
H
O OH
O
HN
H
N
H
N
F
O O
F F
F F
N
S
O O
Cl
F
N
O
N
H2N
O
CF3
H
N
O
N
H
O
O
N
OH
S
Cl
O
O
F
F
O
HO
N
N
S
O
S
O
N
H
N
S
N
O
O
O
HN
N
H
O
N
H
O
O
S
N Cl
N
N
H
O
N
F
F
O
H
N
N
H
O
O
O
HO
O
H
N
O
N
H
N
O
F3C
O
H
N
O
N
H
N
O
N
OH
Size
Size
Size
DMSO RO4929097
6
2
-7
2
h
p
a
tre
a
tm
e
n
t
1
-7
2
h
p
a
tre
a
tm
e
n
t
6
2
-7
2
h
p
a
tre
a
tm
e
n
t
B
rd
U
+
c
e
ll/ D
A
P
I n
u
c
le
i in
%
0
4
8
12
16
20
DM
SO
RO4929079
Proliferation in the
blastema after
10h treatment
DMSO RO4929097 DMSO RO4929097
P
P
P
P
P
P
P
P
P
P
P
P
(cAMP)
Ca2+
PI3K
SUFU
GRK
CKI
Axin
Axin APC
PTC SMO
Frizzled
AKT
GTP
GTP
GTP
i
Hedgehog
PKA
Gli
Gli NFAT
API
-Secretase
Proteasome
Ub Ub Ub
Ub
GSK3
GSK3
GSK3
DSH
Rac
Rho
PLC
PKC
JNK
SHARP
HDAC
SMRT
CtBp
Nicd
CSL
Nicd
CSL
STAT3
Hes1 TAK2
Hes1 STAT3
STAT3
LIF
LIFR gp130
FGF
MAPK
Cdx2
Gata6
Others
Caspase-3
Ronin
STAT3
P300
Mam
SMAD1
SMAD4
SMAD1
SMAD4 gfap
idl
FGFR
-cat
-cat
-cat
-cat
TCF/LEF
Intracellular
vesicle
TGF
T
ra
n
s
lo
c
a
tio
n
S2
ADAM17
Sanpodo
TGFR
TGFR
Gene expression
E(spl)
hey
herp2
hey
hes1
hey1
hes1
Dll13,4/Jagged1,2
Wnt
BMP
Vi smodegi b
Cycl opami ne
LY2940680
Hedgehog inhibitors
CHIR-99021
CHIR-98014
LY2090314
Pan-GSK3 inhibitors
SB 216763(GSK-3)
Tideglusib(GSK-3)
TWS119(GSK-3)
Selective GSK3 inhibitors
Fl udarabi ne(STAT1)
NSC 74859(STAT3)
Ni cl osami de(STAT3)
Selective STAT inhibitors
SB-505124(ALK4 & ALK5)
SB 431542(TRI/ALK5)
LY2157299(TRI/ALK5)
SB 525334(TRI/ALK5)
LDE225
PF-5274857
LY2940680
Smoothened antagonists
XAV-939
ICG-001
IWP-2
IWR-1-endo
Wnt/beta-catenin
inhibitors
RO4929097
DAPT
YO-01027
Semagacestat
BMS-708163
-secretase inhibitors
XAV-939
ICG-001
IWP-2
IWR-1-endo
Wnt/beta-catenin
inhibitors
Gamma-secretase / Hedgehog/Smoothened
S
t
e
m

C
e
l
l
s

a
n
d

W
n
t
YO-01027 (Dibenzazepine, DBZ) is a
dipeptidic-secretase inhibitor with IC50 of 2.6
nM and 2.9 nM for APPL and Notch cleavage,
respectively.
S2711 YO-01027
LY2811376 is the first orally available
non-peptidic -secretase(BACE1) inhibitor
with IC50 of 239 nM-249 nM, that act to
decrease A secretion with EC50 of 300 nM,
demonstrated to have 10-fold selectivity
towards BACE1 over BACE2, and more than
50-fold inhibition over other aspartic
proteases including cathepsin D, pepsin, or
renin. Phase 1.
S1528 LY2811376
Hedgehog/Smoothened Inhibitors
& Chemicals
LY-411575 is a potent -secretase inhibitor
with IC50 of 0.078 nM/0.082 nM (membrane
/cell-based), also inhibits Notch clevage with
with IC50 of 0.39 nM.
S2714 LY411575
LY2811376
RO4929097
Semagacestat
DAPT
MK-0752
LY411575
S1528
S1575
S1594
S2215
S2660
S2714
+++
++
+++
++++
4 nM [IC50]
20 nM [IC50]
5 nM [IC50]
0.078 nM [IC50]
+
++
++
+++
303 nM [IC50]
14 nM [IC50]
12.1 nM [IC50]
5 nM [IC50]
+
++
299 nM [IC50]
10.9 nM [IC50] ++ 12.0 nM [IC50]
Cat.No. Inhibitor Name -Secretase A40 A42 A38
GDC-0449 (Vismodegib, HhAntag691) is a
potent, novel and specific hedgehog inhibitor
with IC50 of 3 nM and also inhibits P-gp with
IC50 of 3.0 M.
S1082 Vismodegib (GDC-0449)
Data from[ Gut, 2013, 62(2):
299-309 ]
Vismodegib purchased from
Selleck
Product Citations:
Gastroenterology, 2012, 143(5): 1319-29.e1-11
Hepatology, 2011, 54(5): 1580-90
10 mM/1 mL in DMSO
5 mg 200 mg 50 mg
Size
Cyclopamine is a specific Hedgehog (Hh)
signaling pathway antagonist of Smoothened
(Smo) with IC50 of 46 nM.
S1146 Cyclopamine
Data from[ Cancer Lett,
2012, 322(2): 169-76 ]
Cyclopamine purchased
fromSelleck
Product Citations:
Cancer Res, 2012, 72(9): 2262-74
Neuro Oncol, 2012, 14(12): 1441-51
10 mM/1 mLin DMSO
5mg 50mg 25 mg
Size
F
F
H
N
O
N
H
O
N O
F
F
H
N
O
N
H
O
N O
OH
Cl
N
N
H
O Cl
S
O O
O
HN
HO
H
H
H
H
H
N
N
F F
N
S
NH2
Size
Size
Size
Normal control 100 ng/mL SDF-1
100 ng/mL SDF-1
+
10 M Cyclopamine
MiaCaPa-2
Panc-1
90
Phone:+1-832-582-8158
www.selleckchem.com
Hedgehog/Smoothened
S
t
e
m

C
e
l
l
s

a
n
d

W
n
t
LY2940680 binds to the Smoothened (Smo)
receptor and potently inhibits Hedgehog (Hh)
signaling. Phase 1/2.
S2157 LY2940680
5 mg 50 mg 200 mg
Size
PF-5274857 is a potent and selective
Smoothened (Smo) antagonist, inhibits
Hedgehog (Hh) signaling with IC50 and Ki of
5.8 nM and 4.6 nM, respectively, and can
penetrate the blood-brain barrier.
S2777 PF-5274857
LEQ506 is a selective smoothened (SMO)
receptor inhibitor with IC50 of 2 nM.
S7212 LEQ506 new
PF-04449913 is a potent and orally
bioavailable inhibitor of Smoothened with IC50
of 5 nM.
S7160 PF-04449913 new
TAK-441 is a potent and selective
smoothened (Smo) antagonist with IC50 of 4.4
nM.
S7066 TAK-441 new
10mg
Size
SANT-1 directly binds to Smoothened (Smo)
receptor with Kd of 1.2 nM and inhibits Smo
agonist effects with IC50 of 20 nM.
S7092 SANT-1
LDE225 (NVP-LDE225) is a Smoothened
(Smo) antagonist, inhibiting Hedgehog (Hh)
signaling with IC50 of 1.3 nM (mouse) and 2.5
nM (human), respectively. Phase 3.
S2151 LDE225 (NVP-LDE225,Erismodegib)
Data from[ Nat Chem Biol,
2013, 9(4): 247-9 ]
LDE225 purchased from
Selleck
Product Citation:
Nat Chem Biol, 2013, 9(4): 247-9
10 mM/1 mL in DMSO
5 mg 50 mg 25 mg
Size
Licensed by Pfizer
N
N O HN
O
F3CO
N N
N N
O
F
F3C
N N
N
N
N
Cl
N O
S
O
O
N
N
N
OH
N
N
N
N
H
N N
HN
O
HN CN
O
N
N
O O
CF3
HN
O
N
O
OH
N
N
N
N
N
Size
10 mg 50 mg
Size
10 mg 50 mg
Size
10 mg 50 mg
Size
91
DUB
U
b
i
q
u
i
t
i
n
S2243
S7134
S7130
Ubiquitin Pathway
RING-type
AMP+PPi
ADP+Pi
Proteasome
Proteasome
Proteasome
Cellular stress
ARF
p53
p53
IB
IB
MDM2
Stress
IB kinase
Proteasome
Proteasome
Proteasome inhibition
CDC25C
CDKcyclin B
CDKcyclin A
CDKcyclin D
CDKcyclin E
CDC25A, CDC25C
KIP1
Apoptosis
Apoptosis
G0
M
G2
G1
S
WAF1
CDC25B
CDKcyclin A
ATP
ATP
E2
E1
S
S
S
C
Ub
O =
S
C
Ub
O =
N H
C O =
S
26S Proteasome
RP
DUBs
DUBs
C Ub
UbUb
Ub
UbUbUb Ub
Ub
Ub
Ub
Ub
Ub
Ub
Ub
Ub
Ub
UbUbUb
O =
S
C
Ub
O =
HECT-type
Cellular pathways associated with the proteasome
HECT
RING Finger S
NF-B
IB NF-B
p53 Gene
expression
Gene
expression
Pro-survival
pathway
Senescence
NF-B
E3
E3
E2
P
P
MG-132
Bortezomi b
Carfi l zomi b
MLN9708
MLN2238
Del anzomi b
Proteasome inhibitors
b-AP15
WP1130
NSC 632839
IU1
PR-619
DUB inhibitors
JNJ 26854165
Nutl i n-3
Thal i domi de
TAME
NSC-207895
E3 ligase inhibitors
MLN4924
PYR-41
E1 activating inhibitors
BAY 11-7082
E2 conjugating inhibitors
DUB Inhibitors
Proteasome Inhibitors
WP1130
WP1130 (Degrasyn) is a selective deubiquitinase (DUB: USP5,
UCH-L1, USP9x, USP14, and UCH37) inhibitor and also supresses
Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome)
and activator of transcription (STAT).
P5091(P005091) is a selective and potent
inhibitor of ubiquitin-specific protease 7
(USP7) with EC50 of 4.2 M and the closely
related USP47.
S7132 P5091 (P005091) new
10 mg 50 mg
Size
P22077 is an inhibitor of ubiquitin-specific
protease USP7 with EC50 of 8.6 M, also
inhibits the closely related USP47.
S7133 P22077 new
10 mg 50 mg
Size
LDN-57444 is a reversible, competitive
proteasome inibitor for Uch-L1 with IC50 of
0.88 M, 28-fold selectivity over isoform
Uch-L3.
S7135 LDN-57444 new
25 mg
Size
IU1 is a cell-permeable, reversible and
selective proteasome inhibitor of human
USP14 with IC50 of 4.7 M, 25-fold selective
to IsoT.
IU1 new
10 mg 50 mg
Size
PR-619 is a non-selective, reversible inhibitor
of the deubiquitinylating enzymes (DUBs)
with EC50 of 1-20 M.
PR-619 new
25 mg
Size
F
N
O
N
N H2N NH2
NCS SCN
S O
NO2
S Cl
Cl
S
O
O2N
S
F
F
N
Cl
NOAc
O
Cl
Cl
Page 39
92
Phone:+1-832-582-8158
www.selleckchem.com
DUB / E1 Activating / Autophagy
U
b
i
q
u
i
t
i
n
b-AP15 is a deubiquitinases inhibitor for 19S
proteasomes activity of Ub-AMC cleavage
with IC50 of 2.1 M.
S4920 b-AP15 new
5 mg 25 mg
Size
NSC 632839 is not only a DUB inhibitor, but
also a deSUMOylase inhibitor, it inhibits
USP2, USP7, and SENP2 with IC50 of 45 M,
37 M, and 9.8 M, respectively.
S4922 NSC 632839 new
10 mg 50 mg
Size
TCID is a DUB inhibitor for ubiquitin
C-terminal hydrolase L3 with IC50 of 0.6 M,
125-fold selective to L1.
S7140 TCID new
10 mg 200 mg
Size
S1208 Doxorubicin (Adriamycin)
Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA
topoisomerase II and induces DNA damage and apoptosis.
Licensed by Pfizer
O
O
Cl
Cl
Cl
Cl
O2N N
O
O
NO2
N
H
O
HCl
E1 Activating Inhibitors
MLN4924 is a small molecule inhibitor of
Nedd8 activating enzyme (NAE) with IC50 of 4
nM.
S7109 MLN4924
1 mg
Size
PYR-41 is a cell-permeable pyrazone
compound that is reported to irreversibly
inhibit ubiquitin-activating enzyme E1 activity.
S7129 PYR-41
10mg 25 mg
Size
N
N N
NH
HO
O
S
O
O
NH2
O
O
N
HN
O
O
O
NO2
Autophagy Chemicals
Methazolastone (Temozolomide, Temodar,
Temodal) is a DNA damage inducer.
S1237 Temozolomide
Size
Product Citation:
Clin Cancer Res, 2013, 19(7): 1740-7
N
N
N
N
N
O
NH2
O
Divalproex sodium consists of a compound of
sodium valproate and valproic acid in a 1:1
molar relationship in an enteric coated form.
S1703 Divalproex sodium
O-Na+
O
O
HO
S1047 Vorinostat (SAHA, MK0683)
Vorinostat (suberoylanilide hydroxamic acid, SAHA, Zolinza) is an
HDAC inhibitor with IC50 of ~10 nM.
S1002 ABT-737
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with
EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively; no inhibition
observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
S1049 Y-27632 2HCl
Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of
140 nM, exhibits >200-fold selectivity over other kinases, including
PKC, cAMP-dependent protein kinase, MLCK and PAK.
S1023 Erlotinib HCl (OSI-744)
Erlotinib HCl (OSI-744, CP358774, NSC718781) is an EGFR inhibitor
with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human
c-Src or v-Abl. Phase 3.
S1105 LY294002
LY294002 is the first synthetic molecule known to inhibit PI3K//
with IC50 of 0.5 M/0.57 M/0.97 M, respectively; more stable in
solution than Wortmannin, and also blocks autophagosome
formation.
S1057 Obatoclax mesylate (GX15-070)
Obatoclax (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 M,
can assist in overcoming MCL-1 mediated resistance to apoptosis.
Phase 1/2.
S1039 Rapamycin
(Sirolimus, AY22989, NSC226080)
Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR
inhibitor with IC50 of ~0.1 nM.
Trifluoperazine is a dopamine D2 receptor
S3201 Trifluoperazine 2HCl
Sulfacetamide Sodium is an anti-biotic.
S4081 Sulfacetamide Sodium
Azithromycin (Zithromax) is an antibiotic for
inhibitionof parasitegrowthwithIC50 of 8.4 M.
S1835 Azithromycin Licensed by Pfizer
Licensed by Pfizer
O
N
O
HO
HO
HO O O
N
HO
O
O
OH
O
S
N
F
F
F
N N
2HCl
H2N
S
N-
O O O
Na+
Size
Size
Size
Size
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93
Autophagy
U
b
i
q
u
i
t
i
n
Omeprazole(Prilosec) is a proton pump
inhibitor used in the treatment of dyspepsia.
S1389 Omeprazole
Carbamazepine (Carbatrol) is a sodium
channel blocker with IC50 of 131 M in rat
brain synaptosomes.
S1693 Carbamazepine
S2713 Geldanamycin
Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 M,
specifically disrupts glucocorticoid receptor (GR)/HSP association.
S1714 Gemcitabine
Gemcitabine(Gemzar) belongs to the group of medicines called
antimetabolites.
S2758 Wortmannin
Wortmannin is a PI3K with IC50 of 3 nM, first described PI3K
inhibitors, but little selectivity within the PI3K family. Also blocks
autophagosome formation and potently inhibits DNA-PK/ATM with
IC50 of 16 nM and 150 nM. Phase 4.
S2767 3-Methyladenine
3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and
PI3K with IC50 of 25 M and 60 M; blocks class I PI3K consistently,
whereas suppression of class III PI3K is transient, and also blocks
autophagosome formation.
S2827 Torin 1
Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM;
exhibits 1000-fold selectivity for mTOR than PI3K.
Dexamethasone is an anti-inflammatory and
immunosuppressant.
S1322 Dexamethasone (DHAP)
2013, 32(10): 1316-29 ]
Dexamethasone purchased
fromSelleck
Product Citation:
Oncogene, 2013, 32(10): 1316-29
O
H
HO
F H
OH
O
HO
Metformin hydrochloride(Glucophage) is a
biguanide hypoglycemic agent used in the
treatment of non-insulin-dependent diabetes
mellitus not responding to dietary
modification.
S1950 Metformin HCl
Size
Tamoxifen Citrate is an antagonist of the
estrogen receptor by competitive inhibition of
estrogen binding.
S1972 Tamoxifen Citrate
Product Citation:
Anal Chem Insights, 2012, 7: 31-46
S1150 Paclitaxel
Paclitaxel (Taxol, Onxol, Nov-Onxol) is a microtubule polymer
stabilizer with IC50 of 0.1 pM in human endothelial cells.
S1241 Vincristine
Vincristine is an inhibitor of polymerization of microtubules by binding
to tubulin with IC50 of 32 M.
S1038 PI-103
S1149 Gemcitabine HCl
Gemcitabine Hydrochloride (Gemzar) is a DNA synthesis inhibitor
with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2,
BxPC3 and Capan2 cells, respectively.
Valproic acid sodium salt (Sodium valproate) is an HDAC inhibitor
with IC50 of 0.4 mM and also inhibits GABA-transaminase or succinic
S2218 PP242
PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both
mTOR complexes with >10- and 100-fold selectivity for mTOR than
PI3K or PI3K//, respectively.
S1573 Fasudil (HA-1077) HCl
Fasudil is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK
with Ki of 0.33 M, 1.6 M, 1.6 M, 3.3 M and 36 M, respectively.
S1396 Resveratrol
Resveratrol is a phytoalexin produced naturally by several plants with
anti-cancer, anti-inflammatory, blood-sugar-lowering and other
beneficial cardiovascular effects.
H2N N
H
N
NH NH
HCl
O
N
HO2C CO2H
CO2H
OH
N
H
N
O
S
O
N
O
N
O NH2
Loperamide is an opioid-receptor agonist with
an ED50 of 0.15 mg/kg.
S2480 Loperamide HCl
Size
Size
10 mM/1 mL in DMSO
50 mg
Size
Page 2
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Page 3
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Cl
N
OH
O
N
HCl
Size
Size
94
Phone:+1-832-582-8158
www.selleckchem.com
Autophagy / E2 conjugating / E3 Ligase
U
b
i
q
u
i
t
i
n
S1061 Nutlin-3
Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent
ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90
nM; stabilizes p73 in p53-deficient cells.
S1172 JNJ 26854165 (Serdemetan)
JNJ-26854165 acts as a HDM2 ubiquitin ligase antagonist and also
induces early apoptosis in p53 wild-type cells, inhibits cellular
proliferation followed by delayed apoptosis in the absence of
functional p53. Phase 1.
E3 Ligase Inhibitors
S8000 Tenovin-1
Tenovin-1 protects against MDM2-mediated p53 degradation, which
involves ubiquitination, and acts through inhibition of protein-
deacetylating activities of SirT1 and SirT2.
S1193 Thalidomide
Thalidomide was introduced as a sedative drug, immunomodulatory
agent and also is investigated for treating symptoms of many
cancers. Thalidomide inhibits an E3 ubiquitin ligase which is a
CRBN-DDB1-Cul4A complex.
S2225 TAME
Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
S2678 NSC 207895
S2754 AT406 (SM-406, ARRY-334543)
AT-406 is a potent Smac mimetic and an antagonist of IAP (inhibitor
of apoptosis protein via E3 ubiquitin ligase), binding to XIAP, cIAP1
and cIAP2 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold
higher affinities than the Smac AVPI peptide. Phase 1.
S2781 RITA (NSC 652287)
RITA (NSC 652287) induces both DNA-protein and DNA-DNA
cross-links with no detectable DNA single-strand breaks, and also
inhibits MDM2-p53 interaction by targeting p53.
S3030 Niclosamide
Niclosamide can inhibit DNA replication and inhibit STAT with IC50 of
0.7 M.
Amiodarone HCl is an antiarrhythmic drug for
inhibition of ATP-sensitive potassium channel
with IC50 of 19.1 M.
S1979 Amiodarone HCl
S2775 Nocodazole
Nocodazole is a rapidly-reversible inhibitor of microtubule
polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50
of 0.21 M, 0.53 M and 0.64 M, respectively.
O
O
I
I
O
N
HCl
S2929 Pifithrin- (PFT)
Pifithrin- is an inhibitor of p53, inhibiting p53-dependent
transactivation of p53-responsive genes.
Brefeldin A is a lactone antibiotic and ATPase
inhibitor for protein transport with IC50 of 0.2
M in HCT 116 cells, induces cancer cell
differentiation and apoptosis.
S7046 Brefeldin A
Bay 11-7082 is a NF-B inhibitor, inhibits TNF
-induced IB phosphorylation with IC50 of
10 M.
S2913 BAY 11-7082
E2 conjugating Inhibitor
Size
O
O
H
OH
OH
H
S
O
O
N
Size
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Gamma-secretase / Beta Amyloid / 5-HT Receptor
N
e
u
r
o
n
a
l

