Catalog No.: PC-43316Not For Human Use, Lab Use Only.
PF-3758309 (PF03758309) is a potent, ATP-competitive p21-activated kinase (PAK) inhibitor with Ki of 18.7 nM, shows similar enzymatic potency against other group B PAKs (PAK5 Ki=18.1 nM, PAK6 Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), less active against PAK2 and PAK3 (IC50=190 nM and 99 nM).
PF-3758309 (PF03758309) is a potent, ATP-competitive p21-activated kinase (PAK) inhibitor with Ki of 18.7 nM, shows similar enzymatic potency against other group B PAKs (PAK5 Ki=18.1 nM, PAK6 Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), less active against PAK2 and PAK3 (IC50=190 nM and 99 nM).
PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM).
PF-3758309 inhibits PAK4-dependent pathways in proteomic studies and regulates functional activities related to cell proliferation and survival; blocks the growth of multiple human tumor xenografts.
