Description General description 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. 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. Packaging 1 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target GSK-3β, Cdk1/cyclin B Product competes with ATP. Reversible: yes Target IC50: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively Packaging Packaged under inert gas Warning Toxicity: Standard Handling (A) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Other Notes Leost, M., et al. 2000. Eur. J. Biochem.267, 5983. Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.