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Beschreibung

A cell-permeable indolylmaleimide derivative and SB-216763 analog that acts as a GSK-3beta 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-3beta activity to 27% in an enzymatic assay at 3 µ,M concentration. It is shown to attenuate hNPC (human neural progenitor cells) cell proliferation, and enrich beta-catenin around the nucleus of ST14 cells in the same extent of SB-216763. Furthermore, it can mimic the effect of stabilized beta-catenin, up-regulates TCF-activity in a luciferase reporter gene assay, and enhances human progenitor cell differentiation.