Biochem/physiol Actions

Reversible: no

Product competes with ATP.

Target K_i: 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively

Primary TargetCdk1

Cell permeable: yes

General description

A cell-permeable quinolinyl thiazolinone compound that acts as a potent and ATP-competitive inhibitor of Cdk1 (K_i = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively). It affects Cdk2/E, PKCδ, and SGK only at much higher concentrations (K_i = 340, 318, and 497 nM, respectively), and shows little effect against Cdk4/D and six other commonly studied kinases (K_i ≥ 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).

Legal Information

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

Other Notes

Vassilev, L.T., et al. 2006. Proc. Natl. Acad. Sci. USA103, 10660.

Packaging

5 mg in Glass bottle

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: Irritant (B)