p21-Activated kinases (PAKs) are STE20 serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAKs results in release of an autoinhibitory domain that blocks activity of the kinase domain. PAKs are upregulated in several human cancers and are potential therapeutic...

Description: PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition. Target: Apoptosis, PAK. Smiles: CN(C)C[C@@H](NC(=O)N1Cc2c(Nc3nc(C)nc4ccsc34)n[nH]c2C1(C)C)c1ccccc1. References: Murray BW, et al. Proc Natl Acad Sci U S A, 2010, 107(20), 9446-9451.