S
i
g
n
a
l
i
n
g
DAPT (GSI-IX) is a novel -secretase inhibitor, which inhibits A
production with IC50 of 20 nM in HEK 293 cells.
S2215 DAPT (GSI-IX)
RO4929097 is a secretase inhibitor with IC50 of 4 nM, inhibiting
cellular processing of A40 and Notch with EC50 of 14 nM and 5 nM,
S1575 RO4929097
BMS-708163 is a potent, selective, orally bioavailable -secretase
inhibitor of A40 and A42 with IC50 of 0.3 nM and 0.27 nM,
demonstrating a 193-fold selectivity against Notch. Phase 2.
S1262 BMS-708163 (Avagacestat)
S2660 MK-0752
MK-0752 is a moderately potent -secretase inhibitor, which reduces
A40 production with IC50 of 5 nM. Phase 1/2.
S1528 LY2811376
LY2811376 is the first orally available non-peptidic -secretase
(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease
A secretion with EC50 of 300 nM, demonstrated to have 10-fold
selectivity towards BACE1 over BACE2, and more than 50-fold
inhibition over other aspartic proteases including cathepsin D, pepsin,
or renin. Phase 1.
Beta Amyloid Inhibitors
Neuronal Signaling
Di zoci l pi ne
(-)-Huperzi ne A
Di mebon
ADX-47273
MPEP
LY2140023
GluR agonist
GluR antagonists
Gabapenti n
Val proi c aci d sodi um sal t
Etomi date
Fl umazeni l
Nefi racetam
Gi nkgol i de A
GABA receptor chemicals
Tol terodi ne tartrate
Donepezi l
Gal anthami ne
AChE inhibitors
Bethanechol chl ori de
mAChR agonist
Pancuroni um
Vi nbl asti ne
nAChR inhibitors
mAChR inhibitor
MAPK
Pathway
GPCR
Pathway
Na+
Ca2+
Cl
-
MEK
ERK
Glutamate
mGLuR CB1/2
Glutamute
AMPAK NMDAR
ATP
P2X
GABA
GABAR
ACh
AChR
Cam
Camk
nNOS
G-protein
5-HT Receptor Antagonists &
Agonists
Olanzapine(Zyprexa) is a high affinity for
5-HT2 serotonin and D2 dopamine receptor
antagonist.
S2493 Olanzapine HTR2selective
Fluoxetine HCl is an antidepressant of the
selective serotonin reuptake inhibitor (SSRI)
class.
S1333 Fluoxetine HCl
Venlafaxine is an arylalkanolamine
serotonin-norepinephrine reuptake inhibitor
(SNRI).
S1441 Venlafaxine
Clozapine (Clozaril) is a potent 5-HT1C
receptor antagonist with an IC50 of 110 nM for
5-HT-stimulated phosphoinositide hydrolysis.
S2459 Clozapine HTR1selective
Agomelatine is classified as a
norepinephrine-dopamine disinhibitor (NDDI)
due to its antagonism of the 5-HT2C
receptor.
S1243 Agomelatine HTR2selective
O
NH
O
N
H
N
S
N
N
O
F
F
F
N
H
HCl
OH
N
O
HCl
Sumatriptan succinate is a triptan sulfa drug
containing a sulfonamide group for the
treatment of migraine headaches.
S1432 Sumatriptan Succinate
N
H
N
S
H
N
O O
CO2H
HO2C
Size
Size
Size
Size
Size
Size
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96
Phone:+1-832-582-8158
www.selleckchem.com
5-HT Receptor / COX
N
e
u
r
o
n
a
l

S
i
g
n
a
l
i
n
g
HTR2selective
RS-127445 is a selective 5-HT2B receptor
antagonist with pKi of 9.5 and pIC50 of 10.4,
exhibits >1000-fold selectivity against other
5-HT receptors.
S2698 RS-127445
F
N
N
NH2
HTR2selective
Asenapine inhibits adrenergic receptor (1,
2A, 2B, 2C) with Ki of 0.25-1.2 nM and
also inhibits 5-HT receptor (1A, 1B, 2A, 2B,
2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
S1283 Asenapine
Ketanserin (Vulketan Gel) is specific 5-HT2A
serotonin receptor antagonist with a Ki of 2.5
nM for rat and human 5-HT2A.
S2232 Ketanserin
50 mg 100 mg 500 mg
Size
Dimebon is an antihistamine drug.
S1245 Latrepirdine
5 mg 10 mg 50 mg
Size
Risperidone(Risperdal) is an atypical
antipsychotic used to treat schizophrenia.
S1615 Risperidone
N
N
O
N
O N
F
Tianeptine is a selective serotonin reuptake
enhancer (SSRE) compound used for
treating major depressive episodes.
S1436 Tianeptine sodium
WAY 100635 is a potent and selective
5-HT1A receptor agonist with pIC50 of 8.87,
exhibits >100-fold selectivity against other
5-HT receptor subtypes and major
neurotransmitter receptors.
S2663 WAY-100635 HCl HTR1selective
O
N
N
N
O
N
N
H
N
O
O
N
O
F
O
N
H H
Cl
S N
O
O
NH
O
NaO
Cl
Naratriptan (Amerge) is a triptan agent that is
used for the treatment of migraine
headaches.
S1488 Naratriptan
Dapoxetine hydrochloride is a short-acting
novel selective serotonin reuptake inhibitor.
S1869 Dapoxetine HCl
N
H
N
S
O
O
H
N
HCl
O N
HCl
Paroxetine is an antidepressant drug of the
SSRI type.
S3005 Paroxetine HCl
NH O O
O
HCl
F
Duloxetine is a serotonin-norepinephrine
reuptake inhibitor with Ki of 4.6 nM, used for
treatment of major depressive disorder and
generalized anxiety disorder (GAD).
S2084 Duloxetine HCl
HTR2selective
Blonanserin is a novel atypical antipsychotic
agent with potent dopamine D2 (Ki, 14.8 nM)
and serotonin 5-HT2 (Ki, 3.98 nM) receptors
antagonist properties.
S2112 Blonanserin
20 mg 100 mg
Size
O
H
N
S HCl
N
F
N
N
Celecoxib is a selective COX-2 inhibitor with
IC50 of 40 nM.
S1261 Celecoxib COX-2selective
Ibuprofen (Advil, Dolgesic) is an
anti-inflammatory inhibitor targeting COX-1
and COX-2 with IC50 of 13 M and 370 M,
respectively.
S1638 Ibuprofen
Piroxicam (Feldene) is a non-selective COX
inhibitor with an IC50 of 6 mM.
S1713 Piroxicam
COX Inhibitors
Product Citation:
Blood, 2011, 118(22): 5891-900
Licensed by Pfizer
S
N
N
F
F F
NH2
O
O
OH
O
N N
H
O
N
S
OH
O O
Ketoprofen (Actron) is a non-selective NSAID
with IC50 of 0.5 M and 2.33 M for human
recombinant COX-1 and COX-2, respectively.
S1645 Ketoprofen
Etodolac (Lodine) is a COX inhibitor with an
IC50 of 53.5 nM.
S1328 Etodolac
O
OH
O
H
N
O
O
OH
Size
Size
Size
Size
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO 100 mg 1 g
Size
Size
Size
Size
Size
N
N
N
2HCl
N
H
N
Cl
N
N
98
Phone:+1-832-582-8158
www.selleckchem.com
Adrenergic Receptor / AChR / Histamine Receptor
N
e
u
r
o
n
a
l

S
i
g
n
a
l
i
n
g
Epinephrine bitartrate (D02149,
Adrenalinium) is alpha- and beta-adrenergic
receptor stimulator.
S2521 Epinephrine Bitartrate
HO
HO
OH
H
N
O
HO
OH
OH
O
OH
Bisoprolol is a selective type 1 adrenergic
receptor blocker.
S1206 Bisoprolol 1 selective
O
OH
NH
O
O
OH
OH
O
O
Indacaterol is an ultra-long-acting
-adrenoceptor agonist with pKi of 7.36.
S3083 Indacaterol Maleate
3 selective
Mirabegron is a selective 3-adrenoceptor
agonist with EC50 of 22.4 nM.
S4009 Mirabegron
NH
O
OH
OH
N
H
O
OH
O
OH
S
N
O
N
H
H
N
OH
NH2
Donepezil is a specific and potent AChE
inhibitor for bAChE and hAChE with IC50 of
S2462 Donepezil HCl
10 mg 50 mg
Size
AChE selective
AChR Inhibitors & Chemicals
Pancuronium (Pavulon) is a competitive
acetylcholine antagonist with an IC50 of
5.50.5 nM.
S2497 Pancuronium nAChR selective
S1754 Oxybutynin
Oxybutynin (Ditropan) is an anticholinergic
medication used to relieve urinary and
bladder difficulties.
Acetylcysteine is a pharmaceutical drug and
nutritional supplement used primarily as a
mucolytic agent and in the management of
paracetamol (acetaminophen) overdose.
S1623 Acetylcysteine
mAChR selective
Tolterodine tartrate (Detrol LA) is a tartrate
salt of tolterodine that is a competitive
muscarinic receptor antagonist.
S2550 Tolterodine tartrate mAChR selective Licensed by Pfizer
N
S
O O
Cl
F
N
O
N
H2N
O
CF3
O
O
O
N
HCl
N+ H
O
N+
O
H
H H
O
O
Br -
Br -
O
O
OH
N
OH
N
O
OH
OH
HO
HO
O
Rocuronium is an aminosteroid non-
depolarizing neuromuscular blocker or
muscle relaxant.
S1397 Rocuronium Bromide
mAChR selective
nAChR selective
Fesoterodine fumarate (Toviaz) is an
antimuscarinic agent and is rapidly
de-esterified to its active metabolite
5-hydroxymethyl tolterodine that is a
S2240 Fesoterodine fumarate
Varenicline is a prescription medication used
to treat smoking addiction.
S1440 Varenicline tartrate
5 mg 10 mg
Size
PNU-120596is a positive allosteric modulator
of 7 nAChR with EC50 of 216 nM.
S2629 PNU-120596 nAChR selective
Licensed by Pfizer
O
N
OH
O
OH
HO
O
O
N+
O
H
N
O
HO
H
H H
O
Br-
O O
Cl HN
N
H
O
N O
HO
O
OH
OH
OH
O
NH
N
N
mAChR selective
Tiotropium Bromide hydrate is a
monohydrate of tiotropiumbromide (Spiriva;
Tiova; BA 679BR; tiopropium) that is an
anticholinergic and bronchodilator and a
S2547 Tiotropium Bromide hydrate
(BA 679BR)
mAChR selective
Trospiumchloride (Sanctura) is a competitive
muscarinic cholinergic receptor antagonist.
S2549 Trospium chloride
N+
O
H
H
O
O
S
S
OH
Br -
xH2O
N+
H
H
O
O
OH
Cl -
Histamine H1-receptor selective
Clemastine Fumarate (Clemastine) is a
selective histamine H1 receptor antagonist
with IC50 of 3 nM.
S1847 Clemastine Fumarate
Loratadine is a selective inverse peripheral
histamine H1-receptor agonist with an IC50 of
>32 M.
S1358 Loratadine
Histamine Receptor Antagonists
& Agonists
Cl
O N
HO
OH
O
O
N
N
Cl
O O
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
97
COX / GluR / Adrenergic Receptor
N
e
u
r
o
n
a
l

S
i
g
n
a
l
i
n
g
2011, 6(7): e22235 ]
Selleck
50 mg 5 mg 25 mg
Size
LY404039 is a potent agonist of recombinant
human mGlu2/mGlu3 receptors with Ki of 149
nM/92 nM, shows >100-fold selectivity over
ionotropic glutamate receptors, glutamate
transporters, and other receptors. Phase 3.
S6001 LY404039
Product Citation:
Neuropharm, 2012, 62(7): 2184-91
GluR Chemicals
S1245 Latrepirdine
(-)-Huperzine Ais a potent, highlyspecific and
reversible inhibitor of acetylcholinesterase
(AChE) with Ki of 7 nM, exhibiting 200-fold
more selectivity for G4AChE over G1AChE.
Phase 4.
S2251 (-)-Huperzine A (HupA)
2 mg 5 mg 10 mg
Size
AChE selective
ADX47273 is a potent and specific mGlu5
positive allosteric modulator (PAM) with EC50
of 0.17 M, showing no activity at other mGlu
subtypes.
S2690 ADX-47273 mGlu5 selective
S
O
O
H
H
NH2
H
HOOC
COOH
F
N
O
N
N
O
F
NH2
H
HN
O
Dizocilpine is a potent N-methyl-D-aspartate
(NMDA) receptor antagonist with Ki of 30.5
nM.
S2857 Dizocilpine (MK 801)
HN
Alfuzosin(Uroxatral) is an alpha1 receptor
antagonist used to treat benign prostatic
hyperplasia (BPH).
S1409 Alfuzosin HCl 1 selective
Salbutamol (Albuterol) is a short-acting 2-
adrenergic receptor agonist with an IC50 of
8.93 M.
S2507 Salbutamol Sulfate
250 mg 500 mg
Size
2 selective
1 selective
Doxazosin mesylate is an alpha-1 adrenergic
receptor blocker.
S1324 Doxazosin mesylate
1 selective
Silodosin(Rapaflo) is an 1-adrenoceptor
antagonist with high uroselectivity.
S1613 Silodosin
1 selective
Nebivolol selectively inhibits 1-adrenoceptor
with IC50 of 0.8 nM.
S1549 Nebivolol
Isoprenaline is a non-selective
-adrenoceptor, inhibits the
3
H-inositol
phosphate accumulation with IC50 of 0.08 M.
S2566 Isoprenaline HCl
Adrenergic Receptor Antagonists
& Agonists
Asenapine inhibits adrenergic receptor (1, 2A, 2B, 2C) with Ki of
0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A,
6, 7) with Ki of 0.03-4.0 nM.
S1283 Asenapine
Xylazine HCl is 2 class of adrenergic
receptor agonist.
S2516 Xylazine HCl 2 selective
Product Citation:
Acad Radiol, 2012, 19(3): 358-65
OH
OH
OH
H
N
H2SO4
O
O
F
F
F
N
H
H2N O
N
OH
N
N
H2N
O
O
N N
O
O O
S
O HO
O
OH
HO
H
N
HO
HCl
O
F
H
N O
OH
H H
F
OH
HCl
N
N
NH2
N N
H
O
O
HCl
O
O
Celecoxib
Etodolac
Ibuprofen
Ketoprofen
S1261
S1328
S1638
S1645
+
++
+++
15 M [IC50]
13 M [IC50]
0.5 M [IC50]
++
++
+
++
40 nM [IC50]
1.4 M [IC50]
370 M [IC50]
2.33 M [IC50]
Cat.No. Inhibitor Name Cox-1 Cox-2
Notes:
1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is.
COX-2 selective
Rofecoxib (Vioxx) is a COX-2 inhibitor with
IC50 of 18 nM.
S3043 Rofecoxib
S
O
O
O
O
Size
Size
Size
Size
Size
Size
Size
Size
Size
Page 96
Page 96
H
N
S
N
HCl
100
Phone:+1-832-582-8158
www.selleckchem.com
P-gp / P2 Receptor / OX Receptor / MT Receptor / BACE
N
e
u
r
o
n
a
l

S
i
g
n
a
l
i
n
g
LY335979(Zosuquidar) is a potent modulator
of P-glycoprotein-mediated multi-drug
resistance with Ki of 60 nM. Phase 3.
S1481 Zosuquidar (LY335979) 3HCl
Tariquidar (XR9576) is a potent and selective
noncompetitive inhibitor of P-glycoprotein
with Kd of 5.1nM, reverses drugresistance in
MDR cell Lines. Phase 3.
S8028 Tariquidar
P-gp Chemicals
A novel platelet inhibitor.
S1258 Prasugrel
25 mg 100 mg 300 mg
Size
Clopidogrel (Plavix) is an oral, thienopyridine
class antiplatelet agent.
S1415 Clopidogrel
P2 Receptor Inhibitors
N
O
N
N
OH
F F
HCl HCl HCl
F
O
N
S
O
O
N
N
H
O
O
O
N
H
O
N
O
O
N
Cl
S
O O
HO S OH
O
O
Allopurinol (Zyloprim) is a xanthine oxidase
inhibitor with an IC50 of 7.820.12 M.
S1630 Allopurinol
SB-408124 (Tocris-1963) is a non-peptide
antagonist for OX1 receptor with Ki of 57 nM
and 27 nM in both whole cell and membrane,
respectively, exhibits 50-fold selectivity over
OX2 receptor.
S1545 SB-408124
OX Receptor Chemicals
N
F
F
HN
H
N
N
O
N
N N
H
NH
O
Ramelteon (TAK-375) is a novel melatonin
receptor agonist for human MT1 and MT2
receptors and chick forebrain melatonin
receptors with Ki of 14 pM, 112 pM and 23.1
pM, respectively.
S1259 Ramelteon
MT Receptor Agonist
O
H
N
O
AZD3839is a potent andselective inhibitor of
human BACE1 with Ki of 26.1 nM.
S7118 AZD3839
5 mg 50 mg
Size
BACE Inhibitor
N
F
N
F3C
NH2
N
N
Size
Size
Size
Size
Size
Size
99
Histamine Receptor / Dopamine Receptor / Opioid Receptor / GABA Receptor
N
e
u
r
o
n
a
l

S
i
g
n
a
l
i
n
g
Mianserin is a psychoactive agent of the
tetracyclic antidepressant.
S1382 Mianserin HCl
Ranitidine (Zantac) is a histamine H2-receptor
antagonist with IC50 of 3.31.4 M.
S1801 Ranitidine
S1245 Latrepirdine
N
N
HCl
N
O
S
H
N
NO2
H
N
HCl
Benztropine is a dopamine transporter (DAT)
S3163 Benztropine mesylate
50 mg
Size
N O
S O O
OH
Quetiapine fumarate (Seroquel) is an atypical
antipsychotic used in the treatment of
schizophrenia, bipolar I mania, bipolar II
depression, bipolar I depression.
S1763 Quetiapine fumarate
Dopamine Receptor Chemicals
Amfebutamone (Bupropion) is a selective
norepinephrine-dopamine reuptake inhibitor
withIC50 of 6.5 M and 3.4 M for the reuptake
of dopamineandnorepinephrine, respectively.
S2452 Amfebutamone
Chlorpromazine (Sonazine) is a dopamine and
potassiumchannel inhibitor with IC50 of 6.1 M
and 16 M for nward-rectifying K
+
currents and
time-independent outwardcurrents.
S2456 Chlorpromazine
D2 selective
Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2
dopamine receptor antagonist.
S2493 Olanzapine
S
N N
N
HO OH
O
O
S
N N
N O HO
O OH
Cl
O
H
N
HCl
Amantadine hydrochloride (Symmetrel) is
used to treat or prevent infections of the
respiratory tract caused by a certain virus.
S2451 Amantadine HCl
NH2
HCl
Loperamide is an opioid-receptor agonist with an ED50 of 0.15 mg/kg.
S2480 Loperamide HCl
Opioid Receptor Antagonists
& Agonists
S1139 ADL5859 HCl
ADL5859 HCl is a -opioid receptor agonist
with Ki of 0.8 nM, selectivity against opioid
receptor , , and weak inhibitory activity at
the hERG channel. Phase 2.
Size
Product Citation:
Expert Opin Investig Drugs, 2012, 21(11): 1607-18
OH
O
NH
N O
HCl
J TC-801 is a selective opioid receptor-like1
(ORL1) receptor antagonist with IC50 of 94
nM, weakly inhibits receptors , , and .
S2722 JTC-801
O
HN
N
O
NH2
HCl
Valproic acid sodiumsalt (Sodiumvalproate) is an HDAC inhibitor
with IC50 of 0.4 mM and also inhibits GABA-transaminase or succinic
GABA Receptor Inhibitors
Flumazenil is a benzodiazepine antagonist.
S1332 Flumazenil
Gabapentin Hydrochloride is a GABA
analogue.
S1338 Gabapentin HCl
10 mg 50 mg
Size
Etomidate is a GABAA receptors agonist at
GABAA receptors.
S1329 Etomidate
Licensed by Pfizer
N
N
F
N
O
O
O
OH O
NH2
HCl
N
N
O
O
Gabapentin (Neurontin) is a pharmaceutical
agent, specifically a GABA analogue.
S2133 Gabapentin
25 mg 100 mg
Size
Licensed by Pfizer
OH O
NH2
Size
Size
Size
Size
Size
Size
Size
Size
Size
Page 96
Page 93
Page 95
Page 84
S
N
N
Cl
101
HDAC / NF-B / IB/IKK / NOD1
N
F
-
B
Sodium 4-Aminosalicylate is an antibiotic
used to treat tuberculosis via NF-B inhibition
and free radical scavenging.
S4073 Sodium 4-Aminosalicylate
IKK 16 is a selective IB kinase (IKK) inhibitor
for IKK-2, IKK complex and IKK-1 with IC50 of
40 nM, 70 nM and 200 nM, respectively.
S2882 IKK-16
NF-B
HDAC Inhibitors
NF-B Inhibitors
IB/IKK Inhibitors
QNZ (EVP4593) shows potent inhibitory activity toward both NF-B
activation and TNF- production with IC50 of 11 nM and 7 nM,
respectively.
S4902 QNZ (EVP4593)
SC-514 is an orally active, ATP-competitive
IKK-2 inhibitor with IC50 of 3-12 M, blocks
NF-B-dependent gene expression, does not
inhibit other IKK isoforms or other
serine-threonine and tyrosine kinases.
S4907 SC-514
10 mg 50 mg
Size
TPCA-1 is an inhibitor of IKK-2 with IC50 of
17.9 nM, inhibits NF-B pathway, exhibits
22-fold selectivity over IKK-1.
S2824 TPCA-1 IKK2 selective
IKK2 selective
Bay 11-7082 is a NF-B inhibitor, inhibits TNF-induced IB
phosphorylation with IC50 of 10 M.
S2913 BAY 11-7082
ML130 is a potent and selective inhibitor of
NOD1 with IC50 of 0.56 M, inhibits NF-B
activation, exhibits 36-fold selectivity over
NOD2.
S2863 ML130 (Nodinitib-1)
NOD1 Inhibitor
102
Phone:+1-832-582-8158
www.selleckchem.com
5-HT Receptor / Adrenergic Receptor / Histamine Receptor / Dopamine Receptor /
Opioid Receptor / Hedgehog/Smoothened / OX Receptor / MT Receptor
G
P
C
R

