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.

Cell permeable: yes

Primary Target
GSK-3β

Reversible: yes

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)