Biochem/physiol Actions

Cell permeable: no

Reversible: no

Target IC₅₀: 2 µM, 673 nM, 1.4-5.5 µM, against GSK-3β, Flt-3, and PKC activities, respectively

Product does not compete with ATP.

Primary TargetGsk-3β

General description

A cell-permeable, thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP-competitive inhibitor of GSK-3β (IC₅₀ = 2 µM). Inhibits Flt-3 and PKC activities (IC₅₀ = 673 nM and 1.4-5.5 µM, respectively). Does not significantly affect the activities of Cdk1/cyclin B, CK-II, PKA, or PKC (IC₅₀ >100 µM). Shown to inhibit collagen- and thrombin-induced platelet aggregation.

A thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP competitive inhibitor of GSK-3β (IC₅₀ = 2 µM). Inhibits Flt-3 and PKC activities (IC₅₀ = 673 nM and 1.4-5.5 µM, respectively). Does not significantly affect the activities of Cdk-1/cyclin B, CK-II, and PKA, (IC₅₀ >100 µM). Binds to the active site of GSK-3β.

Legal Information

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

Other Notes

Guzman, M.L., et al. 2007. Blood110, 4436.Barry, F.A., et al. 2003. FEBS Lett.553, 173.Martinez, A., et al. 2002. J. Med. Chem.45, 1292.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

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)