&

G

P
r
o
t
e
i
n
OX Receptor Chemicals
MT Receptor Agonist
GPCR & G Protein
cAMP
PI3K
PTC SMO
MMPs
GPCR
HB-EGF
5HT2B Glutamate ET1 5HT1D Thrombin
EGFR
AKT
AC
i
q s
i
12
SOS
Hedgehog
GRB2
JAK
STAT
PI3K
AKT
MEKs
mTOR
IKKs
NF-B
p70S6K
SHC
RAS
RAF
MEKs
ERK
ERK
ERK
PKA
GLI
CDC42
PAK
p38
RAC
PI3K
SRC
SRC
SRC
RAS
PLC
IP3
AC
GEFs
Rho
ROCK
cAMP
PKA
MEKs
-arrestin
GEFs
DAG
PKC
GEFs
RHO
ROCK
Ca
2+
RAF
MEKs
Transcription factors
Gene expression
Proliferation,survival,invasion,
migration,angiogenesis
Smoothened antagonists
LDE225
PF-5274857
LY2940680
Endothelin receptor antagonists
Bosentan Hydrate
Zi botentan
Si taxentan sodi um
Adenylate cyclase activator
cAMP production inhibitor
Forskol i n
Bupi vacai ne
Pan-5-HT receptor inhibitor
Asenapi ne
Selective 5-HT receptor inhibitors
Ketanseri n(5-HT2)
Fl uoxeti ne(5-HT1)
Ol anzapi ne(5-HT2)
Ri speri done(5-HT2)
Cl ozapi ne (5-HT1)
5-HT Receptor Antagonists &
Agonists
& Agonists
Adrenergic Receptor Antagonists
& Agonists
Hedgehog/Smoothened Inhibitors
& Chemicals
Histamine Receptor Antagonists
& Agonists
Dopamine Receptor Chemicals
-O
Na+
O
HO NH2
HN
N
N
S
O
N
N
S
O
H2N
F
HN
O NH2
S
S
O
H2N
H2N
N
N
NH2
S
O O
Size
Size
Size
Size
Page 46
Page 94
Inflammation Immune Regulation Survival Proliferation Lymphogenesis B Cell Maturation
PI3K
Akt
RIP
MEKK3
PKC8
PI3K
NIK RIPK1
TRADD
IKK
IKK
IKK
PKC
PKC
PLC 2
PLC 2
IKK/
Gsk-3
IB
NF-B2
P50/52
NF-B2
P52
NF-B2
P52
NF-B2
P50
NF-B2
p100
MSK1
HDAC
ATM
RelB
NF-B2
p100
RelB
NF-B2
p100
RelB
IKK
NEMO
PKR
P65/RelA
P65/RelA
P65/RelA
P38
MAPK
Growth factors TNF Ag-MHC Ag
LT, CD40L,
BAFF/BLys
UV
Pan-IKK inhibitor
IKK-16
Selective IB/IKK inhibitors
TPCA-1(IKK2)
IMD 0354(IKK2)
PHA-408(IKK2)
BAY 11-7082(IB)
Pan-HDAC inhibitors
Enti nostat
Selective HDAC inhibitors
CI994(HDAC1)
Vori nostat
Panobi nostat
MC1568(HDAC4)
Roci l i nostat(HDAC6)
PCI-34051(HDAC8)
NF-B inhibitors
QNZ
Ami nosal i cyl ate Sodi um
104
Phone:+1-832-582-8158
www.selleckchem.com
LPA Receptor / CGRP Receptor / PAFR / cAMP / CXCR /
Protease-activated Receptor / Vasopressin Receptor / CaSR
G
P
C
R

&

G

P
r
o
t
e
i
n
NPS 2143 is a novel potent and selective
antagonist of Ca
2+
receptor with IC50 of 43 nM.
S2633 NPS-2143
10 mg 50 mg 200 mg
Size
Plerixafor is a chemokine receptor antagonist
for CXCR4 and CXCL12-mediated
chemotaxis with IC50 of 44 nM and 5.7 nM,
respectively.
S8030 Plerixafor (AMD3100)
2 mg 10 mg 25 mg
Size
WZ811 is a highly potent competitive CXCR4
antagonist with EC50 of 0.3 nM.
S2912 WZ 811
Size
Plerixafor 8HCl (DB06809, Mozobil,
AMD3100) is the hydrochloride of Plerixafor,
a chemokine receptor antagonist for CXCR4
and CXCL12-mediated chemotaxis with IC50
of 44 nM and 5.7 nM, respectively.
S3013 Plerixafor 8HCl (AMD3100 8HCl)
CXCR Antagonists
Vorapaxar (SCH 530348) is a potent and
orally active thrombin receptor (PAR-1)
antagonist with Ki of 8.1 nM.
S8067 Vorapaxar
5 mg 25 mg
Size
Protease-activated Receptor
Antagonist
Size
Tolvaptan (OPC-41061) is a selective,
competitive arginine vasopressin receptor 2
antagonist with an IC50 of 1.28 M for the
inhibition of AVP-induced platelet
aggregation.
S2593 Tolvaptan
Mozavaptan (OPC-31260) is a novel
competitive vasopressin receptor antagonist
for both V1 and V2 receptors with IC50 of 1.2
M and 14 nM, respectively.
S2920 Mozavaptan
10 mg 100 mg
Vasopressin Receptor Antagonists
AMG-073 HCl (Cinacalcet hydrochloride)
represents a newclass of compounds for the
treatment of hyperparathyroidism.
S1260 Cinacalcet HCl
CaSR Chemicals
Size
Bupivacaine hydrochloride (Marcain) is a
more potent cAMP production inhibitor with
an IC50 of 2.3 M.
S2454 Bupivacaine HCl
Forskolin is a ubiquitous activator of
eukaryotic adenylyl cyclase (AC), commonly
used to raise levels of cAMP in the study and
research of cell physiology.
S2449 Forskolin
cAMP Chemicals
MK 3207 is a potent CGRP receptor
antagonist with IC50 and Ki of 0.12 nM and
0.022 nM, highly selective versus human
AM1, AM2, CTR, andAMY3. Phase 2.
S1542 MK3207 HCl
5 mg 50 mg 200 mg
Size
CGRP Receptor Antagonist
Ginkgolide B (BN 52021) is a PAFR
antagonist with IC50 of 3.6 M.
S1343 Ginkgolide B
25 mg 50 mg 500 mg
PAFR Antagonist
Ki16198 is the methyl ester of Ki16425, which
is a LPA antagonist and inhibits LPA1- and
LPA3-induced inositol phosphate production
with Ki of 0.34 M and 0.93 M, respectively,
shows weaker inhibition for LPA2, no activity
at LPA4, LPA5, LPA6.
S2906 Ki16198
NH
N
O
N
H
N
O HN
F F
O
HCl
O
O
O
O
OH
H
HO
O
O H
OH
O
N
HN
NH
NH
N
NH
HN
HN
8HCl
CF3
N
H
HCl
Cl O
H
N
N
OH
N
O N
H
S
O O
O
O
Cl
H
N
O
N
HCl
O
OH
H
OH
O
OH
O
O
HN
NH
N N
N
N NH
NH
HN
NH
HN
HN
O O
H
HN
O
O
H H
H
N
F
Cl
N
O
H
N
O
HO
O
N
N
H
O
N
Size
Size
Size
Size
Size
Size
103
Cannabinoid Receptor / Endothelin Receptor / S1P Receptor / SGLT / LPA Receptor
Zibotentan (ZD4054) is a specific Endothelin
(ET) A antagonist with IC50 of 21 nM,
exhibiting no activity at ETB. Phase 3.
S1456 Zibotentan (ZD4054)
Bosentan is an endothelin (ET) receptors
antagonist for ET-A and ET-B with Ki of 4.7
S3051 Bosentan Hydrate
Sitaxentansodium(TBC-11251) is a selective
endothelin A receptor (ETA) antagonist with
IC50 and Ki of 1.4 nM and 0.43 nM,
respectively, exhibits 7000-fold selectivity
over ETB. Phase 3.
S3034 Sitaxentan sodium
Endothelin Receptor Antagonists
AM-1241 is a selective cannabinoid CB2
receptor agonist with Ki of 3.4 nM, exhibits
82-fold selectivity over CB1 receptor.
S1544 AM-1241
Cannabinoid Receptor Chemicals
CB2 selective
Rimonabant is a selective antagonist of CB1
with IC50 of 13.6 nM and EC50 of 17.3 nM in
hCB1 transfected HEK 293 membrane.
S3021 Rimonabant CB1 selective
AM251 is a cannabinoid CB1 receptor
antagonistwithIC50 of 700nM, binds invivo to
mouse brain CB1 receptor.
S2819 AM251 CB1 selective
Org 27569 is an allosteric modulator of
cannabinoid CB1 receptor, induces a CB1
receptor state that is characterized by
enhanced agonist affinity and decreased
inverse agonist affinity.
S1534 Org 27569
10 mg 50 mg 200 mg
Size
10 mg 50 mg
Size
CB1 selective
GW842166X is a potent and highly selective
agonist of cannabinoidreceptor CB2receptor
with EC50 of 63 nM, shows no significant
activity at CB1 receptor. Phase 2.
S2778 GW842166X CB2 selective
G
P
C
R

&

G

P
r
o
t
e
i
n
PF-543 is a novel Sphingosine kinase 1
(SphK1, SK1) inhibitor with Ki of 3.6 nM.
S7177 PF-543
5 mg
Size
S1P Receptor Chemicals
FTY720 (Fingolimod, Gilenya) is a S1P antagonist with IC50 of 0.033
nM.
BAF312 (Siponimod) is a next-generation
S1P receptor modulator, selective for S1P1
andS1P5receptors withEC50 of 0.39nM and
0.98 nM, respectively.
S7179 BAF312 (Siponimod)
Dapagliflozin is a potent and selective
hSGLT2 inhibitor with EC50 of 1.1 nM,
exhibiting 1200-fold selectivity over hSGLT1.
Phase 3.
S1548 Dapagliflozin
Canagliflozin is a highly potent and selective
SGLT2 inhibitor for hSGLT2 with IC50 of 2.2
nM, exhibits 413-fold selectivity over
hSGLT1. Phase 3.
S2760 Canagliflozin
Empagliflozin (BI-10773) is a potent and
selective SGLT-2inhibitor with IC50 of 3.1nM,
exhibits >300-fold selectivity over SGLT-1, 4,
5 and 6. Phase 3.
S8022 Empagliflozin (BI10773)
SGLT Inhibitors
Ki16425 is a competitive, potent and
reversible antagonist to LPA1, LPA2 and
LPA3 with Ki of 0.34 M, 6.5 M and 0.93 M,
respectively, shows no activityatLPA4, LPA5,
LPA6.
S1315 Ki16425
2 mg 5 mg 10 mg
Size
LPA Receptor Antagonists
N
O
NO2
N
I
N
H
Cl
O
H
N
N
N
S O O
NH
O
N
N N
N O
Cl O
O
HO
HO
OH
HO
O
OH
HO OH
HO S F
Cl
O O
HN
N
O
S
HO
O
N N
O
NH N
Cl
Cl
Cl
N N
O
NH N
I
Cl
Cl
N
N
O
H
N
O
F
F
F
H
N
Cl Cl
O
O
N
N
O
OH
N
N
HN
S
O
O
H2O
S S
O
O
N-
O
O
O
O
N
Cl
Na+
O
N
HO
S
O O
N
O
HO N
O
F F
F
O
Cl O
O
OH
HO OH
OH
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Page 40
106
Phone:+1-832-582-8158
www.selleckchem.com
Estrogen/progestogen Receptor / Androgen Receptor
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Raloxifene is estrogen antagonists, inhibits
human cytosolic aldehyde oxidase-catalyzed
phthalazine oxidation activity with IC50 of 5.7
nM.
S1227 Raloxifene HCl
LY500307 (SERBA-1) is a potent, selective
estrogen receptor agonist with EC50 of 0.66
nM, 32-fold selectivity against estrogen
receptor . Phase 2.
S1598 LY500307
5 mg 50 mg 200 mg
Size
Dienogest is an orally active synthetic
progesterone (or progestin).
S1251 Dienogest
Mifepristone (Mifeprex, RU-486, RU-38486,
Mifegyne) is a remarkably active antagonist
of progesterone receptor and glucocorticoid
receptor with IC50 of 0.2 nM and 2.6 nM,
respectively.
S2606 Mifepristone
Toremifene Citrate (Fareston, Acapodene) is
anoral selective estrogenreceptor modulator
(SERM) which helps oppose the actions of
estrogen in the body.
S1776 Toremifene Citrate
Gestodene is a progestogen hormonal
contraceptive.
S1376 Gestodene
Drospirenone is a synthetic progestin that is
an analog to spironolactone.
S1377 Drospirenone
Clomifene citrate (Serophene) is a selective
estrogen receptor modulator.
S2561 Clomifene citrate
Medroxyprogesterone acetate is a progestin,
a synthetic variant of the human hormone
progesterone and a potent progesterone
receptor agonist.
S2567 Medroxyprogesterone acetate
S
HO
OH
O
N
O
.HCl
O
OH
HO
H H
O
OH
N
H
H
O
OH
N
H
H
Cl
O
N
O
H
H
H
H
OH
O
O
O
H
H
H
H H
H H
Cl
O
N
HO OH
O O
O OH
OH
O
O
H
H H
O
O
Bazedoxifene HCl is a novel, non-steroidal,
indole-based estrogen receptor modulator
(SERM) binding to both ER and ER with
IC50 of 23 nM and 89 nM.
S2128 Bazedoxifene HCl Licensed and Manufactured by Pfizer
N
OH
HO
O N
HCl
Andarine (GTX-007) is a selective
non-steroidal androgenreceptor (AR) agonist
with Ki of 4 nM, tissue-selective for anabolic
organs.
S1140 Andarine
Size
Megestrol Acetate is a synthetic
progesteronal agent with an IC50 of 260 M
for the inhibition of HegG2.
S1304 Megestrol Acetate
ARN-509 is a selective and competitive
androgen receptor inhibitor with IC50 of 16
nM, useful for prostate cancer treatment.
Phase 2.
S2840 ARN-509
5 mg 50 mg 100 mg
Size
Ostarine (GTx-024, MK-2866, Enobosarm,
S-22) is a selective androgen receptor
modulator (SARM) with Ki of 3.8 nM, and is
tissue-selective for anabolic organs. Phase 3.
S1174 MK-2866 (GTx-024)
Size
Product Citation:
Drug Test Anal, 2011, 3(5): 331-6
Androgen Receptor Chemicals
MDV3100 is an androgen-receptor (AR)
antagonist with IC50 of 36 nM.
S1250 MDV3100 (Enzalutamide)
Product Citations:
Int J Cancer, 2012, 131(6): E872-83
Neoplasia, 2012, 14(1): 74-83
2013, 8(1): e53701 ]
MDV3100 purchased from
Selleck
10 mM/1 mL in DMSO
10 mg 50 mg 5 mg
Size
O
H
H
H
O
O
O
S
N N
N
O
F
N
H
O
N
F
F F
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
105
Opioid Receptor / 5-alpha Reductase / Estrogen/progestogen Receptor
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Endocrinology & Hormones
Finasteride is an inhibitor of steroid Type II 5
-reductase.
Finasteride
CGS 21680hydrochloride is anadenosine A2
receptor agonist with Ki of 27 nM, 140-fold
more selective againstA1 receptor.
CGS 21680 HCl
Dutasteride is a 5-alpha-reductase inhibitor.
Dutasteride
5-alpha Reductase Chemicals
P
P
P
P
Growth Factors Estrogen
Estrogen
Estrogen
ER
Estrogen
ER
Estrogen
ER
Estrogen
ER
GPCR
G G G
cAMP
PKA
CREB BCL2
Akt
eNOS
NO
Antiapoptosis
PI3K
Vasodilation
Src
SHC Ras
Raf
MEKKs
IKKs
NF-B
NF-B
MAPKs
JNKs
p38
ERK1/2
ERK1/2
GRB2
SOS
RTKs
Gene
Expression
CREB Sp1 c-J un c-Fos Elk1
PELP1
BRG1
E6AP
Sim3
NCOR
HDACs
BRCA1
RP-A
RTA
REA
p72
TRAP220
P6S
PGC1
SRA
AIB1
SRC1 TIF2
AR
AR
AR
AR
Cyclin D1
SHP
DAX1 RIP140
T
HSP
HSP
DHT
5-Reductase
IL-6R RTK
IGF-1
EGF
Ras
JAK1
STAT3
p300
MEK
PI3K
Src
Akt
cAMP
PKA
BEZ235
LY294002
GDC-0941
BYL719(p110)
GSK2636771(p110)
TGX-221(p110)
AS-252424(p110)
CAL-101(p110)
IPI-145(p110)
Pan-PI3K inhibitors
CCT128930(Akt2)
Pan-Akt inhibitors
MK-2206
GSK690693
GDC-0068
A-674563(Akt1)
Pan-Raf inhibitors
Vemurafeni b
Sorafeni b
PLX-4720
GDC-0879(B-Raf)
GW5074(C-Raf)
5-reductase inhibitors
Dutasteri de
Fi nasteri de
Nol vadex
CGS 21680
Estrogen/progestogen
receptor chemicals
Ful vestrant
Tamoxi fen Ci trate
Evi sta
Toremi fene Ci trate
Mi fepri stone
Di enogest
Androgen receptor chemicals
Ostari ne
Megestrol Acetate
Gal eterone
Andari ne
Dehydroepi androsterone
MDV3100
& Agonists
N
H
O
HN
O
F
F
F F
F
F
H
H
H H
N
H
O
H
HN
O
H
H H
N
N N
N
NH2
O
N
H
O NH
OH
O
HO OH
HCl
Size
Size
Size
S1197
S2153
S1202
Estrogen/progestogen Receptor
Chemicals
Fulvestrant is an estrogen receptor (ER)
S1191 Fulvestrant
Product Citation:
PLoS One, 2011, 6(7): e21112
2011, 6(7): e21112 ]
Fulvestrant purchased from
Selleck
Tamoxifen Citrate is an antagonist of the estrogen receptor by
competitive inhibition of estrogen binding.
S1972 Tamoxifen Citrate
HO
OH
S
O
F
F
F
F
F
H
H
H
10 mM/1 mL in DMSO
100 mg 25 mg
Size
Page 93
108
Phone:+1-832-582-8158
www.selleckchem.com
RAAS / Aromatase / GPR
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Candesartan cilexetil (Atacand) is a specific
nonpeptide Ang II receptor (ATR) antagonist
and the prodrug of candesartan which is an
ATR antagonist with an IC50 of 15 g/kg.
S2037 Candesartan Cilexetil
Clinofibrate inhibits hydroxymethylglutaryl
coenzyme A reductase (HMGCR) with IC50 of
0.47 mM, is a lipid-lowering agent used for
controlling high cholesterol and
triacylglyceride levels in the blood.
S2664 Clinofibrate
O O O O
O
N
N
O
N
N N
NH
Azilsartan Medoxomil is a potent angiotensin
II type 1 (AT1) receptor antagonist, inhibits
the RAAS, exhibits >10,000-fold selectivity
overAT2, usedtotreat hypertension. Phase3.
S3057 Azilsartan Medoxomil
Notes:
1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is.
++
20 nM [IC50]
+++
1.05 nM [IC50]
+++
1.94 nM [IC50]
+++
5 nM [IC50]
+++
1.3 nM [IC50]
+
39.5-116 M [IC50]
++++
0.26 nM [IC50]
Cat.No. Inhibitor Name angiotensin II receptor ACE
S1359
S1506
S1507
S1657
S1793
Losartan
potassium
Perindopril
Erbumine
Irbesartan
Enalaprilat
dihydrate
Ramipril
S1894 Valsartan
S2037 Candesartan
N
N
O
O
O
O NH
N
O
O
O
O
Letrozole is a third generation inhibitor of
aromatase with IC50 of 0.07-20 nM.
S1235 Letrozole
Aromatase Inhibitors
Product Citation:
Endocrinology, 2013, 154(7): 2296-307
Anastrozole inhibits the enzyme aromatase.
S1188 Anastrozole
Formestane is a second generation selective
aromatase inhibitor with an IC50 of 80 nM.
S2208 Formestane
GSK-1292263 is a novel GPR119 agonist,
showing potential for the treatment of type 2
diabetes. Phase 2.
S2149 GSK1292263
GW9508 is a potent and selective agonist for
FFA1 (GPR40) with pEC50 of 7.32, 100-fold
selective against GPR120, stimulates insulin
secretion in a glucose-sensitive manner.
S8014 GW9508
TAK-875 is a selective GPR40 agonist with
EC50 of 14 nM, 400-fold more potent than
oleic acid.
S2637 TAK-875
GPR Agonists
Exemestane is an aromatase inhibitor,
inhibits human placental and rat ovarian
aromatase with IC50 of 30 nM and 40 nM,
respectively.
S1196 Exemestane
Product Citation:
Drug Metab Dispos, 2012, 40(7): 1268-78
Licensed by Pfizer
Aminoglutethimide (AMG, Cytadren) is an
aromatase inhibitor with IC50 of 10 M.
S1672 Aminoglutethimide
O
OH
O
H
H H
NH2 HN
O
O
N
H
O
O
OH
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
107
Androgen Receptor / RAAS
E
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Flutamide (Eulexin) is an oral nonsteroidal
antiandrogen agent primarily used to treat
prostate cancer.
S1908 Flutamide
Bicalutamide (Casodex, Cosudex, Calutide,
Kalumid) is an androgen receptor (AR)
antagonist with IC50 of 0.16 M.
S1190 Bicalutamide
RAAS Chemicals
Cyproterone acetate is an androgen receptor
(AR) antagonist withIC50 of 7.1nM, as well as
a weak progesterone receptor agonist with
weak pro-gestational and glucocorticoid
activity.
S2042 Cyproterone acetate
Galeterone (TOK-001, VN/124-1) is a
selective CYP17 inhibitor and androgen
receptor (AR) antagonist with IC50 of 300 nM
and 384 nM, respectively, and is a potent
inhibitor of human prostate tumor growth.
Phase 2.
S2803 Galeterone
Dehydroepiandrosterone (DHEA) is a
19-carbon endogenous natural steroid
hormone.
S2604 Dehydroepiandrosterone (DHEA)
10mg
Size
Rosuvastatin calcium is a competitive
inhibitor of HMG-CoA reductase with IC50 of
11 nM.
S2169 Rosuvastatin Calcium
Aliskiren hemifumarate is a direct renin
S2199 Aliskiren hemifumarate
Candesartan is an angiotensin II receptor
S1578 Candesartan
HO
N
N
HO
H
O
H H
Enalaprilat is an angiotensin-converting
enzyme (ACE) inhibitor with IC50 of 1.94 nM.
S1657 Enalaprilat dihydrate
Losartan is an angiotensin II receptor
antagonist, competes with the binding of
angiotensin II to AT1 receptors with IC50 of 20
nM.
S1359 Losartan potassium (DuP 753)
KN
N N
N
N
N
Cl
HO
HO O
N
H
N
O
O
OH
2H2O
Irbesartan(Avapro, SR-47436, BMS-186295)
is a highly potent and specific angiotensin II
type 1 (AT1) receptor antagonist with IC50 of
1.3 nM.
S1507 Irbesartan
10 mg 50 mg
Size
Valsartan (Diovan) is an angiotensin II
receptor antagonist with IC50 of ranging from
39.5 to 116 M.
S1894 Valsartan
Perindopril Erbumine (Aceon) is a potentACE
S1506 Perindopril Erbumine
50 mg
Size
Telmisartan (Micardis) is an angiotensin II
receptor antagonist (ARB) used in the
management of hypertension.
S1738 Telmisartan
Ramipril (Altace) is anangiotensin-converting
enzyme (ACE) inhibitor with IC50 of 5 nM.
S1793 Ramipril
Benazepril is a medication used to treat high
blood pressure.
S1284 Benazepril HCl
Olmesartan medoxomil (Benicar) is a
compound which is hydrolyzed to olmesartan
that is a selective AT1 subtype angiotensin II
receptor antagonist.
S1604 Olmesartan Medoxomil
N
N HN
N
N
O
O OH
H
O O
N
H
N
O
H
H
OH
O
H2N
HO
O
N
N
N N
O
O
H
N
N
O
HO
O
N
N
OH
O
O
O
O
O
N
NH N
N
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
Size
109
GABA Receptor / P-gp / CalciumChannel
T
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T
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s
p
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s
N
a
+
/H
+

