Biochem/physiol Actions
Reversible: no
Product competes with ATP.
Primary TargetCdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9
Target IC50: 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively
Cell permeable: yes
General description
A cell-permeable pyrazolo-pyrimidinone compound that acts as a potent, selective, and ATP-competitive inhibitor of Cdks (IC50 = 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively). It inhibits Cdk4/D1, Cdk6/D3, and GSK-3β only at much higher concentrations (IC50 = 839 nM, 282 nM, and 754 nM, respectively) and exhibits little activity towards a panel of 60 other kinases. A broad-spectrum growth inhibitor toward tumor cells, but not non-transformed quiescent fibroblasts.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Caligiuri, M., et al. 2005. Chem. Biol.12, 1103.
Packaging
1 mg in Plastic ampoule
Packaged under inert gas
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria to qualify for the following awards: