533379 Sigma-Aldrichp21-Activated Kinase Inhibitor III, FRAX597 - CAS 1286739-19-2 - Calbiochem

This product has been discontinued.

A cell-permeable, orally bioavailable, pyridopyrimidinone compound that acts as a potent, reversible, and ATP-competitive isoforms selective inhibitor of p21 activated kinase (PAK; IC₅₀ = 7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively). Binds to the back cavity of the ATP binding site of PAK1, and exhibits much reduced activity towards V342F and V342Y mutant forms of PAK1 (IC₅₀ = 3 and 2 µM, respectively). Does not affect the activity of PAK4, 6, and 7 (IC₅₀ > 10 µM). At higher concentrations (100 nM), is shown to cause over 80% inhibition of YES1, RET, CSF1R, and TEK. Reported to block the proliferation of schwannoma cell proliferation by blocking cell cycle at G1 phase. Also blocks the neurofibromatosis 2 (NF2)-associated tumor growth in mice (100 mg/kg, oral for 14 days).

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.