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Datasheet of IPA-3

Description:
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). in
vitro: Saturable binding of IPA-3 to full-length Pak1 was observed with an apparent dissociation constant of 1.92 0.2 M,
consistent with the reported IC50 of 2.5 M. IPA-3 bound the isolated RD with an even higher apparent affinity (0.1 0.01
M) whereas the kinase domain showed a weaker interaction. IPA-3 blocks activation of PAK2 at Ser192/197 that antagonises
PAK's interaction with Pix. Accordingly, Pix-mediated Rac1 activation is decreased in IPA-3 treated schwannoma cells,
indicating that PAK acts upstream of Rac. In K562 cells, both chorein silencing and PAK1 inhibition with IPA-3 decreased
phosphorylation of Bad, a Bcl2-associated protein, promoting apoptosis by forming mitochondrial pores, followed by
mitochondrial depolarization, DNA fragmentation, and phosphatidylserine exposure at the cell surface, all hallmarks of apoptosis.
in vivo: Inhalation of the small molecule synthetic Pak1 inhibitor, IPA3, also significantly reduced in vivo airway responsiveness
to ACh and 5-hydroxytryptamine (5-Ht) in wild type mice. IPA3 inhibited the contractility of isolated human bronchial tissues to
ACh, confirming that this inhibitor is also effective in human airway smooth muscle tissue.

Chemical Information
Catalog

DC9575

Purity of current batch:

>98%

Molecular Weight (MW)

350.45

Molecular Formula

C20H14O2S2

CAS No.

42521-82-4

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.