General description

A cell-permeable indolylmaleimide derivative and SB-216763 analog that acts as a GSK-3β inhibitor, with an IC₅₀ of 53 nM in an in vitro binding assay, compared with 92 nM for SB-216763 in the same assay condition, and reduces GSK-3β activity to 27% in an enzymatic assay at 3 µM concentration. It is shown to attenuate hNPC (human neural progenitor cells) cell proliferation, and enrich β-catenin around the nucleus of ST14 cells in the same extent of SB-216763. Furthermore, it can mimic the effect of stabilized β-catenin, up-regulates TCF-activity in a luciferase reporter gene assay, and enhances human progenitor cell differentiation.

Legal Information

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

Other Notes

Schmole, AC., et al. 2010. Bioorg. Med. Chem.18, 6785.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)