Purity ~99% (HPLC). A cell-permeable pyrrolopyrazole that acts as a potent inhibitor against p21-activated kinases (Ki innM/[ATP] inuM = 13.7/200, 18.7/40, 18.1/80. 17.1/72, respectively, in PAK1, PAK4, PAK5, PAK6 kinase assays; IC50 = 190 and 99nM against PAK1 and PAK3, respectively) by directly targeting the kinase ATP-binding site in a reversible manner (Kd = 4.5nM using rhPAK4300-591 kinase domain). Inhibits PAK4-dependent cellular signaling (IC50 = 24.2nM against TNFalpha-stimulated NF-kappa-B activity in HEK293T) and proliferation (IC50 = 0.24 and 27nM, respectively, against HCT116 and A549 colonies formation) in vitro and the growth of human tumors in nude mice in vivo (10 to 25mg/kg; b.i.d. p.o). Alternate Names: (S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-(2-methylthieno[3,2-d]pyrimidin-4-ylamino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, PAK Inhibitor II, PF3758309
Size
5mg
Concentration
n/a
Applications
n/a
Other Names
p21-Activated Kinase Inhibitor II, PF-3758309 (PAK Inhibitor II, PF3758309, (S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-(2-methylthieno[3,2-d]pyrimidin-4-ylamino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide)