General description
A cell-permeable quinolinyl thiazolinone compound that acts as a potent and ATP-competitive inhibitor of Cdk1 (Ki = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively). It affects Cdk2/E, PKCδ, and SGK only at much higher concentrations (Ki = 340, 318, and 497 nM, respectively), and shows little effect against Cdk4/D and six other commonly studied kinases (Ki ≥ 2 µM). Short-term treatment for up to 20 hrs results in fully reversible G2/M cell cycle arrest, while prolonged treament (>48 hrs) results in apoptotic cell death in proliferating cancer cells, but not in nontumorigenic epithelial cell lines. Also available as a 10 mM solution in DMSO (Cat. No. 217721).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk1
Product competes with ATP.
Reversible: no
Target Ki: 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Vassilev, L.T., et al. 2006. Proc. Natl. Acad. Sci. USA103, 10660.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51112000
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 217699-5MG
