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 M). 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. The solid form of this compound (Cat. No. 217699) is also available.

Cell permeable: yes

Primary Target
Cdk1/B1 and Cdk1/A

Reversible: yes

Secondary Target
Cdk2/E, PKCδ, and SGK

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

Packaged under inert gas

Toxicity: Irritant (B)

A 10 mM (2 mg/569 L) solution of Cdk1 Inhibitor IV, RO-3306 (Cat. No. 217699) in DMSO.

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.

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

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