tr
a
n
s
p
o
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te
r
Aldosterone
SAH
Hydrolase
MR/Classical
AR
MR/Classical
AR
Transcription
Factors
Translation
Aldosterone
Aldosterone
MR/Classical
AR
MR/Classical
AR
SRE
mRNA
Transcription
Factors
Membrane
AR
IPYK
PIP5K
Na
+
KRas2A PI3K
N
a
+ C
h
a
n
n
e
l
PIP2
PIP3
SOS
PDK
NEDD4
SGK
Raf
MEK
MAPK
MKP1
IP3
Ca
2+
PKC
HSP
HSP
Ca
2+
Na
+
Ca2+ Channel
Mitochondria
Ca
2+
Ca2+
Ca2+
Ca2+
Ca2+
Ca
2+
Ca2+
TnC
ATP
Contraction
IP3R
SERCA
RyR
MAPK
Pathway
Ca
2+
CaM PDE
CaMK
NFAT-3
MCIP-1
CaMKIV
CREB
HDAC4/5
Transcription
Hypertrophy
Ca
2+
Phospho-
lamban
PKA-C
PKA-R
GDP
Receptor
q

PLC
PIP2
IP3
DAG
PKC
Ca
2+
Ca
2+
CaM
Calci-neurin
PLC
Proton pump inhibitors
Lansoprazol e
Omeprazol e
Esomeprazol e magnesi um
PF 3716556
Sodium channel blockers
Ri l uzol e
Carbamazepi ne
A-803467
Lamotri gi ne
Sodium channel stabilizer
Phenytoi n sodi um
Calcium channel blockers
Aml odi pi ne besyl ate
Ranol azi ne
Fel odi pi ne
Mani di pi ne
Ci l ni di pi ne
Laci di pi ne
Transmembrane Transporters
Ranolazine (Ranexa), is an antianginal
medication.
S1425 Ranolazine 2HCl
Manidipine 2HCl is a HCl salt form of
Manidipine, which is a calcium channel
blocker with IC50 of 2.6 nM, used clinically as
an antihypertensive. Phase 4.
S2482 Manidipine 2HCl
Felodipine (Plendil) is a selective L-type Ca
2+
channel blocker with IC50 of 0.15 nM.
S1885 Felodipine
Isradipine (Dynacirc) is a calcium channel
blocker with IC50 of 348 M.
S1662 Isradipine
Manidipine (Manyper) is a lipophilic,
third-generation, highly vasoselective
dihydropyridine calcium antagonist with IC50
of 2.6 nM.
S2481 Manidipine
Amlodipine (Norvasc) is a long-actingcalcium
channel blocker with an IC50 of 1.9 nM.
S1813 Amlodipine besylate
Cilnidipine is a calciumchannel blocker.
S1293 Cilnidipine
Calcium Channel Chemicals
GABA Receptor Inhibitors
P-gp Chemicals
HN
O
O
O
H2N
O O
Cl
S
HO
O
O
NO2
H
N
O
O
O
O
O
N
H
O
O
Cl
O
O
Cl
N
O
N
N
H
O
O
O
O
N+
-O
O
N
H
O
O
O
O
N
N
HN
O
N
N
OH
O
O
2HCl
Size
Size
Size
Size
Size
Size
Size
110
Phone:+1-832-582-8158
www.selleckchem.com
SodiumChannel / ATPase / PotassiumChannel
T
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a
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T
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r
s
Riluzole (Rilutek) is a drug used to treat
amyotrophic lateral sclerosis.
S1614 Riluzole
Rufinamide, a triazole derivative, is an
anticonvulsant medication.
S1256 Rufinamide
Size
10 mg 25 mg 100 mg
Sodium Channel Chemicals
Carbamazepine (Carbatrol) is a sodiumchannel blocker with IC50 of
131 M in rat brain synaptosomes.
S1693 Carbamazepine
F
F
N
N N
O
NH2
Phenytoin sodium (Dilantin) is an inactive
voltage-gated sodiumchannel stabilizer.
S2524 Phenytoin sodium
HN
N
ONa
O
Ibutilide is a Class III antiarrhythmic agent
that is indicatedfor acute cardioconversionof
atrial fibrillation and atrial flutter of a recent
onset to sinus rhythm by induction of slow
inward sodiumcurrent, which prolongs action
potential and refractory period of myocardial
cells.
S2118 Ibutilide Fumarate Licensed by Pfizer
H
N S
O
O
N
OH
HO
O
O
OH
H
N S
O
O
N
OH
Omecamtivmecarbil (CK-1827452) is a
specific cardiac myosinactivator anda clinical
drug for left ventricular systolic heart failure.
Phase 2.
S2623 Omecamtiv mecarbil (CK-1827452)
Size
5 mg 50 mg 200 mg
OligomycinA is an inhibitor of ATP synthase;
it is used to prevent state 3 (phosphorylating)
respiration in oxidative phosphorylation
research.
S1478 Oligomycin A
ATPase Chemicals
O
O
OH
O
O
OH
HO
H O
OH
HO
O
H
Milrinone(Primacor) is a potent and selective
phosphodiesterase 3 inhibitor with IC50 of
0.42 M for the inhibition of FIII PDE.
S2484 Milrinone
N
N
H
O
N
Sodium orthovanadate is an alkaline
phosphatase and (Na,K)-ATPase inhibitor
with IC50 of 10 M.
S2000 Sodium orthovanadate
Size
100 mg
Repaglinide is for the treatment of type II
diabetes.
S1426 Repaglinide
Potassium Channel Chemicals
PF 3716556 is a potent and selective P-CAB
(potassium-competitive acid blocker), with
pIC50 of 6.026 and 7.095 for the inhibition of
porcine H
+
/K
+
, ATPase activity in ion-leaky
and ion-tight assay, respectively, inhibits
gastric acid secretion, displays no activity at
Na
+
/K
+
-ATPase.
S2222 PF 3716556
Size
10 mg 50 mg
Brefeldin A is a lactone antibiotic and ATPase inhibitor for protein
transport with IC50 of 0.2 M in HCT 116 cells, induces cancer cell
differentiation and apoptosis.
S7046 Brefeldin A
(-)-Blebbistatin is a cell-permeable inhibitor
for non muscle myosin II ATPase with IC50 of
2 M, does not inhibit myosin light chain
kinase, inhibits contraction of the cleavage
furrowwithoutdisruptingmitosis or contractile
ring assembly.
S7099 (-)-Blebbistatin
N N
OH
O
O
HO
O
H
N
O
N
Amiodarone HCl is an antiarrhythmic drug for inhibition of
ATP-sensitive potassiumchannel with IC50 of 19.1 M.
S1979 Amiodarone HCl
Nicorandil(Ikorel) is a potassium channel
activator.
S1971 Nicorandil
Nateglinide(Starlix) is an insulin secretagog
agent that lowers blood glucose levels by
stimulating insulin secretion from the
pancreas.
S2489 Nateglinide
N
O
N
H
O
N+O-
O
H
N
O
O HO
Size
Size
Size
Size
Size
Size
Size
Size
Size
Page 93
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111
PotassiumChannel / Proton Pump / CFTR
T
r
a
n
s
m
e
m
b
r
a
n
e

