500613 Sigma-Aldrichp21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem

This product has been discontinued.

A cell-permeable pyrrolopyrazole that acts as a potent inhibitor against p21-activated kinases (K_i in nM/[ATP] in µM = 13.7/200, 18.7/40, 18.1/80. 17.1/72, respectively, in PAK1, PAK4, PAK5, PAK6 kinase assays; IC₅₀ = 190 and 99 nM against PAK1 and PAK3, respectively) by directly targeting the kinase ATP-binding site in a reversible manner (K_d = 4.5 nM using rhPAK4_300-591 kinase domain). Inhibits PAK4-dependent cellular signaling (IC₅₀ = 24.2 nM against TNFα-stimulated NF-κB activity in HEK293T) and proliferation (IC₅₀ = 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 25 mg/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.