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PAK inhibitors act on p21-activated kinases (PAK), effector kinases of the small GTPases Rac and Cdc42. The first family member was described in 1994 as a brain serine/threonine kinase activated by Cdc42 and Rac1. Group I PAKs (PAK1 to PAK3) are held inactive by an autoinhibitory region, whereas group II PAKs (PAK4 to PAK6) are regulated differently. PAK signaling remodels the actin cytoskeleton and contributes to cell motility and neurite outgrowth. IPA-3, reported in 2008, blocks PAK1 activation by targeting this autoregulatory mechanism. NVS-PAK1-1 is a further allosteric PAK1 inhibitor, and FRAX486 and FRAX597 act mainly on group I PAKs. PF-3758309 was developed against PAK4, while KPT 9274 inhibits PAK4 and nicotinamide phosphoribosyltransferase (NAMPT).