T
r
a
n
s
p
o
r
t
e
r
s
Chlorpromazine (Sonazine) is a dopamine and potassiumchannel
inhibitor withIC50 of 6.1 M and 16 M for nward-rectifying K
+
currents
and time-independent outward currents.
S2456 Chlorpromazine
TRAM-34is a selective andpotent inhibitor of
the intermediate-conductance Ca
2+
-activated
K
+
channel (IKCa1, KCa3.1) withKd of 20nM,
200- to 1500-fold selective over other ion
channels, and does not block cytochrome
P450.
S1160 TRAM-34
Size
5 mg 25 mg
Lansoprazole is a proton-pumpinhibitor (PPI)
which prevents the stomach fromproducing
gastric acid.
S1354 Lansoprazole
Proton Pump Inhibitors
Omeprazole (Prilosec) is a proton pump inhibitor used in the
treatment of dyspepsia.
S1389 Omeprazole
PF 3716556 is a potent and selective P-CAB (potassium-competitive
acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of
porcine H
+
/K
+
, ATPase activity in ion-leaky and ion-tight assay,
respectively, inhibits gastric acid secretion, displays no activity at
Na
+
/K
+
-ATPase.
S2222 PF 3716556 Licensed and Manufactured by Pfizer
N
H
N
S
O N
O
F
F F
CFTR Chemicals
Ivacaftor (VX-770, Kalydeco) is a potentiator
of CFTR targeting G551D-CFTR and
F508del-CFTR with EC50 of 100 nM and 25
nM, respectively.
S1144 Ivacaftor (VX-770)
VX-661 is a second F508del CFTR corrector
and is believed to help CFTR protein reach
the cell surface. Phase 2.
S7059 VX-661
Data from[ Hum Mutat,
2012, 33(6): 973-80 ]
Ataluren purchased from
Selleck
10 mM/1 mL in DMSO
100 mg 50 mg 10 mg
Size
PTC124 (Ataluren) selectively induces
ribosomal read-through of premature but not
normal termination codons, with EC50 of 0.1
M, may provide treatment for genetic
disorders caused by nonsense mutations
(e.g. CF caused by CFTR nonsense
mutation). Phase 3.
S6003 Ataluren (PTC124)
Product Citation:
Hum Mutat, 2012, 33(6): 973-80
2012, 287(52): 43630-8 ]
Selleck
10 mM/1 mL in DMSO
50 mg 200 mg 5 mg
Size
VX-809 acts to correct CFTR mutations
common in cystic fibrosis by increasing
mutant CFTR (F508del-CFTR) maturation,
EC50 of 0.1 M. Phase 3.
S1565 VX-809
Product Citation:
J Biol Chem, 2012, 287(52): 43630-8
Product Citation:
Am J Respir Crit Care Med, 2012, 186(7): 694-6
O
OH
N O
N
F
O
O F
F
N
H
O
N OH
O
O
O
F
F
O
NH
N
F
HO
OH
OH
Size
Size
Size
Page 99
Page 93
Page 110
p.W531*/p.G407fs p.Y314*p.E331*
m
R
N
A
le
v
e
ls
(%
)
Notreatment DMSO Gentamicin300g/mL
Gentamicin500g/mL G41850g/mL G41875g/mL
PTC 10M PTC 20M
5
10
15
20
25
30
35
40
45
50
P1 P2 P3 P4
p.R313*/p.R313* p.S562*/p.S562*
0
M
e
t
a
b
o
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i
s
m
112
Phone:+1-832-582-8158
www.selleckchem.com
HSP(e.g.HSP90) / PPAR
MYD88
J AK-STAT
NF-B
IRAK
pSTAT3
p38-
MAPK
IRS1
SOCS3
PI3K
pAkt
PKC/
PP2A
SIRT1
PDH
ACC
AMPK
CAMKK
CDK5 PPAR
SIRT1 PGC-1 PPAR
pCREB
PPAR
C/EBP
C/EBP
LKB1
TCS1/2
mTORC
J NK
TRAF6
IKK NEMO
PKA
Lipolysis
Lipogenesis
Adiponectin
HIF-1
destabilization
Glycerol
neogenesis
Glut4
translocation
Autophagy
BCAA
catabolism
Adipocyte-specific
gene expression
NF-B-mediated
inflammation
Chaperones regulating
adiponectin secretion
Mitochondrial
biogenesis
program
FA
oxidation
OXPHOS
Normal
oxidative
stress
Insulin
signaling
LPL
HSL
MGL
ATGL
CGI-58
TNF
F
A
T
P
FAs
FAs
CD36
ATP
Glucose
O2
(normoxia)
Caveolins
Lipoprotein
particles
SNS signaling
3AR
Glucose
TNFR
Insulin R
M2 MACROPHAGE
IL-10
(anti-inflammatory)
Insulin
Adipo R
S1P
S1PR
S1P
Ca
2+
BCAAs
GOLGI
Malonyl-
CoA
Acetyl-
CoA
Glucose
Perilipins
Pyruvate
LIPID
DROPLET
CPT1
[AMP:ATP]
UCP1
Citrate
ROS
ROS
CYTOSOL
NUCLEUS
NAD
+
/NADH
Acetyl-
CoA
MITOCHONDRIA
(normal function)
Ceramide
Ceramide
FGF21
IL-6
Saturated
FAs
TLR4
FGFRs/
Klotho
Adiponectin
release
(to other
organs)
G
lu
t4
S
L
C
6
g
p
1
3
0
IL
-
6
R
g
p
1
3
0
AC Gs
cAMP
TG
FSP27
CIDEA
Size
Metabolism
HSP (e.g.HSP90) Inhibitors
PPAR Chemicals
Rosiglitazone maleate (Avandia) is an
anti-diabetic agent in the thiazolidinedione
class of agents.
S2505 Rosiglitazone maleate
PPAR/ selective
GW501516 is a potent and highly selective
PPAR/ agonist, with IC50 of 1 nM, with
1000-fold selectivity over hPPAR and
hPPAR. Phase 4.
S1473 GW501516
5 mg 25 mg 100 mg
Size
O
HO
O
S
S
N
F
F
F
Ciprofibrate is a peroxisome proliferator-
activated receptor agonist.
S2665 Ciprofibrate
PPAR selective
GW9662 is a selective PPAR antagonist for
PPAR with IC50 of 3.3 nM, with at least 100-
to 1000-fold functional selectivity in cells with
PPAR versus PPAR and PPAR.
S2915 GW9662
O
OH
O
Cl
Cl
HN
O
Cl
N+ O
O-
PPAR selective
T0070907 is a potent and selective PPAR
inhibitor with IC50 of 1 nM, with a >800-fold
selectivity over PPAR and PPAR.
S2871 T0070907
O
NH N
N+
O
O-
Cl
Size
Size
Size
113
P450 (e.g. CYP17) / PDE
M
e
t
a
b
o
l
i
s
m
Size
MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36
nM.
S1250 MDV3100 (Enzalutamide)
Abiraterone (CB-7598) is a potent CYP17
Product Citation:
Chem Res Toxicol, 2012, 25(8): 1720-31
S1123 Abiraterone
5 mg 25 mg 100 mg
Size
Bicalutamide (Casodex, Cosudex, Calutide, Kalumid) is anandrogen
receptor (AR) antagonist with IC50 of 0.16 M.
S1190 Bicalutamide
Voriconazole (VFEND) is a triazole antifungal
medication that is generally used to treat
serious, invasive fungal infections.
S1442 Voriconazole
Abiraterone acetate (CB7630, CB 7630,
CB-7630) is an acetate salt form of
Abiraterone which is a steroidal cytochrome
CYP17 inhibitor with IC50 of 72 nM.
S2246 Abiraterone Acetate
5 mg 25 mg 100 mg
Size
Avasimibe inhibits ACAT with IC50 of 3.3 M,
also inhibits human P450 isoenzymes
CYP2C9, CYP1A2andCYP2C19withIC50 of
2.9 M, 13.9 M and 26.5 M.
S2187 Avasimibe
P450 (e.g. CYP17) Inhibitors
Ketoconazole inhibits cyclosporine oxidase
andtestosterone 6beta-hydroxylase withIC50
of 0.19 mM and 0.22 mM, respectively.
S1353 Ketoconazole
TAK-700 (Orteronel) is a potent and highly
selective human 17,20-lyase inhibitor with
IC50 of 38 nM, exhibits >1000-fold selectivity
over other CYPs (e.g. 11-hydroxylase and
CYP3A4). Phase 3.
S1195 TAK-700 (Orteronel)
5 mg 10 mg 50 mg
Size
Size
Size
Clarithromycin (Biaxin, Klacid) is a macrolide
antibiotic and a CYP3A4 substrate inhibitor.
S2555 Clarithromycin
O
O
OH
HO O
O
O
O
N
O
O
OH
O
HO
Size
TH-302 is selective hypoxia-activated
prodrug targeting hypoxic regions of solid
tumors with IC50 of 19 nM, demonstrates
270-foldenhancedcytotoxicityunder hypoxia
versus their potency under aerobic
conditions, stable to cytochrome P450
metabolism.
S2757 TH-302
5 mg 50 mg 200 mg
Size
Galeterone (TOK-001, VN/124-1) is a selective CYP17 inhibitor and
androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM,
respectively, andis a potentinhibitor of humanprostate tumor growth.
Phase 2.
S2803 Galeterone
CYP3Aselective
Cobicistat (GS-9350) is a potent and
selective inhibitor of CYP3A with IC50 of
30-285 nM.
S2900 Cobicistat (GS-9350)
5 mg 10 mg 200 mg
Size
CYP3A4selective
PF-4981517is a potentandselective inhibitor
of CYP3A4 (P450) with IC50 of 0.03 M,
exhibits >500-fold selectivity over CYP3A5
and CYP3A7.
S2921 PF-4981517 Licensed and Manufactured by Pfizer
Cyproterone acetate is an androgen receptor (AR) antagonist with
IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with
weak pro-gestational and glucocorticoid activity.
S2042 Cyproterone acetate
N N
H
O H
N
O
S
N
N
H
O
O
N
S
N
O
N
N
N
N
N
N
N
N
Size
PDE Inhibitors
PDE4selective
Roflumilast (Daxas) is a selective inhibitor of
PDE4 with IC50 of 0.2-4.3 nM.
S2131 Roflumilast
Product Citation:
J Mass Spectrom, 2012, 47(12): 1612-9
Data from[ J Mass
Spectrom, 2012, 47(12):
1612-9 ]
Roflumilast purchased from
Selleck
N
Cl
Cl
N
H
O
O
O F
F
10 mM/1 mL in DMSO
50 mg 5 mg 25 mg
Size
Page 107
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RFM
IC-87114
RFN
0
200
400
600
800
1000
1200
1400
M
e
a
n
P
la
s
m
a
C
o
n
c
e
n
tra
io
n
(n
g
.m
L
-1)
Time (h)
0 3 6 9 12 15 18 21 24
M
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114
Phone:+1-832-582-8158
www.selleckchem.com
PDE
+++
++++
1.8 nM [IC50]
0.7 nM [IC50]
PDE5 PDE3 PDE10
+
+
0.2 M [IC50]
0.32 M [IC50]
++++ 0.37 nM [IC50]
Cilostazol
Cilomilast
Tadalafil
Pimobendan
Roflumilast
S1294
S1455
S1512
S1550
S2131
S2515
+
++++
100 nM [IC50]
0.8 nM [IC50]
+ 74 nM [IC50]
+ 180 nM [IC50]
Cat.No. Inhibitor Name PDE4 PDE1
Vardenafil
Hydrochloride
Trihydrate
S2620
S2687
GSK256066
PF-2545920
S8034 Apremilast
++++ 3.2 pM [IC50]
PDE5 PDE3 PDE10
Size
PDE4selective
PDE4selective
S2620
S1430
GSK256066
GSK256066 is a selective PDE4B (equal
affinity to isoforms A-D) inhibitor with IC50 of
3.2 pM, >380,000-fold selectivity versus
PDE1/2/3/5/6 and >2500-fold selectivity
against PDE4B versus PDE7.
Rolipram
Rolipram is a PDE4-inhibitor and an
anti-inflammatory agent.
PDE10selective
5 mg 50 mg
Size
S2687
200 mg
PF-2545920
PF-2545920 is a potent and selective
PDE10A inhibitor with IC50 of 0.37 nM, with
>1000-fold selectivity over the PDE.
PDE3selective
Product Citation:
J Mass Spectrom, 2012, 47(12): 1612-9
Data independently
Pimobendan purchased
fromSelleck
S1550 Pimobendan
Pimobendan is a selective inhibitor of PDE3
with IC50 of 0.32 M.
S2515 Vardenafil HCl Trihydrate
Vardenafil Hydrochloride Trihydrate (Vivanza)
is a newtype PDE inhibitor withIC50 of 0.7nM
and 180 nM for PDE5 and PDE1,
respectively.
PDE5selective S1512 Tadalafil
Tadalafil is a PDE-5 inhibitor with IC50 of 1.8
nM.
PDE4selective
Cilomilast (SB-207499) is a potent PDE4
inhibitor with IC50 of about 110 nM, has
anti-inflammatory activity and low central
nervous systemactivity.
S1455 Cilomilast
Product Citation:
Biochimie, 2012, 94(11): 2360-5
Data from[ Biochimie,
2012, 94(11): 2360-5 ]
Cilomilast purchased from
Selleck
S1431 Sildenafil citrate
Sildenafil citrate is an agent used to treat
erectile dysfunction and pulmonary arterial
hypertension (PAH).
S
N
O
O
N
O
N
HN
O
N
N
OH
OH
OH
O
HO
O
O
N
N
S
O O
O
N
N
HN
O
N
HCl 3H2O
N
N N
H
O
O
H
O
O
PDE3selective S1294 Cilostazol
Cilostazol is a potent cyclic nucleotide
phosphodiesterase type 3 (PDE3) inhibitor
with IC50 of 0.2 M and inhibitor of adenosine
uptake.
N
H
O
O
N N
N
N
PDE4selective
Apremilast (CC-10004) is a potent and orally
active PDE4 and TNF- inhibitor with IC50 of
74 nM and 77 nM, respectively.
S8034 Apremilast (CC-10004)
NH
O
N
O
O
S
O
O
O
O
Size
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO
50 mg 200 mg 5 mg
Size
10 mM/1 mL in DMSO
50mg 200mg 5mg
Size
Runx2
Osterix
Osteocalcin
p<0.05
p<0.05
p<0.05
G
e
n
e
e
x
p
re
s
s
io
n
re
la
tiv
e
to
c
o
n
tro
l
0
1
2
3
4
5
6
7
BMP-2 (ng/mL)
PDE4 I (M)
Medium
DMSO (%)
OCN level
without DMSO
Osx level
without DMSO
Runx2 level
without DMSO
-
-
-
-
- - 300
40 C
OM SM SM SM SM SM
40 C 40 R 40 R
300 300
115
Hydroxylase / Factor Xa / DHFR / Aminopeptidase / Dehydrogenase
M
e
t
a
b
o
l
i
s
m
Size
Size
Size
Size
Size
Size
Factor Xa Inhibitors
Rivaroxaban (Xarelto, BAY 59-7939) is a
direct inhibitor of Factor Xa withKi andIC50 of
S3002 Rivaroxaban
Apixaban is a highly selective, reversible
inhibitor of Factor Xa with Ki of 0.08 nM and
0.17 nM in human and rabbit, respectively.
S1593 Apixaban
Hydroxylase Inhibitors
It was developed to be used as a
chemotherapymedicationfor the treatment of
brain cancer, pancreatic cancer and more.
S1379 Isotretinoin
Nepicastat hydrochloride is a potent and
selective inhibitor of both bovine and human
dopamine--hydroxylase with IC50 of 8.5 nM
and 9 nM, with negligible affinity for twelve
other enzymes and thirteen neurotransmitter
receptors. Phase 2.
S2695 Nepicastat (SYN-117) HCl
5 mg 50 mg 200 mg
Size
O HO
DHFR Inhibitors
Pemetrexeddisodium(Alimta) is a novel antifolate andantimetabolite
for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM,
respectively.
S1135 Pemetrexed
Abitrexate (Methotrexate) is anantimetabolite
and antifolate agent with antineoplastic and
immunosuppressant activities.
S1210 Methotrexate
Pralatrexate (Folotyn) is an antifolate, and
structurallya folate analog. Its IC50 is <300nM
in some cell lines.
S1497 Pralatrexate
N
N N
N
H2N
NH2 N
H
O
OH
O OH
O
Dehydrogenase Inhibitors
Aminopeptidase Inhibitor
CHR-2797 is an aminopeptidase inhibitor for
LAP, PuSAandAminopeptidase N withIC50 of
100 nM, 150 nM and 220 nM, respectively,
anddoes not effectivelyinhibit either PILSAP,
MetAP-2, LTA4 hydrolase, or MetAP-2.
Phase 2.
S1522 Tosedostat (CHR2797)
Product Citation:
Science, 2011, 334(6062): 1553-7
S2776 CPI-613
CPI-613, a lipoate analog, inhibits
mitochondrial enzymes pyruvate
dehydrogenase (PDH) and -ketoglutarate
dehydrogenase, disrupts tumor cell
mitochondrial metabolism. Phase 2.
S S OH
O
Mycophenolate mofetil is a non-competitive,
selective and reversible inhibitor of inosine
monophosphate dehydrogenase I/II with IC50
of 39 nM and 27 nM, respectively.
S1501 Mycophenolate Mofetil
Product Citation:
Front Immunol, 2013, 4: 46
Data from[ Front Immunol,
2013, 4: 46 ]
Mycophenolate Mofetil
S1404 Trilostane
Trilostane is an inhibitor of 3 -hydroxysteroid
dehydrogenase used in the treatment of
Cushings syndrome.
Product Citation:
Biol Reprod, 2012, 87(2): 35
Data from[ Biol Reprod,
2012, 87(2): 35 ]
Trilostane purchased from
Selleck
O
O
O OH
O
O
N
O
N
HO
H O
H
OH
H H
Size
10 mM/1 mL in DMSO
25 mg 100 mg 10 mg
Size
10 mM/1 mL in DMSO
100 mg 200 mg 50 mg
Size
M
e
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i
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116
Phone:+1-832-582-8158
www.selleckchem.com
Dehydrogenase / Phospholipase (e.g. PLA) / Carbonic Anhydrase / MAO / FAAH / HMG-CoA Reductase
Size
Size
Size
URB597 (KDS-4103) is a potent, orally
bioavailable FAAH inhibitor with IC50 of 4.6
nM, with no activity on other cannabinoid-
related targets.
S2631 URB597
PF-3845is a potent, selective andirreversible
FAAH inhibitor with Ki of 230 nM, showing
negligible activity against FAAH2.
S2666 PF-3845
FAAH Inhibitors
Size
S1158
200 mg
Size
200 mg
Size
500 mg
Size
200 mg
Size
MK-8245
MK-8245 is a liver-targeting inhibitor of
stearoyl-CoA desaturase (SCD) with IC50 of 1
nM for human SCD1 and 3 nM for both rat
SCD1 and mouse SCD1, with anti-diabetic
and anti-dyslipidemic efficacy. Phase 2.
5 mg 25 mg
Size
S7185 AGI-5198
AGI-5198 is the first highly potent and
selective inhibitor of IDH1 R132H/R132C
mutants with IC50 of 0.07 M/0.16 M.
new
N N
N
N
O
HO
O N
N
O F
Br
N
H
O
N
F
O
N
N
Phospholipase (e.g. PLA) Inhibitor
Carbonic Anhydrase Inhibitors
S1110
Size
Size
Varespladib (LY315920)
LY315920 (Varespladib) is a potent and
selective human non-pancreatic secretory
phospholipase A2(hnsPLA) inhibitor withIC50
of 7 nM. Phase 3.
10 mg 25 mg 100 mg
Size
S1375 Dorzolamide HCl
Dorzolamide HCl is a carbonic anhydrase
inhibitor.
S1438 Topiramate
Topiramate is an anticonvulsant compound.
O
O
O
O
S NH2
O
O
O
O
S2866 U-104
U-104 is a potent carbonic anhydrase (CA)
inhibitor for CA IX and CA XII with Ki of 45.1
nM and 4.5 nM, respectively, very low
inhibition for CA I and CA II.
N
H
N
H
O
F S
NH2
O
O
Rasagiline mesylate is a newMAO-B inhibitor
for the treatment of idiopathic Parkinson's
disease.
S2102 Rasagiline Mesylate
Safinamide Mesylate is mesylate salt of
Safinamide, selectivelyandreversiblyinhibits
MAO-B with IC50 of 98 nM, exhibits 5918-fold
selectivity against MAO-A. Phase 3.
S1472 Safinamide Mesylate
MAO Inhibitors
HN
O S O
OH
Fluvastatin sodium inhibits HMG-CoA
reductase activity with IC50 of 8 nM.
S1909 Fluvastatin Sodium
Lovastatin is an inhibitor of HMG-CoA
reductase with IC50 of 3.4 nM, used for
lowering cholesterol (hypolipidemic agent).
S2061 Lovastatin
HMG-CoA Reductase Inhibitors
N
F
(R) (R) (S) (S)
OH OH
ONa
O
O
H
O
O
O HO
Page 78
117
HMG-CoA Reductase / Transferase / IDO / CETP / Procollagen C Proteinase
M
e
t
a
b
o
l
i
s
m
S2821 RG108
RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM,
does not cause trapping of covalent enzymes.
Size
200 mg
Size
200 mg
Size
Size
200 mg 10 mg 10 mM/1 mL in DMSO 50 mg
Size
Size
Size
Size
Atorvastatin (Lipitor) is an inhibitor of
HMG-CoA reductase used as a cholesterol-
lowering medication that blocks the
production of cholesterol.
S2077 Atorvastatin calcium
Product Citation:
BMC Pharmacol Toxicol, 2013, 14: 15
N O-
O OH OH
O
NH
F
N -O
O OH OH
O
HN
F
Ca2+
Pravastatin sodium is an HMG-CoA
reductase inhibitor against sterol synthesis
with IC50 of 5.6 M.
S3036 Pravastatin sodium
Product Citation:
Clin Cancer Res, 2012, 18(13): 3524-31
Tipifarnib (Zarnestra, R115777) is a potent
and specific farnesyltransferase (FTase)
inhibitor with IC50 of 0.6 nM, its anti-
proliferative effects are most prominent in
H-ras or N-ras mutant cells. Phase 3.
S1453 Tipifarnib
Lonafarnib (SCH 66336) is an orally
bioavailable FPTase inhibitor for H-ras,
K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2
nM and 2.8 nM, respectively. Phase 3.
S2797 Lonafarnib
A922500is aninhibitor for humanandmouse
DGAT-1 with IC50 of 7 nM and 24 nM,
respectively, good selectivity over related
acyltransferases, hERG, and a panel of
anti-targets.
S2674 A 922500
Transferase Inhibitors
5 mg 25 mg 50 mg
Size
S2799 FK866 (APO866)
APO866 effectively inhibits nicotinamide
phosphoribosyltransferase (NMPRTase) with
IC50 of 0.09 nM. Phase 1/2.
HO
H
O
O
CO2Na
HO OH
(R) (R)
N
Br
Cl
Br
N
O
N
NH2
O
O
HN
N
N
O
IDO Inhibitor
NLG919 is a novel and potent
indoleamine-2,3-dioxygenase (IDO) inhibitor
with EC50 of 75 nM.
S7111 NLG919
10 mg 50 mg
Size
CETP Inhibitors
S2925 Evacetrapib (LY2484595)
LY2484595 is a potent and selective inhibitor
of CETP with IC50 of 5.5 nM, elevates HDL
cholesterol without increases in aldosterone
or blood pressure. Phase 3.
N
N
HO
Licensed and Manufactured by Pfizer S2792 Torcetrapib
Torcetrapib (CP-529414) is a CETP inhibitor
