1129669-05-1

Glycogen synthase kinase 3β (GSK3β) is a constitutively active serine/threonine protein kinase implicated in several important regulatory processes. It can phosphorylate β-catenin, an intracellular signal transducer in the Wnt signaling pathway, which leads to β-catenin degradation. IM-12 is a non-symmetrically substituted indolylmaleimide that increases β-catenin levels by inhibiting GSK3β (IC₅₀ = 53 nM). It has been shown to reduce proliferation and increase differentiation of a ReNCell VM cell line derived from human ventral midbrain. IM-12 is also reported to have a depolymerizing effect on in vitro tubulin assembly.

GSK-3β inhibitor (IC50=53nM (enzymatic), 3.8μM (cellular)). The compound significantly increases β-catenin levels, leads to TCF-induction and promotes neuronal differentiation in human neural progenitor cells via activation of canonical Wnt signaling.

ChEBI: 3-[2-(4-fluorophenyl)ethylamino]-1-methyl-4-(2-methyl-1H-indol-3-yl)pyrrole-2,5-dione is an organonitrogen compound, an organooxygen compound and a member of maleimides. It is functionally related to an alpha-amino acid.

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[1]. schm?le ac, brennführer a, karapetyan g, et al. novel indolylmaleimide acts as gsk-3beta inhibitor in human neural progenitor cells. bioorg med chem, 2010, 18(18): 6785-6795.