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Beschreibung

A cell-permeable azo-pyrazole compound that acts as a potent, ATP-competitive, and Cdk9-selective inhibitor (IC50 = 350 nM, using Cdk9/T1). It inhibits Cdk1/B, Cdk2/E, Cdk2/A, Cdk4/D1, Cdk7/H, and p70S6K only at much higher concentrations (IC50 = 44, 20, 69, 13.5, 26, and 10 µ,M, respectively) and shows little or no activity against eight other commonly studied kinases even at concentrations as high as 10 µ,M. Shown to exhibit antiproliferative activity in human tumor cell lines.