GSK-3β Inhibitor I

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.

Cell permeable: no

Primary Target
Gsk-3β

Product does not compete with ATP.

Reversible: no

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

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

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.

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

Toxicity: Standard Handling (A)