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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk2/A, Cdk2/E
Product competes with ATP.
Reversible: yes
Target IC50: 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1
Packaging
Packaged under inert gas
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Bhattacharjee, R.N., et al. 2001. Mol. Cell. Biol.21, 5417.
Brooks, E.E., et al. 1997. J. Biol. Chem.272, 29207.
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
- UPC:
- 41116113
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 238803-1MG