Biochem/physiol Actions

Reversible: no

Target K_i: 25 nM against GSK-3β

Product competes with ATP.

Primary TargetGsk-3β

Cell permeable: yes

General description

A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and ATP-competitive inhibitor of GSK-3β (K_i = 25 nM) and minimally inhibits a panel of 79 commonly studied protein kinases, including several PKC isozymes. Shown to increase intracellular glycogen synthase activity in HEK293 cells with an EC₅₀ of 32 nM and demonstrate metabolic stability in human liver microsomes (HLM; t_1/2 >100 min).

A cell-permeable, potent, specific, and ATP-competitive inhibitor of GSK-3β (K_i = 25 nM) that exhibits minimal inhibition against a panel of 79 commonly studied protein kinases, including several PKC isozymes. Shown to increase intracellular glycogen synthase activity in HEK293 cells (EC₅₀ = 32 nM) and demonstrate metabolic stability in human liver microsomes (HLM; t_1/2 >100 min).

Legal Information

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

Other Notes

Justman, Q.A., et al. 2009. Science324, 509.O′Neill, D.J., et al. 2004. Bioorg. Med. Chem.12, 3167.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)