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.

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).

Cell permeable: yes

Primary Target
Cdk1/cyclin B, Cdk2/cyclin A3

Product competes with ATP.

Reversible: no

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

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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.

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

Toxicity: Carcinogenic / Teratogenic (D)