Biochem/physiol Actions

Reversible: no

Product competes with ATP.

Primary TargetCdk1/cyclin B, Cdk2/cyclin A3

Target IC₅₀: 9.5 nM, 5.4 nM against Cdk1/cyclin B, Cdk2/cyclin A3, respectively

Cell permeable: yes

General description

A cell-permeable purine analog that displays anti-proliferative properties and acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC₅₀ = 9.5 nM and 5.4 nM, respectively). Displays greater selectivity for Cdk′s over other kinases tested (IC₅₀ = 30 nM, 600 nM, 800 nM, 900 nM, and 1.6 µM for Cdk2/A, ROCKII, PDK1, DYRK1A, and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth (GI₅₀ of 8 µM).

A cell-permeable 2,6-disubstituted purine compound that displays antiproliferative properties. Acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC₅₀ = 9.5 nM and 5.4 nM). Displays greater selectivity for Cdk1/2 over other kinases tested (IC₅₀ = 600 nM, 800 nM, 900 nM and 1.6 µM for ROCKII, PDK1, DYRK1A and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth with a GI₅₀ of 8 µM.

Legal Information

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

Other Notes

Hardcastle, I.R., et al. 2004. J. Med. Chem.47, 3710.Sayle, K.L., et al. 2003. Bioorg. Med. Chem. Lett.13, 3079.Davies, T.G., et al. 2002. Nat. Struct. Biol.9, 745.

Packaging

1, 5 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: Carcinogenic / Teratogenic (D)