General description
A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and ATP-competitive inhibitor of GSK-3β (Ki = 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; t1/2 >100 min).
A cell-permeable, potent, specific, and ATP-competitive inhibitor of GSK-3β (Ki = 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; t1/2 >100 min).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Gsk-3β
Product competes with ATP.
Reversible: no
Target Ki: 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
- UPC:
- 51183800
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 361553-1MG