InSolution Cdk1 Inhibitor IV; RO-3306

Biochem/physiol Actions

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

Primary TargetCdk1/B1 and Cdk1/A

Reversible: yes

Cell permeable: yes

Secondary TargetCdk2/E, PKCδ, and SGK

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 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.

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

Packaged under inert gas

2 mg in Glass bottle

Physical form

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

Reconstitution

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

Warning

Toxicity: Irritant (B)