with IC50 of 37 nM, elevates HDL-C and
reduces nonHDL-C in plasma. Phase 3.
S2748 Anacetrapib (MK-0859)
Anacetrapib (MK0859) is a potent, selective,
reversible rhCETP and mutant CETP(C13S)
increases HDL-C and decreases LDL-C,
does not increase aldosterone or blood
pressure. Phase 3.
N
F
F
F
O O
N
O
O
F
F
F
F
F
F
Procollagen C Proteinase Inhibitor
10 mg 25 mg
Size
S2224 UK 383367
UK-383367 is a procollagen C-proteinase
inhibitor with IC50 of 44 nM, has excellent
selectivity over MMPs.
N
N
O
H2N
O
N
H
OH
O
Page 85
10 mM/1 mL in DMSO
25 mg 100 mg 5 mg
Size
10 mM/1 mL in DMSO
25 mg 100 mg 5 mg
Size
Proteases
Caspase Inhibitors & Activators
118
Phone:+1-832-582-8158
www.selleckchem.com
Caspase / Gamma-secretase / Proteasome
P
r
o
t
e
a
s
e
s
RING-type
AMP+PPi
ADP+Pi
Proteasome
Proteasome
Proteasome
Cellular stress
ARF
p53
p53
IB
IB
MDM2
Stress
IB kinase
Proteasome
Proteasome
CDC25C
CDKcyclin B
CDKcyclinA
CDKcyclin D
CDKcyclin E
CDC25A, CDC25C
KIP1
Apoptosis
Apoptosis
G0
M
G2
G1
S
WAF1
CDC25B
CDKcyclinA
ATP
ATP
E2
E1
S
S
S
C
Ub
O =
S
C
Ub
O =
N H
C O =
S
26S Proteasome
RP
DUBs
DUBs
C Ub
UbUb
Ub
UbUbUb Ub
Ub
Ub
Ub
Ub
Ub
Ub
Ub
Ub
Ub
UbUbUb
O=
S
C
Ub
O =
HECT-type
Cellular pathways associated with the proteasome
HECT
RING Finger S
NF-B
IB NF-B
p53 Gene
expression
Gene
expression
Pro-survival
pathway
Senescence
NF-B
E3
E3
E2
P
P
MG-132
Bortezomi b
Carfi l zomi b
MLN9708
MLN2238
Del anzomi b
Proteasome inhibitors
b-AP15
WP1130
NSC 632839
IU1
PR-619
DUB inhibitors
JNJ 26854165
Nutl i n-3
Thal i domi de
TAME
NSC-207895
E3 ligase inhibitors
MLN4924
PYR-41
E1 activating inhibitors
BAY 11-7082
E2 conjugating inhibitors
Proteasome Inhibitors
S1013 Bortezomib (PS-341)
Bortezomib is a potent 20S proteasome
inhibitor with Ki of 0.6 nM.
Product Citations:
Cell Stem Cell, 2012, 11(2): 242-52
Hepatology, 2013, 57(2): 625-36
119(11): 2579-89 ]
Bortezomib purchased from
Selleck
S2619 MG-132
MG-132 (ZLLLal) is an inhibitor of
proteasome with IC50 of 100 nM, and also
inhibits calpain with IC50 of 1.2 M.
Product Citations:
EMBO Mol Med, 2013, 5(3): 397-412
Data from[ Plant Physiol,
2012, 160(1): 118-34 ]
MG-132 purchased from
Selleck
ACY-1215 1M
Bortezomib 2.5 nM
- -
- -
+ +
+ +
- -
- -
+ +
+ +
MM.1S RPMI
p-IRE1
p-eIF2
eIF2
GAPDH
XBP-1
IRE1
PERK
-actin
-s
-u
ACY-1215 1M
Bortezomib 2.5 nM
- -
- -
+ +
+ +
- -
- -
+ +
+ +
MM.1S RPMI
p-IRE1
p-eIF2
eIF2
GAPDH
XBP-1
IRE1
PERK
-actin
-s
-u
N
F3C
CF3
N
N N
N
N
H
H H
OH
O
119
Proteasome / HCV Protease
P
r
o
t
e
a
s
e
s
MLN9708 immediately hydrolyzed to
MLN2238, the biologically active form, on
exposure to aqueous solutions or plasma.
MLN2238 inhibits the chymotrypsin-like
proteolytic (5) site of the 20S proteasome
with IC50/Ki of 3.4 nM/0.93 nM, less potent to
1 and little activity to 2. Phase 3.
S2181 MLN9708
Product Citation:
Data from[ Mol Cell
1898-912 ]
Selleck
50 mg 5 mg
Size
S1482 BMS-790052 (Daclatasvir)
BMS-790052 is a highly selective inhibitor of
HCV NS5A with EC50 of 9-50 pM, for a broad
range of HCV replicon genotypes and the
J FH-1 genotype 2a infectious virus in cell
culture. Phase 3.
Product Citations:
J Virol, 2012, 86(16): 8581-91
PLoS One, 2013, 8(6): e65273
Data from[ J Virol, 2012,
86(16): 8581-91 ]
BMS-790052 purchased
fromSelleck
200 mg
10mM/1mLinDMSO
Size
S1183 Danoprevir (ITMN-191)
Danoprevir (ITMN-191) is a peptidomimetic
inhibitor of the NS3/4Aprotease of hepatitis C
virus (HCV) withIC50 of 0.2-3.5nM, inhibition
effect for HCV genotypes 1A/1B/4/5/6 is
~10-fold higher than 2B/3A. Phase 2.
Product Citations:
Curr Protoc Microbiol, 2011, 17: 17.7
PLoS One, 2012, 7(8): e42481
Data from[ Antimicrob
Agents Chemother, 2012,
56(10): 5365-73 ]
Danoprevir purchased from
Selleck
5 mg 2 mg 50 mg
Size
Size
200 mg
Size
200 mg
HCV Protease Inhibitors
S1480 VX-222 (VCH-222)
VX-222 (VCH-222) is a novel, potent and
selective inhibitor of HCV polymerase with
IC50 of 0.94-1.2 M, 15.3-fold less effective for
mutant M423T, and 108-fold less effective for
mutant I482L. Phase 2.
10 mg 5 mg
Size
S1538 Telaprevir (VX-950)
Telaprevir (VX-950) is anHCV NS3-4Aserine
protease inhibitor with IC50 of 0.35 M.
Product Citation:
Antimicrob Agents Chemother, 2012, 56(7): 3888-97
Data from[ Antiviral Res,
2013, 99(1): 6-11 ]
Telaprevir purchased from
Selleck
50 mg
S2853 Carfilzomib (PR-171)
Carfilzomib is an irreversible proteasome
inhibitor with IC50 of <5 nM, displayed
preferential in vitro inhibitory potency against
the ChT-L activity in the 5 subunit, but little
or no effect on the PGPH andT-L activities.
S2180 MLN2238
MLN2238 inhibits the chymotrypsin-like
proteolytic (5) site of the 20S proteasome
with IC50 and Ki of 3.4 nM and 0.93 nM,
respectively, also inhibits the caspase-like (
1) and trypsin-like (2) proteolytic sites, with
IC50 of 31 nM and 3500 nM.
Product Citation:
J Cell Sci, 2012, 125(Pt23): 5733-44
Data from[ J Cell Sci, 2012,
125(Pt23): 5733-44 ]
Selleck
N
O
H
N
O
N
H
O
H
N
O
N
H
O
O
O
S1386 Nafamostat Mesylate
Nafamostat is an anticoagulant.
5 mg 50 mg
Size
S1157
200 mg
Delanzomib (CEP-18770)
CEP-18770 is an orally active inhibitor of the
chymotrypsin-like activity of proteasome with
IC50 of 3.8 nM, with only marginal inhibition of
the tryptic and peptidylglutamyl activities of
the proteosome. Phase 1/2.
5 mg 50 mg
Size
S7049 Oprozomib (ONX 0912)
Oprozomib is an orally bioavailable inhibitor
for CT-L activity of 20S proteasome 5/LMP7
with IC50 of 36 nM/82 nM.
N
H
H
N
O
N
H
O
O
O
O
N
S
O
O
10 mM/1 mL in DMSO
10 mg 200 mg 5 mg
Size
10 mM/1 mL in DMSO
50 mg 200 mg 5 mg
Size
NM-107
A-837093
Telaprevir
gt non-specific
gt non-specific
protease inhibitor
gt1 specific
gt1 RNA replication
gt1 RNA replication
4.06 M
EC50 CC50
6.1 M
0.84 M
16.5 M
>16.7 M
0.59 M
0.20 M
>300 M
>300 M
(GFP analysis)
gt2 HCVcc infection
gt2 HCVcc infection
gt1 RNA replication
gt2 HCVcc infection
(RFP translocation analysis)
NS5B inhibitor
NS5B inhibitor
L
u
c
ife
ra
s
e
a
c
tiv
ity
(%
o
f m
o
c
k
)
0
50
100
150
Danoprevir
-2 -1 0 1 2 3 4
-2 -1 0 1 2 3 4
F
lu
o
re
s
c
e
n
c
e
(%
o
f m
o
c
k
)
0
50
100
150
log10 nM
120
Phone:+1-832-582-8158
www.selleckchem.com
DPP-4 / HIV Protease / MMP
P
r
o
t
e
a
s
e
s
HIV Protease Inhibitors
10mM/1mLinDMSO
100 mg 50 mg 10 mg
Size
S1185 Ritonavir
Ritonavir is an inhibitor of HIV protease used
to treat HIV infection andAIDS.
Product Citation:
Blood, 2012, 119(20): 4686-97
119(20): 4686-97 ]
Ritonavir purchased from
Selleck
S1380 Lopinavir
Lopinavir (ABT-378) is a potent HIV protease
inhibitor with Ki of 1.3 pM.
Product Citation:
Cell, 2012, 148(1-2): 201-12
Lopinavir purchased from
Selleck
Size
100 mg
Size
50 mg
Size
Size
200 mg
Size
Size
Size
Glimepiride is a medium-to-long acting
sulfonylurea anti-diabetic compound with an
ED50 of 182 g/kg.
S1344 Glimepiride
Saxagliptin (BMS-477118, Onglyza) is a
selective and reversible DPP4 inhibitor with
IC50 of 26 nM.
S1540 Saxagliptin
Sitagliptin phosphate (MK-0431) is a potent
inhibitor of DPP-IV with IC50 of 19 nM in
Caco-2 cell extracts.
S4002 Sitagliptin phosphate monohydrate
DPP-4 Inhibitors
S
N
H
N
H
O O
O
N
N
H
O
O
HO
N
O
H
H
N
NH2
Linagliptin is a highly potent, selective DPP-4
S3031 Linagliptin
Vildagliptin (LAF-237) inhibits DPP4 with
IC50 of 2.3 nM.
S3033 Vildagliptin (LAF-237)
N
O NC
H
N
OH
S1457 Atazanavir Sulfate
Atazanavir is anHIV protease inhibitor withKi
of 2.66 nM.
S1639 Amprenavir
Amprenavir is an HIV protease inhibitor with
IC50 of 14.6 ng/mL in wild-type HIV isolates.
5 mg 50 mg
Size
S1620 Darunavir Ethanolate
Darunavir Ethanolate is an HIV protease
inhibitor.
O N
H
O
H
N
O
N
OH
N
H
O
H
N O
O
N
H2SO4
H2N
S
N
O
O
H
N O
O
OH
O
O O
H
H H
O N
H
O H
N
H OH
S
NH2
O O
OH
MMP Inhibitors
1 mg 10 mg
Size
S7155 BB-94
BB-94 is a potent, broad spectrum matrix
metalloprotease (MMP) inhibitor for MMP-1,
MMP-2, MMP-9, MMP-7andMMP-3withIC50
of 3 nM, 4 nM, 4 nM, 6 nM and 20 nM,
respectively.
5 mg 25 mg
Size
S7156 Marimastat
Marimastat (BB-2516) is a broad spectrum
matrix metalloprotease (MMP) inhibitor for
MMP-9, MMP-1, MMP-2, MMP-14 and
MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM
HO
N
H
H
N
O
S
O
S
O
N
H
HO
H
N
O
OH O
N
H
O
NH
10 mM/1 mL in DMSO
200 mg 10 mg 100 mg
Size
A
Z
D
1
1
5
2
A
B
T
-3
4
8
v
e
h
ic
le
pre-treatment
Tx1 Tx2
1 day 6 days 1 day 6 days
N
N
N
N O
O
N
N
N
NH2
121
HCV Protease / HIV Protease / Integrase
M
i
c
r
o
b
i
o
l
o
g
y
Microbiology
S/GSK1349572 (GSK1349572) is a two-
metal-bindingHIV integrase inhibitor withIC50
of 2.7 nM, modest activity against raltegravir-
resistant signature mutants Y143R, Q148K,
N155H, and G140S/Q148H. Phase 3.
S2667 Dolutegravir (GSK1349572)
BMS-707035is a specific HIV-I integrase (IN)
inhibitor with IC50 of 15 nM. Phase 2.
S1366 BMS-707035
MK-2048is a potent inhibitor of integrase (IN)
and INR263K with IC50 of 2.6 nM and 1.5 nM,
respectively.
S2765 MK-2048
Integrase Inhibitors
HCV Protease Inhibitors
HIV Protease Inhibitors
Raltegravir (MK-0518, Isentress) is a potent
integrase (IN) inhibitor for WT and S217Q
PFV IN with IC50 of 90 nM and 40 nM,
respectively.
S2005 Raltegravir (MK-0518)
Product Citations:
Cancer Res, 2012, 72(23): 6200-8
J Virol, 2012, 86(17): 9337-50
Data from[ Virus Res, 2013,
171(1): 121-8 ]
Raltegravir purchased from
Selleck
Fusion
CD4
Co-receptorCCR5 or CXCR4)
Host Cell
Budding
Maturation
ALIX,
ESCRT-I,
ESCRT-III
Attachment
Env
HIV-1
Uncoating
Reverse
transcription
Nuclear
export
Nuclear
import
CRM1
Tat
Rev
Vpu
Vif
RNA Pol II
P-TEFb
Translation
Transcription
Release
AAA
AAA
AAA
AAA
AAA
AAA
AAA
AAA
AAA
5LTR 3LTR
Integration
LEDGF
Accessory viral
proteins
Assembly
Pre-integration
complex
Gag Gag Pol
Gag
Gag
Pol
1
12
10
11 2
o
8
7
+
.
1
-
Translation
-
Tenofovi r
Tenofovi r Di soproxi l Fumarate
Emtri ci tabi ne
Adefovi r Di pi voxi l
Stavudi ne(d4T)
Reverse transcriptase
chemicals
Lopi navi
Atazanavi r sul fate
Ri tonavi r
Darunavi r Ethanol ate
Amprenavi r
HIV protease inhibitors
Ral tegravi r
El vi tegravi r
Dol utegravi r
BMS-707035
MK-2048
Integrase inhibitors
Pl eri xafor 8HCl
WZ 81
Pl eri xafor
SCH527123
CXCR antagonists
Maravi roc
Vi cri vi roc Mal ate
CCR antagonists
Size
Size
Size
10 mM/1 mL in DMSO
10mg 50mg 5mg
Size
122
Phone:+1-832-582-8158
www.selleckchem.com
Integrase / Reverse Transcriptase / CCR
M
i
c
r
o
b
i
o
l
o
g
y
Tenofovir blocks reverse transcriptase and
hepatitis B virus infections.
S1401 Tenofovir
Tenofovir disoproxil fumarate belongs to
nucleotide analogue reverse transcriptase
inhibitors (nRTIs).
S1400 Tenofovir Disoproxil Fumarate
Emtricitabine (Emtriva) is a nucleoside
reverse transcriptase inhibitor with IC50 of
27.7 M.
S1704 Emtricitabine
Adefovir Dipivoxil (Preveon, Hepsera) works
byblockingreverse transcriptase, anenzyme
thatis crucial for the hepatitis B virus (HBV) to
reproduce in the body.
S1718 Adefovir Dipivoxil
Stavudine is a nucleoside analog reverse
transcriptase inhibitor (NARTI) active against
HIV.
S1398 Stavudine (d4T)
Didanosine (Videx, Videx EC) is a reverse
transcriptase inhibitor with IC50 of 0.49 M.
S1702 Didanosine
Reverse Transcriptase Inhibitors
Elvitegravir (EVG, J TK-303/GS-9137) is an
HIV integrase inhibitor for HIV-1 IIIB, HIV-2
EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8
S2001 Elvitegravir (GS-9137, JTK-303)
Product Citations:
Cancer Res, 2012, 72(23): 6200-8
J Virol, 2011, 85(7): 3677-82
2012, 72(23): 6200-8 ]
Elvitegravir purchased from
Selleck
CCR Antagonists
Maraviroc (Selzentry, UK-427857, Celsentri)
is a CCR5 antagonist for MIP-1, MIP-1 and
RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2
nM, respectively.
S2003 Maraviroc
Product Citation:
Cancer Res, 2012, 72(15): 3839-50
Data from[ Mol Cell
Biochem, 2013, 379(1-2):
283-93 ]
Maraviroc purchased from
Selleck
Vicriviroc (SCH-417690, SCH-D) is a potent
CCR5 antagonist with IC50 of 0.91 nM,
showing broad-spectrum activity against
genetically diverse HIV-1 isolates, and also
drug-resistant viruses with RTI, PRI, or MDR
phenotypes. Phase 3.
S2004 Vicriviroc Malate
Product Citations:
Nature, 2013, 493(7430): 51-5
Cancer Res, 2012, 72(15): 3839-50
2012, 72(15): 3839-50 ]
Vicriviroc Malate purchased
fromSelleck
5mg 10mg 50mg
Size
N
N N
N
NH2
O
P O O O
O
O
O
O
O
O
CO2H
HO2C
N N
H2N
F
O
O
S
OH
N
N
N
N
O P O
NH2
O
O
O
O
O
O
O
HO
N
N
H
O
O
O HO
N
N
N
NH
O
Nevirapine (Viramune) is a non-nucleoside
reverse transcriptase inhibitor (NNRTI) used
to treat HIV-1 infection andAIDS.
S1742 Nevirapine
Zidovudine (Retrovir) is a reverse
transcriptase inhibitor.
S2579 Zidovudine
Size
25 mg 100 mg
N
NH
N N
O
HN
N
O
O
O
OH
N3
Dapivirine is a non-nucleoside inhibitor for
HIV reverse transcriptase with IC50 of 24 nM,
inhibits a broad panel of HIV-1 isolates from
different classes, inclucing a wide range of
NNRTI-resistant isolates. Phase 3.
S2914 Dapivirine (TMC120)
N
HN
N
N
HN
Size
Size
Size
Size
Size
Size
Size
Size
10 mM/1 mL in DMSO
50mg 200mg 10mg
Size
10 mM/1 mL in DMSO
100 mg 5 mg 25 mg
Size
123
Cathepsin K / FXR / gp120/CD4 / IL Receptor / Liver X Receptor / Phosphorylase /
PKA / Substance P / Thrombin / TRPV
Odanacatib (MK 0822) is a potent, selective,
and neutral inhibitor of cathepsin K
(human/rabbit) with IC50 of 0.2 nM/1 nM, and
demonstrated high selectivity versus
off-target cathepsin B, L, S. Phase 3.
S1115 Odanacatib (MK 0822)
Size
Size
Size
Size
Size
Size
Size
Size
Size
Cathepsin K Inhibitor
XL335is a potent, selective FXR agonist with
EC50 of 4 nM, highly selective versus other
nuclear receptors, such as LXR, PPAR, ER
and etc. Phase 1.
S2694 XL335
GW 4064 is an agonist of farnesoid X
receptor (FXR) with EC50 of 65 nM.
S2782 GW4064
FXR Agonists
Cl
O
N
O
Cl
Cl
O
HO
BMS-806 (BMS 378806) selectively inhibits
the binding of HIV-1 gp120 to the CD4
receptor with EC50 of 0.85-26.5 nM in virus.
S2632 BMS-378806
Dexamethasone is an interleukin receptor
inhibitor and also suppresses COX-2.
S4028 Dexamethasone Sodium Phosphate
Size
50 mg
gp120/CD4 Inhibitor
GW3965 is a potent, selective LXR agonist
for hLXR and hLXR with EC50 of 190 nM
S2630 GW3965 HCl
Liver X Receptor Agonist
IL Receptor Inhibitors
Dexamethasone is an anti-inflammatory and immunosuppressant.
S1322 Dexamethasone (DHAP)
O
H
HO
F H
OH
O
O P
-O
O-
O
Na+
Na+
A-674563 is anAkt1 inhibitor with Ki of 11 nM, modest potent to PKA
and >30-fold selective for Akt1 over PKC.
S2670 A-674563
Substance P antagonists (SPA).
S1189 Aprepitant
Substance P Antagonist
CP-91149 is a selective glycogen
phosphorylase (GP) inhibitor with IC50 of 0.13
M in the presence of glucose, 5- to 10-fold
less potent in the absence of glucose.
S2717 CP-91149
Phosphorylase Inhibitor
H 89 2HCl is a potent PKA inhibitor with Ki of
48 nM, 10-fold selective for PKA than PKG,
greater than 500-fold selectivity than PKC,
MLCK, calmodulin kinase II and casein
kinase I/II.
S1582 H 89 2HCl
PKA Inhibitors
N
S
N
H
O
O
H
N
Br
HCl HCl
SB705498 is a TRPV1 antagonist for
hTRPV1, antagonizes capsaicin, acid, and
heat activation of TRPV1 with IC50 of 3 nM,
0.1 nM and 6 nM, shows a degree of voltage
dependence, exhibits >100-fold selectivity for
TRPV1 over TRPM8. Phase 2.
S2773 SB705498
TRPV Antagonist
BIBR 953 (Dabigatran, Pradaxa) is a potent
nonpeptide thrombin inhibitor with IC50 of 9.3
nM.
S2196 BIBR 953 (Dabigatran etexilate)
Thrombin Inhibitor
O
t
h
e
r
s
Page 93
Page 10
Size
5 mg 50 mg 200 mg
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Bioactive Screening Libraries
Bioactive Screening Libraries (96-Well)
What is a Bioactive Screening Library?
Bioactive Screening Libraries are ready-to-use chemical libraries
used for drug discovery, lab drug screening, drug target identification,
and other pharmaceutical-related applications.
You can customize your library by Cherry Picking.
Build the right library for your research endeavors by choosing fromcompounds
in all of our available libraries.
You could select:
Please contact us at info@selleckchem.comto customize your library.
Specific
Compounds
Quantities Plate map Concentration Format
(Dry/solid or
DMSO solution)
The libraries consist of a unique and diverse collection of over 2,500
small molecules with validated biological and pharmacological
activities.
Safety and effectiveness of the compounds has been demonstrated
by preclinical and clinical research, and many of the compounds
are FDA-approved.
The collections of unique small molecules, which include inhibitors, activators, antagonists, and agonists,
are focused on over 200 targets that are part of more than 20 signaling pathways. These pathways
include, among many others, apoptosis, and the PI3K/Akt/mTOR, and MAPK pathways.
Selleck offers customized bioactive screening libraries.
124
Bioactive Compound Library / Kinase Inhibitor Library
Cat.No. L1700 Bioactive Compound Library
A unique collection of 1650 bioactive chemical compounds for high throughput screening (HTS)
and high content screening (HCS)
Bioactivity and safety confirmed by preclinical research and clinical trials
Some compounds have been approved by the FDA
Includes most Selleck inhibitors, APIs, natural products, and chemotherapeutic agents
Structurally diverse, medicinally active, and cell permeable
Rich documentation with structure, IC50, and customer reviews
NMR and HPLC validated to ensure high purity
Cat.No. L1200 Kinase Inhibitor Library
A unique collection of 273 kinase inhibitors for high throughput screening (HTS) and
high content screening (HCS)
Some inhibitors have been approved by the FDA
Most are ATP competitive
Size (Pre-dissolved in DMSO)
100 L/well (10 mM solution) 250 L/well (10 mM solution)
Targets include:
