Biochem/physiol Actions

Reversible: no

Product competes with ATP.

Target K_i: 2 nM and 4 nM against Cdk2/E and Cdk9/T1, respectively

Cell permeable: yes

Primary TargetCdk2/E and Cdk9/T1

General description

A cell-permeable aminopyrimidinyl compound that acts as a potent and ATP-competitive inhibitor of Cdk2/E and Cdk9/T1 (K_i = 2 nM and 4 nM, respectively). It also inhibits GSK-3β, Cdk4/D₁, Cdk7/H, Cdk1/B, and Abl at higher concentrations (K_i = 20, 53, 70, 80, and 160 nM, respectively), but exhibits little activity towards 9 other kinases (K_i >1.0 µM). Shown to inhibit phosphorylation of cellular Cdk substrates, pRb and RNA polymerase II, and Cdk2-mediated S-phase transition.

Legal Information

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

Other Notes

Kontopidis, G., et al. 2006. Chem. Biol.13, 201.Wang, S., et al. 2004. J. Med. Chem.47, 1662.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

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)