General description
A cell-permeable aminopyrimidinyl compound that acts as a potent and ATP-competitive inhibitor of Cdk2/E and Cdk9/T1 (Ki = 2 nM and 4 nM, respectively). It also inhibits GSK-3β, Cdk4/D1, Cdk7/H, Cdk1/B, and Abl at higher concentrations (Ki = 20, 53, 70, 80, and 160 nM, respectively), but exhibits little activity towards 9 other kinases (Ki >1.0 µM). Shown to inhibit phosphorylation of cellular Cdk substrates, pRb and RNA polymerase II, and Cdk2-mediated S-phase transition.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk2/E and Cdk9/T1
Product competes with ATP.
Reversible: no
Target Ki: 2 nM and 4 nM against Cdk2/E and Cdk9/T1, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Kontopidis, G., et al. 2006. Chem. Biol.13, 201.
Wang, S., et al. 2004. J. Med. Chem.47, 1662.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41116113
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 238806-5MG