p21-Activated Kinase Inhibitor III, FRAX597

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).

p21-Activated Kinase Inhibitor III, FRAX597, CAS1286739-19-2, is a cell-permeable, potent, reversible, ATP-competitive inhibitor of PAK (IC₅₀ = 7.7, 12.8, & 19.3 nM for PAK1, 2, & 3, respectively).

Cell permeable: yes

Primary Target
p21 activated kinase

Target IC₅₀: 7.7, 12.8, and 19.3 nM for PAK1, 2, and 3, respectively

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Licciulli, S., et al. 2013. J. Biol. Chem.288, 29105.

Chow, H.Y., et al. 2012. Cancer Res.72, 5966.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)