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.
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Other Notes
Deacon, S.W., et al. 2008. Chem. Biol.15, 322.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 506106-25MG