Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Primary TargetGSK-3β

General description

A cell-permeable pyridinylpyrazinecarboxamide compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of GSK-3β (K_i = 4.9 nM) with ~110-fold greater selectivity over Cdk2 (K_i = 540 nM). Shows only a trivial effect on the activities of 26-related kinases at much higher doses. Blocks GSK-3β-mediated phosphorylation of Ser³⁹⁶ in stably transfected 3T3 fibroblasts expressing four-repeat tau protein (IC₅₀ = 76 nM). Readily crosses blood-brain barrier and exhibits desirable bioavailability and aqueous solubility.

Legal Information

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

Other Notes

Berg. S., et al. 2012. J. Med. Chem.55, 9107.

Packaging

Packaged under inert gas

10 mg in Glass bottle

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)