Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target IC₅₀: 20 nM against Cdk1/B

Primary TargetCdk1/B

Cell permeable: yes

General description

A cell-permeable, potent, reversible, and ATP-competitive inhibitor of Cdk1/cyclin B (IC₅₀ = 20 nM) that displays increased potency over purvalanol A (Cat. No. 540500; IC₅₀ = 50 nM), Roscovitine (Cat. No. 557360; IC₅₀ = 450 nM), Bohemine (Cat. No. 203600; IC₅₀ = 1.1 µM), and Olomoucine (Cat. No. 495620; IC₅₀ = 7.0 µM). Also exhibits greater in vitro cytotoxicity in various cancer cell lines (IC₅₀ = 3.0 µM, 5.3 µM, 6.3 µM, 6.3 µM, and 11.1 µM for CEM, MCF7, HOS, G631, and K562, respectively).

A cell-permeable 2,6,9-trisubstituted purine analog that acts as a potent, reversible, and ATP-competitive inhibitor of Cdk1/B with an IC₅₀ of 20 nM and displays increased potency over purvalanol A (Cat. No. 540500; IC₅₀ = 50 nM), Roscovitine (Cat. No. 557360; IC₅₀ = 450 nM), Bohemine (Cat. No. 203600; IC₅₀ = 1.1 µM) and Olomoucine (Cat. No. 495620; IC₅₀ = 7.0 µM). Further, exerts greater in vitro cytotoxicity in various cancer cell lines (IC₅₀ = 3.0 µM, 5.3 µM, 6.3 µM, 6.3 µM and 11.1 µM for CEM, MCF7, HOS, G631 and K562, respectively).

Legal Information

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

Other Notes

Krystof, V., et al. 2002. Bioorg. Med. Chem. Lett.12, 3283.

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)