Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target IC₅₀: 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1

Primary TargetCdk2/A, Cdk2/E

Cell permeable: yes

General description

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC₅₀ = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC₅₀ >1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC₅₀ = ~1.25-20 µM) in vitro and prevent neointima formation in vivo.

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC₅₀ = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC₅₀ >1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC₅₀ ~1.25-20 µM) in vitro and prevent neointima formation in vivo.

Legal Information

Sold under license of U.S. Patents 6,617,331 and 6,803,371.

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

Other Notes

Bhattacharjee, R.N., et al. 2001. Mol. Cell. Biol.21, 5417.Brooks, E.E., et al. 1997. J. Biol. Chem.272, 29207.

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 3 months at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)