GSK-3beta Inhibitor XI - CAS 626604-39-5 - Calbiochem

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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Gsk-3β

Product competes with ATP.

Reversible: no

Target K_i: 25 nM against GSK-3β

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

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

Other Notes

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

Legal Information

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