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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 µ,M inhibitor, IC50 = 2.5 µ,M for PAK1). Specificity test shows >= 50% inhibition, in the presence of 10 µ,M ATP and inhibitor, against 9 of 214 non-PAK human kinases. Shown to effectively suppress both basal and PDGF-induced PAK activation at 30 µ,M 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.