p21-Activated Kinase Inhibitor III; IPA-3

General description

A cell-permeable symmetrical disulfide allosteric inhibitor that selectively targets the autoregulatory domain of group I, but not group II, PAKs (p21-activated kinases) and prevents the activation of PAK1/2/3 (% inhibition= 95, 70, and 60, respectively, with 10 µM inhibitor; IC₅₀ = 2.5 µM for PAK1). Specificity test shows ≥ 50% inhibition, in the presence of 10 µM ATP and inhibitor, against 9 of 214 non-PAK human kinases. Shown to effectively suppress both basal and PDGF-induced PAK activation at 30 µM in mouse embryonic fibroblasts. IPA-3 does not inhibit the enzymatic activity of preactivated PAKs and reduction of the intramolecular disulfide bond of IPA-3 by DTT renders it inactive.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Deacon, S.W., et al. 2008. Chem. Biol.15, 322.

Packaging

Packaged under inert gas

5, 25 mg in Plastic ampoule

Warning

Toxicity: Irritant (B)