PI3K VEGFR mTOR EGFR Aurora Kinase PDGFR
c-Met c-Kit CDK J AK Flt MEK
Bcr-Abl HER2 Raf Akt FGFR Src
ALK GSK-3 p38 MAPK IGF-1R PKC and more
Product Citations: PLoS One, 2013, 8(5): e63240 Br J Pharmacol, 2012, 166(3): 858-76
Data from[PLoS One, 2013, 8(5): e63240] Data from[Br J Pharmacol, 2012, 166(3): 858-76]
Phone:+1-832-582-8158
www.selleckchem.com
FDA-approved Drug Library / Inhibitor Library
Cat.No. L1300 FDA-approved Drug Library
A unique collection of 1165 FDA approved drugs for high throughput screening (HTS) and
Locate new targets for old drugs
Bioactivity and safety confirmed by clinical trials
All compounds have been approved by FDA
Related to oncology, cardiology, anti-inflammatory, immunology, neuropsychiatry, analgesia etc
Cat.No. L1100 Inhibitor Library
A unique collection of 1159 small molecule inhibitors for high throughput screening (HTS) and
Some inhibitors have been approved by the FDA
Includes most Selleck inhibitors, APIs, natural products, and chemotherapeutic agents
Targets include:
PI3K mTOR Akt GSK-3 VEGFR EGFR
PDGFR J AK FLT3 HER2 Bcl-2 Caspase
STAT MEK Raf p38 MAPK Bcr-Abl Wnt/beta-catenin
5-HT
Receptor
Androgen Receptor
Adrenergic
Receptor
Histamine
Receptor
AChR Calcium
Channel
Sodium Channel
PKC CDK Aurora Kinase HDAC TGF-beta/Smad Proteasome
Estrogen/progestogen Receptor and more
126
Epigenetics Compound Library / Target Selective Inhibitor Library
Cat.No. L1900 Epigenetics Compound Library
A unique collection of 51 small molecule modulators (inhibitors and activators) with biological
activity used for epigenetics research and associated assays. A variety of structurally and
mechanistically different compounds are included
A valuable tool for chemical genomics, epigenetic target identification in pharmacogenomics,
and other biological applications
NMR and HPLC validated to ensure the highest purity
Targets include:
HDAC Aurora Kinase Sirtuin DNA Methyltransferase
HIF Histone demethylases Histone Methyltransferase Epigenetic Reader Domain
Cat.No. L3500 Target Selective Inhibitor Library
A unique collection of validated bioactive compounds covering over 140 targets
Each compound was selected based on its ability to principally interact with a single target,
leading to minimal off-target activity
Selectivity is at least 100-fold higher relative to non-primary target(s)
Targets cover a wide variety of signaling pathways, including PI3K/Akt, MAPK, PTK, JAK,
apoptosis, and others
This unique tool is ideal for studying mechanisms of action or for target screening
Compounds are structurally diverse, biologically active, and cell permeable
Selleck provides rich supporting documentation which includes compound structures, IC50s,
and customer reviews
Compounds are NMR and HPLC validated to ensure our customers receive high purity
compounds
Phone:+1-832-582-8158
www.selleckchem.com
Natural Product Library / GPCR Compound Library
Targets include:
5-HT Receptor Adrenergic Receptor AChR Histamine Receptor Dopamine Receptor
GABA Receptor Opioid Receptor GluR cAMP Cannabinoid Receptor
P2 Receptor OX Receptor
CXCR Estrogen/progestogen Receptor
SGLT MT Receptor
and more
Hedgehog/Smoothened
Cat.No. L2200 GPCR Compound Library
A unique collection of 264 small molecules targeting G protein coupled receptors used in GPCR
screening by pharmaceutical and biotechnology companies in various research and drug
development projects
All of the small molecules in the GPCR library are well characterized with biological and
pharmaceutical activity
A powerful tool for discovering GPCR-based drugs that are the richest signal receptor targets
for drug discovery.
It is estimated about 200 so-called orphan GPCRs are functionally unknown, as a result, use
of our GPCR Small Molecule Compound Library for screening the functionally unknown GPCRs
may yield potentially new GPCR-based drug candidates
Cat.No. L1400 Natural Product Library
A unique collection of 144 natural products for high throughput screening (HTS) and
Structurally diverse, bioactive, and cell permeable
Rich documentation with structure and IC50
NMR and HPLC validated ensure high purity
128
Anti-cancer Compound Library / Tyrosine Kinase Inhibitor Library
Cat.No. L3000 Anti-cancer Compound Library
A unique collection of 349 anti-cancer small molecules for 12 types of cancers: Breast Cancer,
Leukemia, Lung Cancer, Lymphoma, etc
This library contains inhibitors of PI3K, HDAC, mTOR, CDK, Aurora Kinase, JAK, etc
Some compounds have been approved by the FDA
Cat.No. L1800 Tyrosine Kinase Inhibitor Library
A unique collection of 118 tyrosine kinase inhibitors for high throughput screening (HTS) and
Some tyrosine kinase inhibitors have been approved by FDA
Structurally diverse, medicinally active and cell permeable
Rich documentation with structure, IC50 and customer reviews
NMR and HPLC to ensure the high purity
Targets include:
EGFR c-Kit c-Met VEGFR FGFR FGFR
Bcr-Abl IGF-1R PDGFR ALK Axl and more
Phone:+1-832-582-8158
www.selleckchem.com
Stem Cell Signaling Compound Library / Cambridge Cancer Compound Library
Cat.No. L2100 Stem Cell Signaling Compound Library
A unique collection of 75 small molecule inhibitors with biological activity used for stem cell
regulatory and signaling pathway research. All of the small molecule inhibitors in the stem cell
screening library are well characterized with biological and pharmaceutical activity
A powerful tool for researching the mechanism behind stem cells, regenerative therapy, means
differentiation, drug screening based on tumor stem cells, as well as other pharmaceutical and
biological applications
The stem cell inhibitor library contains small molecules associated with signaling pathways
which modulate the function of stem cells such as Wnt, Notch, SMAD, and Hedgehog signaling
Targets include:
Wnt/beta-catenin TGF-beta/Smad Hedgehog/Smoothened J AK STAT
GSK-3 Gamma-secretase IB/IKK Raf and more
Cat.No. L2300 Cambridge Cancer Compound Library
A highly value-added library derived through a collaboration with researchers at the MIT Koch
Institute
A unique collection of 384 cancer-targeted compounds for high throughput screening (HTS) and
Embraces the whole spectrum of cancer targets, from kinases to notch signaling, to metabolic
targets
Structurally diverse, medicinally active and cell permeable
Rich documentation with structure and IC50
NMR and HPLC to ensure the high purity
130
131
Pfizer Licensed Compound Library / Autophagy Compound Library / Ion Channel Ligand Library
Cat.No. L2400 Pfizer Licensed Compound Library
All 96 compounds are licensed by Pfizer and have been marketed or clinically proven bioactive
Wide range of potential uses: from anti-cancer compounds (Bosutinib) to a glycylcycline
antiobiotic (Tigecycline) to combat the growing prevalence of antibiotic resistance
Purchase as a diverse library or individually to meet your drug-discovery needs
Reliability Guarantee: All compounds are developed, validated, and manufactured by Pfizer
All compounds are validated using NMR and HPLC
Detailed preclinical research data and safety information available
Cat.No. L2600 Autophagy Compound Library
A unique collection of 149 small molecules with autophagy-inducing or autophagy-inhibiting
activity
A useful tool for studying the roles of molecules in autophagy
Targets Proteasome, HIF, HDAC, Aurora Kinase, Sirtuin, E3 Ligase, Calcium Channel, mTOR, etc
Targets include:
Calcium Channel Potassium Channel Sodium Channel GABA Receptor
Cat.No. L2700 Ion Channel Ligand Library
A unique collection of 59 small molecule modulators used for Ion channel research
Phone:+1-832-582-8158
www.selleckchem.com
PI3K/Akt Inhibitor Library / Apoptosis Compound Library / MAPK Inhibitor Library
Cat.No. L2800 PI3K/Akt Inhibitor Library
A unique collection of 86 small molecule inhibitors used for PI3K/Akt/mTOR pathway research
A valuable tool for researching the survival, proliferation, and apoptosis of cells
Targets include:
PI3K mTOR Akt ATM/ATR GSK-3
PDK-1 S6 Kinase DNA-PK AMPK
Cat.No. L3300 Apoptosis Compound Library
A unique collection of 23 small molecules used for apoptosis research
Targets include:
Bcl-2 Caspase p53 TNF-alpha
Mdm2 IAP c-RET Survin
Cat.No. L3400 MAPK Inhibitor Library
A unique collection of 34 small molecule inhibitors used for MAPK signaling research
Targets include:
MEK Raf p38 MAPK J NK ERK
132
133
Protease Inhibitor Library / Anti-infection Compound Library / Anti-diabetic Compound Library
Cat.No. L2500 Protease Inhibitor Library
A unique collection of 33 small molecule inhibitors used for chemical genomics,
high-throughput screening (HTS), and high content screening (HCS)
Targets include:
Proteasome DPP-4 HCV Protease HIV Protease Caspase
Gamma-secretase Beta Amyloid Cathepsin K MMP
Cat.No. L2900 Anti-diabetic Compound Library
A unique collection of 31 small molecules affecting the development of diabetes
Cat.No. L3100 Anti-infection Compound Library
A unique collection of 134 anti-infective small molecules with biological activity of antibiotics,
antifungal drugs,anti-HIV,etc
The compounds in this library mainly include sulfonamides, aminoglycosides, tetracyclines
and macrolides
A useful tool to research infectious disease for academic institutions, medical research
organizations, andthe pharmaceutical industry
Product Alphabetical Index
AG-18
AG-490
AGI-5198
Agomelatine
AlfuzosinHCl
Alisertib
Aliskirenhemifumarate
Allopurinol
Alvocidib
AM-1241
AM251
AmantadineHCl
AMD3100
AMD31008HCl
Amfebutamone
AMG900
AMG-208
AMG458
AMG-706
Aminoglutethimide
AmiodaroneHCl
Amlodipinebesylate
AMN-107
Amonafide
Amprenavir
Amuvatinib
Anacetrapib
Anastrozole
Andarine
AP24534
AP26113
Apatinib
Apicidin
Apixaban
APO866
ApoG2
Apogossypolone
ApoptosisActivator 2
Apremilast
Aprepitant
AR-12
AR-42
Arg-Gly-AspPeptides
ARN-509
ARQ197
ARRY-334543
25
22,48
116
95
97
68
107
100
65
103
103
99
104
104
99
69
29
30
19,27,35
108
94,110
109
39
81
120
27,32,34,36
117
108
106
16,27,33,39
36
20
84
115
117
44
44
45
114
123
13
84
63
106
29
46,94
Arry-380
AS-252424
AS-604850
AS-605240
AS703026
Asenapine
AST-1306
AT101
AT13387
AT406
AT7519
AT7867
AT9283
Ataluren
Atazanavir Sulfate
Atorvastatincalcium
AuroraAInhibitor I
AUY922
AV-951
Avagacestat
Avasimibe
AVL-292
Axitinib
AY22989
AZ3146
AZ960
AZ628
Azacitidine
AZD0530
AZD1152-HQPA
AZD1480
AZD2014
AZD217
AZD2281
AZD2461
AZD3839
AZD4547
AZD5363
AZD5438
AZD6244
AZD6482
AZD7762
AZD8055
AZD8330
AZD8931
AzilsartanMedoxomil
24,30
5
4
3
52
96,97
25
44
61
46,94
65
10,14
40,48,69
111
120
117
69
60
17,27,35
88,95
113
42
16,27,35
6,92
62
48
54
85
40,41
68
48
8
17
76
77
100
33
11
66
51
4
71
7
53
23,30
108
0-9
(-)-Blebbistatin
(-)-HuperzineA
(+)-JQ1
10058-F4
17-AAG
17-DMAGHCl
2-MeOE2
2-Methoxyestradiol
3-DeazaneplanocinA
3-Methyladenine
5-Fluoracil
5-FU
6-MP
110
97
85
73
60
60
39
39
86
3,93
78
78
79
117
2
10,66,123
14
77
27,34
113
113
44
43
43,92
62
18,27,37
76
32
24,30
14
98
84
122
99
80,92
97
20,24,30
22,30
77
31
77
24
A
A922500
A66
A-674563
A-769662
A-966492
AB1010
Abiraterone
AbirateroneAcetate
ABT-199
ABT-263
ABT-737
ABT-751
ABT-869
ABT-888
AC220
AC480
Acadesine
Acetylcysteine
ACY-1215
Adefovir Dipivoxil
ADL5859HCl
Adriamycin
ADX-47273
AEE788
Afatinib
AG-014699
AG-1024
AG14361
AG-1478
134
Azithromycin 92
B
98
103
39
44
92
68
49
67
94,101
17,35,54
5
106
120
83
107
99
1,7,13
37
33
5,9
72
103
72
15,27,33
81
123
22,30
107,113
13
60
41
55
46
98
53
52
86
2
78
96
44
77
29,37
20,29
66
123
BA679BR
BAF312
Bafetinib
BAM7
b-AP15
Barasertib
Baricitinib
BAY1000394
BAY11-7082
BAY73-4506
BAY80-6946
BazedoxifeneHCl
BB-94
Belinostat
Benazepril HCl
Benztropinemesylate
BEZ235
BGB324
BGJ398
BGT226
BI 2536
BI10773
BI6727
BIBF1120
BIBR1532
BIBR953
BIBW2992
Bicalutamide
BI-D1870
BIIB021
BIIB057HCl
BIRB796
Birinapant
Bisoprolol
BIX02188
BIX02189
BIX01294
BKM120
BleomycinSulfate
Blonanserin
BM-1074
BMN673
BMS777607
BMS794833
BMS-265246
BMS-378806
C
88
85
62
15,29,32,35,36,37
21,37
2
81
103
107
108
22,30
78
93,110
78
119
80
4
114
45
7
10
69
70
C59
C646
CA4PDisodium
Cabozantinib
Cabozantinibmalate
CAL-101
Camptothecin
Canagliflozin
Candesartan
CandesartanCilexetil
Canertinib
Capecitabine
Carbamazepine
Carboplatin
Carfilzomib
Carmofur
CAY10505
CC-10004
CC-5013
CCI-779
CCT128930
CCT129202
CCT137690
BMS-387032
BMS-536924
BMS-540215
BMS-582664
BMS-599626
BMS-707035
BMS-708163
BMS-754807
BMS-790052
BMS907351
BMS-911543
Bortezomib
BosentanHydrate
Bosutinib
BrefeldinA
Brivanib
Brivanibalaninate
BS-181HCl
BSI-201
Buparlisib
BupivacaineHCl
BX-795
BX-912
BYL719
65
31
18,34
20,34
24,30
121
88,95
31,36
119
15,29,32,35,36,37
48
118
103
41
94,110
18,34
20,34
66
77
2
104
13
13
2
Cediranib
Celecoxib
CEP-18770
CEP-32496
CEP33779
CGI1746
CGK733
CGS21680HCl
CH5126766
CH5132799
CH5424802
CHIR-124
CHIR-258
CHIR-265
CHIR-98014
CHIR-99021HCl
Chlorpromazine
CHR2797
CI-1033
CI-1040
CI994
Cilengitide
Cilnidipine
Cilomilast
Cilostazol
Cinacalcet HCl
Ciprofibrate
Cisplatin
CK-1827452
Cladribine
Clarithromycin
ClemastineFumarate
Clinofibrate
Clofarabine
Clomifenecitrate
Clopidogrel
Clozapine
CNX-2006
Cobicistat
CombretastatinA4PhosphateDisodium
Costunolide
CP673451
CP-466722
CP-473420
CP-690550
CP-690550citrate
CP-724714
CP-868596
CP-91149
17
96
119
37,55
49
42
13
105
52
5,8
36
71
17,27,32,34,35
17,54
11
11
99,111
115
22,30
52
84
63
109
114
114
104
112
78
110
79
113
98
108
79
106
100
95
22
113
62
81
26
12
25
48
47
23,30
26
123
135
Divalproexsodium
Dizocilpine
DMXAA
Docetaxel
Dolutegravir
Donepezil HCl
Doramapimod
DorzolamideHCl
Dovitinib
DovitinibDilacticacid
Doxazosinmesylate
Doxorubicin
Drospirenone
Droxinostat
DuloxetineHCl
DuP753
Dutasteride
Dynasore
DZNeP
92
97
39
62
121
98
55
116
17,27,32,34,35
19,27,32,33,35
97
80,92
106
84
96
107
105
63
86
62
19,29
18
23
60
122
30
103
122
107
19,32,69
21,32,69
86
82
106,113
59
98
81
62
63
62
86
86
90
22,92
96
99
80
E
E7010
E7050
E7080
EKB-569
Elesclomol
Elvitegravir
EMD1214063
Empagliflozin
Emtricitabine
Enalaprilat dihydrate
ENMD-2076
ENMD-2076L-(+)-Tartaricacid
Entacapone
Entinostat
Enzalutamide
Enzastaurin
EpinephrineBitartrate
EpirubicinHCl
EPO906
EpothiloneA
EpothiloneB
EPZ004777
EPZ-5676
Erismodegib
ErlotinibHCl
Etodolac
Etomidate
Etoposide
CPI-613
Crenolanib
Crizotinib
CT99021HCl
CUDC-101
CUDC-907
CX-5461
CX-6258
CYC116
CYC202
Cyclopamine
Cyclophosphamide
Cyproteroneacetate
Cyt387
CYT997
Cytarabine
115
26
28,36
11
23,30,83
5,84
79
50
19,69
65
89
79
107,113
48
63
79
D
122
123
54
79
83
119
24
119
33,36,40,68
103
122
96
88,95
120
34,39,41
81
40
85
7
107
119
84
59
25
93,123
123
93,123
107
122
106
66
d4T
Dabigatranetexilate
Dabrafenib
Dacarbazine
Dacinostat
Daclatasvir
Dacomitinib
Danoprevir
Danusertib
Dapagliflozin
Dapivirine
DapoxetineHCl
DAPT
Darunavir Ethanolate
Dasatinib
DaunorubicinHCl
DCC-2036
Decitabine
Deforolimus
Dehydroepiandrosterone
Delanzomib
depsipeptide
DequaliniumChloride
Desmethyl Erlotinib
Dexamethasone
DexamethasoneSodiumPhosphate
DHAP
DHEA
Didanosine
Dienogest
Dinaciclib
117
6
46,101
80
108
Evacetrapib
Everolimus
EVP4593
EX527
Exemestane
71,93
109
98
39
105
40,59,103
40,59,103
84
117
65
66
79
50,78
78
99
78
95
79
107
116
14
17,28
108
104
62
41
41
40,59,103
105
F
Fasudil HCl
Felodipine
Fesoterodinefumarate
FG-4592
Finasteride
Fingolimod
fingolimodhydrochloride
FK228
FK866
Flavopiridol
Flavopiridol HCl
Floxuridine
Fludarabine
FludarabinePhosphate
Flumazenil
Fluorouracil
FluoxetineHCl
Flupirtinemaleate
Flutamide
FluvastatinSodium
FMK
Foretinib
Formestane
Forskolin
FosbretabulinDisodium
Fostamatinib
Fostamatinibdisodium
FTY720
Fulvestrant
99
99
107,113
61
2
10
46
44
9
89
42
G
Gabapentin
GabapentinHCl
Galeterone
Ganetespib
GDC-0032
GDC-0068
GDC-0152
GDC-0199
GDC-0349
GDC-0449
GDC-0834
136
GDC-0879
GDC-0941
GDC-0980
Gefitinib
Geldanamycin
Gemcitabine
GemcitabineHCl
Genistein
Gestodene
GinkgolideB
Glimepiride
GNF-2
Go6983
Golvatinib
Griseofulvin
GS-1101
GS-9137
GS-9350
GSI-IX
GSKJ4HCl
GSK1059615
GSK1070916
GSK1120212
GSK1292263
GSK1349572
GSK1363089
GSK1838705A
GSK1904529A
GSK2118436
GSK2126458
GSK2334470
GSK256066
GSK2636771
GSK343
GSK429286A
GSK458
GSK461364
GSK690693
GSK923295
GTx-024
GW2580
GW3965HCl
GW4064
GW441756
GW501516
GW5074
GW-572016
GW786034HCl
GW788388
54
2
4,8
22
61,93
79,93
78,93
81
106
104
120
40
59
19,29
63
2
122
113
88,95
85
4,8
70
52
108
121
17,28
31,35
31
54
3,7
13
114
5
86
72
3,7
73
10
62
106
37
123
123
36
112
55
23,30
16,27,35
75
45,94
84
29
65,69
57
99
122
J
JNJ26854165
JNJ-26481585
JNJ-38877605
JNJ-7706621
JNK-IN-8
JTC-801
JTK-303
109
119
91
111
88
88
Isradipine
ITMN-191
IU1
Ivacaftor
IWP-2
IWR-1-endo
K
96
113
96
104
103
20,27,35
20,27
9
76
7
12
2,14
13
12
32,40,69
61
41
88
Ketanserin
Ketoconazole
Ketoprofen
Ki16198
Ki16425
Ki8751
KRN633
KRX-0401
Ku-0059436
Ku-0063794
KU-55933
KU-57788
KU59403
KU-60019
KW2449
KW-2478
KX2-391
KY02111
L
120
111
24,30
23,30
83
96,97,99
82
46
90
36
74
91
LAF-237
Lansoprazole
Lapatinib
LapatinibDitosylate
LAQ824
Latrepirdine
LBH589
LCL161
LDE225
LDK378
LDN193189
LDN-57444
GW842166X
GW9508
GW9662
GX15-070
GZD824
103
108
112
44,92
39
123
71,93
44
68
23,30
73
10,53
60
97
H
H892HCl
HA-1077HCl
HA14-1
Hesperadin
HKI-272
HMN-214
Honokiol
HSP990
HupA
42
96
110
3
88
25
81
2
79
101
26
26,35,39
47,49
49
29
98
77
7
5
39
77
39
63
5
60
107
80
81
97
115
62
I
Ibrutinib
Ibuprofen
IbutilideFumarate
IC-87114
ICG-001
Icotinib
IdarubicinHCl
Idelalisib
Ifosfamide
IKK-16
Imatinib
ImatinibMesylate
INCB018424
INCB028050
INCB28060
Indacaterol Maleate
Iniparib
INK128
INK1197
INNO-406
INO-1001
IOX2
IPA-3
IPI-145
IPI-504
Irbesartan
Irinotecan
IrinotecanHCl Trihydrate
IsoprenalineHCl
Isotretinoin
Ispinesib
