Biochem/physiol Actions
Primary TargetCdk9
Reversible: no
Target IC50: 350 nM, using Cdk9/T1
Product competes with ATP.
Cell permeable: yes
General description
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 µM, respectively) and shows little or no activity against eight other commonly studied kinases even at concentrations as high as 10 µM. Shown to exhibit antiproliferative activity in human tumor cell lines.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Krystof, V., et al. 2006. J. Med. Chem.49, 6500.
Packaging
Packaged under inert gas
5 mg in Plastic ampoule
Warning
Toxicity: Irritant (B)
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