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Beschreibung

A cell-permeable, potent, reversible, and ATP competitive inhibitor of cdk1/cyclin B (IC50 = 35 nM) and GSK-3&beta, (IC50 = 4 nM). One of the most active paullones that acts by competing with ATP for binding to GSK-3&beta, 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&prime,,5&prime,-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-3beta (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-3beta in Alzheimer's disease. Also inhibits Cdk5/p25-dependent phosphorylation of DARPP-32.