137
Lenalidomide
Lenvatinib
LEQ506
Letrozole
Linagliptin
Linifanib
Linsitinib
Lonafarnib
LoperamideHCl
Lopinavir
Loratadine
Losartanpotassium
Lovastatin
LY2090314
LY2109761
LY2157299
LY2228820
LY2484595
LY2603618
LY2606368
LY2784544
LY2811376
LY2835219
LY294002
LY2940680
LY3009104
LY3039478
LY315920
LY317615
LY3359793HCl
LY364947
LY404039
LY411575
LY450139
LY500307
LY900009
45
18
90
108
120
18,27,37
31
117
93,99
120
98
107
116
12
75
75
56
117
71
71
48
89,95
65
1,92
90
49
88
116
59
100
75
97
89
88
106
88
84
109
109
122
120
27,34
83
63
106,113
106
106
M
M344
Manidipine
Manidipine2HCl
Maraviroc
Marimastat
Masitinib
MC1568
Mdivi-1
MDV3100
Medroxyprogesteroneacetate
Megestrol Acetate
Mercaptopurine
MetforminHCl
Methotrexate
MG-132
MGCD0103
MGCD-265
MianserinHCl
Midostaurin
Mifepristone
Milrinone
Miltefosine
Mirabegron
Mizoribine
MK0822
MK801
MK-0457
MK-0518
MK0683
MK-0752
MK-0859
MK-1775
MK-2048
MK-22062HCl
MK-2461
MK-2866
MK3207HCl
MK-4827
MK-5108
MK-8245
MK-8776
ML130
MLN0905
MLN2238
MLN2480
MLN4924
MLN518
MLN8054
MLN8237
MLN9708
Mocetinostat
MotesanibDiphosphate
MoxifloxacinHCl
Mozavaptan
MP-470
MS-275
Mubritinib
MycophenolateMofetil
79
93
115
118
83
18,29,36
99
59
106
110
10
98
79
123
97
68
121
82,92
88,95
117
73
121
9
27,29,34
106
104
77
70
116
66,71
101
73
119
54
92
32
68
68
119
83
19,27,35
81
104
27,32,34,36
82
30
115
119
96
110
43
97
45
79
115
23,30
122
50,94
110
39
15,27,33
77
117
63,94
101
39
104
45,46,79,94
92
45,94
6,92
60
45
7
65
14
2,14
46,94
31
20,24,30
31
60
61
1,7,13
33
5,9
19,36,40,41,54
2
48
30
60
90
42
N
Nafamostat Mesylate
Naratriptan
Nateglinide
Navitoclax
Nebivolol
Necrostatin-1
Nelarabine
Nepicastat HCl
Neratinib
Nevirapine
Niclosamide
Nicorandil
Nilotinib
Nintedanib
Niraparib
NLG919
Nocodazole
Nodinitib-1
NPI-2358
NPS-2143
NSC207895
NSC632839
NSC652287
NSC226080
NSC23766
NSC319726
NSC-683864
NU6027
NU7026
NU7441
Nutlin-3
NVP-ADW742
NVP-AEE788
NVP-AEW541
NVP-AUY922
NVP-BEP800
NVP-BEZ235
NVP-BGJ398
NVP-BGT226
NVP-BHG712
NVP-BKM120
NVP-BSK8052HCl
NVP-BVU972
NVP-HSP990
NVP-LDE225
NVP-TAE226
138
23
22
17,33
52
53
52
23
78,115
9
107
110,111
71
42
42
77
28,36
42,69
29
90
4,8,10
55
61
61
4,8
114
24
24
116
14
113
90
103
42
85
45,94
56
28
69
33,36,40,68
66
66
66
14
110
10,13
2,7,14,93
41
45,94
5
PD153035HCl
PD168393
PD173074
PD184352
PD318088
PD98059
Pelitinib
Pemetrexed
Perifosine
Perindopril Erbumine
PF3716556
PF477736
PF573228
PF-00562271
PF-01367338
PF-02341066
PF-03814735
PF-04217903
PF-04449913
PF-04691502
PF-04880594
PF-04928473
PF-04929113
PF-05212384
PF-2545920
PF299
PF299804
PF-3845
PF-4708671
PF-4981517
PF-5274857
PF-543
PF-562271
PFI-1
PFT
PH-797804
PHA-665752
PHA-680632
PHA-739358
PHA-767491
PHA-793887
PHA-848125
PhenforminHCl
Phenytoinsodium
PHT-427
PI-103
Piceatannol
Pifithrin-
PIK-293
4
3,14
4
4
52
114
81
75
96
77
59
5
4,8
104
104
39
54
54
98
45
16,27,33,39
41
9,14,26
41
7,93
31
119
91
83
115
100
117
41
41
118
111
18,35
83
92
PIK-294
PIK-75
PIK-90
PIK-93
Pimasertib
Pimobendan
Pirarubicin
Pirfenidone
Piroxicam
PJ34
PKC412
PKI-402
PKI-587
Plerixafor
Plerixafor 8HCl
Plinabulin
PLX4032
PLX-4720
PNU-120596
Pomalidomide
Ponatinib
PP1
PP-121
PP2
PP242
PQ401
PR-171
PR-619
Pracinostat
Pralatrexate
Prasugrel
Pravastatinsodium
PRT062607HCl
PRT2607HCl
PS-341
PTC124
PTK7872HCl
PXD101
PYR-41
46,101
99
32
Q
QNZ
Quetiapinefumarate
Quizartinib
32,41
41
37
R
R406
R406(freebase)
R428
44,92
123
95,99
76
110
107
110
93,111
72
119
119
103
113
8
84
24
22,92
25
31
20,34,37
13
78
98
O
P
Obatoclaxmesylate
Odanacatib
Olanzapine
Olaparib
OligomycinA
OlmesartanMedoxomil
Omecamtivmecarbil
Omeprazole
ON-01910
ONX0912
Oprozomib
Org27569
Orteronel
OSI-027
OSI-2040
OSI-420
OSI-744
OSI-774
OSI-906
OSI-930
OSU-03012
Oxaliplatin
Oxybutynin
91
91
65
41
91
8
45
62,93
67
8
98
82
96
62
19,27,35
16,27,35
84
42
84
64
52
51
67
P005091
P22077
P276-00
P505-15HCl
P5091
P529
PAC-1
Paclitaxel
PalbociclibIsethionate
Palomid529
Pancuronium
Panobinostat
ParoxetineHCl
Patupilone
Pazopanib
PazopanibHCl
PCI-24781
PCI-32765
PCI-34051
PD0332991HCl
PD198306
PD0325901
PD0332991Isethionate
139
R547
R788
R788disodium
RAD001
RAF265
Raf265derivative
RaloxifeneHCl
Raltegravir
Raltitrexed
Ramelteon
Ramipril
Ranitidine
Ranolazine2HCl
Rapamycin
RasagilineMesylate
Rebastinib
Regorafenib
Repaglinide
Resminostat
Resveratrol
RG108
RG7204
RG7422
RGDPeptides
Ridaforolimus
Rigosertib
Riluzole
Rimonabant
Risperidone
RITA
Ritonavir
Rivaroxaban
RKI-1447
RO4929097
RO5126766
Rocilinostat
RocuroniumBromide
Rofecoxib
Roflumilast
Rolipram
Romidepsin
Roscovitine
Rosiglitazonemaleate
RosuvastatinCalcium
RS-127445
Rucaparib
Rufinamide
Ruxolitinib
66
41
41
6
17,54
20,55
106
121
79
100
107
99
109
6,92
116
40
17,35,54
110
83
80,93
85,117
54
4,8
63
7
72
110
103
96
45,94
120
115
72
88,95
52
84
98
97
113
114
84
65
112
107
96
77
110
47
50
44
116
82,92
97
90
18
3,7
48
40,41
120
56
55
11
11
74
75
62
100
75
54
123
62
83
101
66,71
66
57
83
65
51
88
20
45,94
86
85
50
29
114
97
103
6,92
80
120
103
56
41
53
S
S3I-201
Sabutoclax
SafinamideMesylate
SAHA
Salbutamol Sulfate
SANT-1
SAR131675
SAR245409
SAR302503
Saracatinib
Saxagliptin
SB202190
SB203580
SB216763
SB415286
SB431542
SB525334
SB743921
SB-408124
SB-505124
SB590885
SB705498
SB-715992
SB939
SC-514
SCH900776
SCH727965
SCH772984
Scriptaid
Seliciclib
Selumetinib
Semagacestat
Semaxanib
Serdemetan
SGC0946
SGI-110
SGI-1776freebase
SGX-523
Sildenafil citrate
Silodosin
Siponimod
Sirolimus
Sirtinol
Sitagliptinphosphatemonohydrate
Sitaxentansodium
Skepinone-L
SKI-606
SL327
46,94
50
81
65
69
61
61
101
110
83
84,93,99
16,26,54
59
57
80
49
33
33
60
61
50
59
122
26,35,39
29
20
18,27,33
92
95
16,26,35
115
SM-406
SMI-4a
SN-38
SNS-032
SNS-314Mesylate
SNX-2112
SNX-5422
Sodium4-Aminosalicylate
Sodiumorthovanadate
SodiumPhenylbutyrate
Sodiumvalproate
Sorafenib
Sotrastaurin
SP600125
SRT1720
S-Ruxolitinib
SSR
SSR128129E
STA-4783
STA-9090
Stattic
Staurosporine
Stavudine
STI571
SU11274
SU5416
SU6668
SulfacetamideSodium
SumatriptanSuccinate
SunitinibMalate
SYN-117HCl
112
46
84
114
42
35
30
56
24,30
90
113
53
108
69
73,94
93,105
T
T0070907
T-3256336
Tacedinaline
Tadalafil
TAE226
TAE684
TAK165
TAK715
TAK-285
TAK-441
TAK-700
TAK-733
TAK-875
TAK-901
TAME
TamoxifenCitrate
140
32
100
48
92
32
12
119
19,27,35
107
92
7
122
122
45,94
5
5
32,36,48
48
2
113
46,94
71
85
96
11
11
36
98
117
29
17,27,35
17,27,32,34,35
19,27,32,33,35
122
48
47
98
104
116
80
117
106
7,93
8,13
115
68
101
111
52
Tandutinib
Tariquidar
Tasocitinib
TCID
TCS359
TDZD-8
Telaprevir
Telatinib
Telmisartan
Temozolomide
Temsirolimus
Tenofovir
Tenofovir Disoproxil Fumarate
Tenovin-1
TG100713
TG100-115
TG101209
TG101348
TGX-221
TH-302
Thalidomide
Thiazovivin
Thioguanine
Tianeptinesodium
TIC10
Tideglusib
Tie2kinaseinhibitor
TiotropiumBromidehydrate
Tipifarnib
Tivantinib
Tivozanib
TKI-258
TKI258Dilacticacid
TMC120
Tofacitinib
Tofacitinibcitrate
Tolterodinetartrate
Tolvaptan
Topiramate
TopotecanHCl
Torcetrapib
ToremifeneCitrate
Torin1
Torin2
Tosedostat
Tozasertib
TPCA-1
TRAM-34
Trametinib
TrichostatinA
Triciribine
Triciribinephosphate
Trifluoperazine2HCl
Trifluoroacetatesalt
Trilostane
Trospiumchloride
TSA
TSU-68
TubastatinA
TubastatinAHCl
TW-37
TWS119
Tyrphostin9
TyrphostinAG1296
TyrphostinAG879
TyrphostinAG-1478
82
10
10
92
86
115
98
82
18,27,33
83
83
44
11
25
28,34,35
30
24
52
116
117
86
86
86
86
86
86
77
116
U
U0126-EtOH
U-104
UK383367
UNC0224
UNC0321
UNC0631
UNC0638
UNC0646
UNC1999
UPF1069
URB597
39
84,93,99
107
16
114
98
116
25
18,35
119
12
76
54
95
60
122
120
V
Vadimezan
Valproicacidsodiumsalt
Valsartan
Vandetanib
Vardenafil HCl Trihydrate
Vareniclinetartrate
Varespladib
Varlitinib
Vatalanib2HCl
VCH-222
VE-821
Veliparib
Vemurafenib
Venlafaxine
VER155008
VicrivirocMalate
Vildagliptin
Vinblastine
Vincristine
VinflunineTartrate
Vinorelbine
Vismodegib
Volasertib
Vorapaxar
Voriconazole
Vorinostat
VX-222
VX-661
VX-680
VX-689
VX-702
VX-745
VX-770
VX-809
VX-950
63
62,93
63
56
89
72
104
113
82,92
119
111
68
70
56
56
111
111
119
96
9
44
25,49
88
5,13,93
49
39,91
8
8
8
8
104
24
23
24
W
WAY-100635HCl
WAY-600
WEHI-539
WHI-P154
Wnt-C59
Wortmannin
WP1066
WP1130
WYE-125132
WYE-132
WYE-354
WYE-687
WZ811
WZ3146
WZ4002
WZ8040
87
3
21,37
15,29,32,35,36,37
123
3,7
61
97
X
XAV-939
XL147
XL184
XL-184
XL335
XL765
XL888
XylazineHCl
141
22
103
16
86
103
122
20
20
54
49
68
59
100
3
45
Z
ZD1839
ZD4054
ZD6474
Zebularine
Zibotentan
Zidovudine
ZM306416
ZM323881HCl
ZM336372
ZM39923HCl
ZM-447439
ZoledronicAcid
Zosuquidar 3HCl
ZSTK474
Z-VAD-FMK
71,92
46
5
89
Y
Y-276322HCl
YM155
YM201636
YO-01027
142
Product Catalog Number Index
S1001
S1002
S1003
S1004
S1005
S1006
S1007
S1008
S1009
S1010
S1011
S1012
S1013
S1014
S1017
S1018
S1019
S1020
S1021
S1022
S1023
S1025
S1026
S1028
S1029
S1030
S1032
S1033
S1034
S1035
S1036
S1037
S1038
S1039
S1040
S1042
S1043
S1044
S1045
S1046
S1047
S1048
S1049
S1052
43
43,92
18,27,37
76
16,27,35
40,41
39
51
1,7,13
15,27,33
22,30
31
118
41
17
17,27,32,34,35
22,30
52
34,39,41
7
22,92
22
26,35,39
23,30
45
82
19,27,35
39
31
16,27,35
51
9
2,7,14,93
6,92
16,26,54
16,26,35
32
7
82
16
82,92
68
71,92
60
S1164
S1165
S1166
S1167
S1168
S1169
S1170
S1171
S1172
S1173
S1174
S1175
S1176
S1177
S1178
S1179
S1180
S1181
S1183
S1185
S1186
S1187
S1188
S1189
S1190
S1191
S1192
S1193
S1194
S1195
S1196
S1197
S1198
S1199
S1200
S1202
S1205
S1206
S1207
S1208
S1209
S1210
S1213
S1214
18
62
78
23,30
84,93,99
2
24
19,69
45,94
23
106
60
39
52
17,35,54
24
87
19,32,69
119
120
81
4
108
123
107,113
105
79
46,94
23,30,83
113
108
105
80
79
85
105
3,14
98
17,27,35
80,92
78
115
79
78
S1110
S1111
S1112
S1113
S1114
S1115
S1116
S1117
S1118
S1119
S1120
S1121
S1122
S1123
S1124
S1129
S1130
S1132
S1133
S1134
S1135
S1138
S1139
S1140
S1141
S1142
S1143
S1144
S1145
S1146
S1147
S1148
S1149
S1150
S1152
S1153
S1154
S1155
S1156
S1157
S1158
S1159
S1160
S1163
116
17,28
29
10
29
123
64
10
3
15,29,32,35,36,37
6
44
83
113
31,36
80
46
77
68
40,48,69
78,115
20,34
99
106
60
60
22,48
111
65
89
68
62
78,93
62,93
54
65
69
50
78
119
116
61
111
61
S1053
S1055
S1056
S1057
S1060
S1061
S1064
S1065
S1066
S1067
S1068
S1069
S1070
S1071
S1072
S1075
S1076
S1077
S1078
S1079
S1080
S1082
S1084
S1085
S1087
S1088
S1090
S1091
S1092
S1093
S1094
S1095
S1096
S1098
S1100
S1101
S1102
S1103
S1104
S1105
S1106
S1107
S1108
S1109
82
59
24,30
44,92
76
46,94
27,34
2
53
74
28,36
60
28
44
3
11
55
56
9
23
29
89
18,34
83
77
31
84
31
12
31
29
83
84
77
68
18,35
52
68
54
1,92
13
33,36,40,68
35
72
143
S1215
S1216
S1217
S1218
S1219
S1220
S1221
S1223
S1224
S1225
S1226
S1227
S1228
S1229
S1230
S1231
S1233
S1234
S1235
S1237
S1241
S1243
S1244
S1245
S1248
S1249
S1250
S1251
S1256
S1258
S1259
S1260
S1261
S1262
S1264
S1266
S1267
S1268
S1274
S1275
S1283
S1284
S1288
S1289
S1293
S1294
S1297
S1299
S1302
78
85
79
79
5
20,34,37
79
81
78
80
7
106
81
78
65
80
39
31
108
92
62,93
95
27,32,34,36
96,97,99
63
65,69
106,113
106
110
100
100
104
96
88,95
17,33
8
54
3
13
13
96,97
107
81
80
109
114
63
79
79
S1304
S1305
S1314
S1315
S1316
S1319
S1322
S1324
S1328
S1329
S1332
S1333
S1334
S1338
S1342
S1343
S1344
S1352
S1353
S1354
S1358
S1359
S1360
S1361
S1362
S1363
S1364
S1366
S1367
S1369
S1375
S1376
S1377
S1378
S1379
S1380
S1382
S1384
S1386
S1389
S1392
S1393
S1396
S1397
S1398
S1400
S1401
S1404
S1409
106
79
59
103
29
81
93,123
97
96
99
99
95
79
99
81
104
120
5
113
111
98
107
4,8
18,29,36
72
20,27,35
62
121
81
39
116
106
106
47
115
120
99
79
119
93,111
23
81
80,93
98
122
122
122
115
97
S1410
S1415
S1421
S1422
S1425
S1426
S1430
S1431
S1432
S1436
S1438
S1440
S1441
S1442
S1451
S1452
S1453
S1454
S1455
S1456
S1457
S1458
S1459
S1460
S1462
S1465
S1470
S1472
S1473
S1474
S1475
S1476
S1478
S1480
S1481
S1482
S1484
S1485
S1486
S1487
S1488
S1489
S1490
S1491
S1494
S1497
S1498
S1501
S1506
3
100
59
84
109
110
114
114
95
96
116
98
95
113
69
62
117
69
114
103
120
56
71
57
4
81
18,27,33
116
112
72
52
75
110
119
100
119
83
73
20,24,30
66
96
4
16,27,33,39
50,78
56
115
61
115
107
S1507
S1512
S1515
S1519
S1522
S1523
S1524
S1525
S1526
S1527
S1528
S1529
S1530
S1531
S1532
S1533
S1534
S1536
S1537
S1538
S1540
S1541
S1542
S1544
S1545
S1548
S1549
S1550
S1555
S1556
S1557
S1558
S1561
S1565
S1567
S1568
S1570
S1572
S1573
S1574
S1575
S1577
S1578
S1579
S1582
S1590
S1593
S1594
S1598
107
114
83
69
115
3,7
65
73
32
56
89,95
68
53
52
71
41
103
26
39
119
120
80
104
103
100
103
97
114
7
10,13
20,27
10,14
29,37
111
45
53
12
66
71,93
55
88,95
36
107
67
123
11
115
88
106
144
S1604
S1613
S1614
S1615
S1620
S1623
S1630
S1638
S1639
S1645
S1648
S1657
S1662
S1672
S1693
S1702
S1703
S1704
S1713
S1714
S1718
S1738
S1742
S1754
S1763
S1774
S1776
S1782
S1793
S1801
S1802
S1813
S1835
S1847
S1869
S1885
S1894
S1908
S1909
S1950
S1971
S1972
S1979
S2000
S2001
S2003
S2004
S2005
S2012
107
97
110
96
120
98
100
96
120
96
79
107
109
108
93,110
122
92
122
96
79,93
122
107
122
98
99
85
106
85
107
99
14
109
92
98
96
109
107
107
116
93
110
93,105
94,110
110
122
122
122
121
84
S2013
S2014
S2018
S2037
S2042
S2061
S2077
S2084
S2102
S2111
S2112
S2118
S2128
S2131
S2133
S2134
S2149
S2150
S2151
S2153
S2157
S2158
S2161
S2162
S2163
S2169
S2178
S2179
S2180
S2181
S2182
S2183
S2185
S2186
S2187
S2192
S2193
S2194
S2195
S2196
S2197
S2198
S2199
S2200
S2201
S2202
S2205
S2206
S2207
42
66
21,32,69
108
107,113
116
117
96
116
24,30
96
110
106
113
99
53
108
23,30
90
105
90
32,40,69
17,54
48
14
107
77
48
119
119
62
33
25
75
113
23,30
73
32,41
63
123
77
50
107
20,55
20,29
19,36,40,41,54
24
41
5
S2208
S2209
S2214
S2215
S2216
S2217
S2218
S2219
S2220
S2221
S2222
S2224
S2225
S2226
S2227
S2230
S2231
S2232
S2235
S2238
S2240
S2243
S2244
S2245
S2246
S2247
S2251
S2310
S2449
S2451
S2452
S2454
S2456
S2459
S2462
S2475
S2480
S2481
S2482
S2484
S2489
S2493
S2497
S2505
S2507
S2515
S2516
S2521
S2524
108
63
48
88,95
30
81
7,93
48
54
20
110,111
117
73,94
2
4
75
19,27,35
96
72
8
98
39,91
84
12
113
2
97
10,53
104
99
99
104
99,111
95
98
26
93,99
109
109
110
110
95,99
98
112
97
114
97
98
110
S2542
S2547
S2549
S2550
S2555
S2561
S2566
S2567
S2579
S2593
S2604
S2606
S2617
S2618
S2619
S2620
S2621
S2622
S2623
S2624
S2625
S2626
S2627
S2628
S2629
S2630
S2631
S2632
S2633
S2634
S2635
S2636
S2637
S2638
S2639
S2656
S2658
S2660
S2661
S2662
S2663
S2664
S2665
S2666
S2667
S2668
S2670
S2671
S2673
14
98
98
98
113
106
97
106
122
104
107
106
53
74
118
114
66
9,14,26
110
8
41
71
83
4,8
98
123
116
123
104
40
10
2
108
2,14
61
61
3,7
88,95
8
88
96
108
112
116
121
8
10,66,123
5
52
145
S2919
S2920
S2921
S2922
S2924
S2925
S2926
S2927
S2928
S2929
S3002
S3005
S3012
S3013
S3020
S3021
S3026
S3030
S3031
S3033
S3034
S3035
S3036
S3043
S3051
S3056
S3057
S3083
S3147
S3163
S3201
S4001
S4002
S4009
S4028
S4066
S4071
S4073
S4081
S4125
S4901
S4902
S4907
S4908
S4909
S4920
S4922
S5001
S5002
39
104
113
25
11
117
12
45
56
45,94
115
96
19,27,35
104
84
103
41
50,94
120
120
103
81
117
97
103
10
108
98
86
99
92
21,37
120
98
123
59
63
101
92
83
57
46,101
101
81
84
92
92
47
40,59,103
S2674
S2676
S2678
S2679
S2680
S2681
S2682
S2683
S2684
S2685
S2686
S2687
S2688
S2689
S2690
S2692
S2693
S2694
S2695
S2696
S2697
S2698
S2699
S2700
S2703
S2704
S2711
S2713
S2714
S2717
S2718
S2719
S2720
S2722
S2725
S2726
S2727
S2728
S2729
S2730
S2731
S2732
S2735
S2736
S2738
S2739
S2740
S2741
S2742
117
42
45,46,79,94
66
42
4
4
71
79
61
48
114
66
9
97
32,36,48
83
123
115
4,8
14
96
5,8
41
31,35
75
89
61,93
89
123
69
69
54
99
42,69
56
24
24
11
26
62
10
66,71
48
45
5
70
77
66
S2743
S2744
S2745
S2746
S2747
S2748
S2749
S2750
S2751
S2752
S2753
S2754
S2755
S2757
S2758
S2759
S2760
S2761
S2762
S2765
S2767
S2768
S2769
S2770
S2773
S2774
S2775
S2776
S2777
S2778
S2779
S2781
S2782
S2783
S2784
S2788
S2789
S2791
S2792
S2796
S2797
S2799
S2801
S2802
S2803
S2804
S2805
S2806
S2807
4,8,10
70
11
54
30
117
5,9
75
66
24,30
29
46,94
25
113
5,13,93
5,84
103
30
36
121
3,93
66
19,27,32,33,35
70
123
27,29,34
63,94
115
90
103
84
45,94
123
8
24,30
29
48
59
117
49
117
117
33
5
107,113
80
75
49
54
S2808
S2811
S2812
S2814
S2816
S2817
S2818
S2819
S2820
S2821
S2823
S2824
S2826
S2827
S2840
S2841
S2842
S2843
S2845
S2851
S2853
S2857
S2859
S2863
S2866
S2867
S2870
S2871
S2872
S2882
S2886
S2890
S2891
S2893
S2895
S2896
S2897
S2898
S2899
S2900
S2902
S2904
S2906
S2907
S2911
S2912
S2913
S2914
S2915
10
7
44
2
30
8,13
84
103
42
85,117
11
101
25
7,93
106
37
18
13
20
49
119
97
19,29
101
116
25,49
5
112
55
101
77
42
36
14
25
20
20
73
40
113
49
71
104
75
59
104
94,101
122
112
146
S6001
S6003
S6005
S7000
S7001
S7008
S7009
S7010
S7012
S7013
S7015
S7017
S7020
S7022
S7023
S7024
S7028
S7029
S7032
S7034
S7037
S7039
S7041
S7046
S7047
S7048
S7049
S7051
S7059
S7060
S7062
S7063
S7064
S7066
S7067
S7070
S7077
S7079
S7083
S7085
S7086
S7087
S7090
S7092
S7093
S7096
S7097
S7099
S7100
97
111
56
36
55
41
46
46
86
85
46
46
86
42
45
50
5
77
86
44
88
22
50
94,110
67
77
119
42
111
41
86
12
14
90
30
85
63
86
36
88
88
13
62
90
63
88
60
110
44
S7101
S7103
S7105
S7109
S7110
S7111
S7112
S7113
S7114
S7118
S7120
S7121
S7122
S7127
S7129
S7130
S7132
S7133
S7134
S7135
S7136
S7140
S7144
S7149
S7150
S7152
S7153
S7155
S7156
S7158
S7160
S7162
S7164
S7165
S7166
S7167
S7168
S7169
S7170
S7173
S7177
S7178
S7179
S7185
S7194
S7195
S7200
S7204
S7206
57
2
44
92
85
117
60
86
65
100
86
54
61
11
92
91
91
91
91
91
13
92
48
45
60
85
73
120
120
65
90
63
86
86
13
33
88
88
52
42
103
71
103
116
39
72
44
62
22
S7210
S7212
S7214
S8000
S8001
S8002
S8003
S8004
S8005
S8006
S8007
S8008
S8009
S8014
S8015
S8019
S8022
S8023
S8024
S8028
S8030
S8031
S8032
S8034
S8037
S8038
S8040
S8042
S8043
S8047
S8048
S8049
S8058
S8061
S8064
S8067
S8069
S8070
S8071
52
90
56
45,94
84
5
31
49
50
86
12
63
25
108
37,55
11
103
32
28,34,35
100
104
60
41
114
45
77
9
37
83
63
44
83
65
44
59
104
86
86
86
147
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