MilliporeSigma™ Calbiochem™ p21-Activated Kinase Inhibitor II, PF-3758309

Description

• A cell-permeable pyrrolopyrazole that acts as a potent inhibitor against p21-activated kinases (K i in nM/[ATP] inμM = 13.7/200, 18.7/40, 18.1/80
• 17.1/72, respectively, in PAK1, PAK4, PAK5, PAK6 kinase assays; IC 50 = 190 and 99nM against PAK1 and PAK3, respectively) by directly targeting the kinase ATP-binding site in a reversible manner ( K d = 4.5nM using rhPAK4 300-591 kinase domain)
• Inhibits PAK4-dependent cellular signaling (IC 50 = 24.2nM against TNFα-stimulated NF-κB activity in HEK293T) and proliferation (IC 50 = 0.24 and 27 nM, 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)
• Please note that the molecular weight for this compound is batch-specific due to variable water content
• Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight
• The molecular weight provided represents the baseline molecular weight without water.