A cell-permeable pyridinylpyrazinecarboxamide compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of GSK-3b (Ki=4.9nM) with ~110-fold greater selectivity over Cdk2 (Ki=540nM). Shows only a trivial effect on the activities of 26-related kinases at much higher doses. Blocks GSK-3b-mediated phosphorylation of Ser396 in stably transfected 3T3 fibroblasts expressing four-repeat tau protein (IC50=76nM). Readily crosses blood-brain barrier and exhibits desirable bioavailability and aqueous solubility.
Formula:C₂₁H₂₃N₇O₃S• 2.5 HCl•5H₂O
Primary Target:GSK-3b
Solubility:DMSO
Molecular Weight:634.8
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
