MilliporeSigma™ Calbiochem™ p21-Activated Kinase Inhibitor II, PF-3758309
p21-Activated Kinase Inhibitor II, PF-3758309, CAS 898044-15-0, is a cell-permeable, reversible, potent inhibitor of p21-activated kinases (IC50 = 190 and 99nM against PAK1 and PAK3, respectively).
Supplier: MilliporeSigma™ 5.00613.0001
DescriptionA cell-permeable pyrrolopyrazole that acts as a potent inhibitor against p21-activated kinases (Ki in nM/[ATP] inμM = 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 ( K d = 4.5nM using rhPAK4300-591 kinase domain). Inhibits PAK4-dependent cellular signaling (IC50 = 24.2nM 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 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.
|99% by HPLC|
|Protect from light|
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