Biochem/physiol Actions

Primary TargetGSK-3β, Cdk1/cyclin B

Reversible: yes

Product competes with ATP.

Target IC₅₀: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively

Cell permeable: yes

General description

A cell-permeable, potent, reversible, and ATP competitive inhibitor of cdk1/cyclin B (IC₅₀ = 35 nM) and GSK-3β (IC₅₀ = 4 nM). One of the most active paullones that acts by competing with ATP for binding to GSK-3β and inhibits the phosphorylation of tau. Also inhibits the activity of Cdk5/p25-dependent phosphorylation of DARPP-32 (a 32 kDa dopamine and adenosine 3′,5′-monophosphate-regulated phosphoprotein). Displays remarkable antitumor activity in vitro. Inhibits growth of the colon cancer cell line HCT-116, with an IC₅₀ in the nanomolar range.

A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC₅₀ = 4 nM) and Cdk1/cyclin B (IC₅₀ = 35 nM). Displays remarkable in vitro antitumor activity. Inhibits Tau phosphorylation at sites that are typically phosphorylated by GSK-3β in Alzheimer's disease. Also inhibits Cdk5/p25-dependent phosphorylation of DARPP-32.

Legal Information

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

Other Notes

Leost, M., et al. 2000. Eur. J. Biochem.267, 5983.Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.

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 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)