Biochem/physiol Actions
Target IC50: 15 nM against Chk1 phosphorylation of cdc25C; 23 nM, 5.6 nM, 16 nM, against CDK1, CDK2, CDK4, respectively
Reversible: yes
Product competes with ATP.
Primary TargetChk1
Cell permeable: yes
General description
A cell-permeable, ATP-competitive, and reversible indolocarbazole derivative that acts as a potent and selective inhibitor of checkpoint kinase (Chk1) in vitro. It inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. However, SB-218078 is a much weaker inhibitor of Cdc2 (IC50 = 250 nM) and PKC (IC50 = 1 µM).
A cell-permeable, ATP competitive, and reversible indolocarbazole derivative that acts as a potent inhibitor of checkpoint kinase (Chk1) in vitro (Ki = 15 nM). Binds to the ATP-binding pocket of Chk1, producing only slight changes in the protein conformation. Also inhibits the activity of CDK1 (Ki = 23 nM), CDK2 (Ki = 5.6 nM), and CDK4 (Ki = 16 nM). Inhibits Chk1 phosphorylation of Cdc25C (IC50 = 15 nM).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Zhao, B., et al. 2002. J. Biol. Chem.277, 46609.Jackson, J.R., et al. 2000. Cancer Res.60, 566
Packaging
1 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: Standard Handling (A)
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