IM-12

Description

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.

The Uses of IM-12

3-((4-Fluorophenethyl)amino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione acts as an enhancer of Wnt signalling, involved in cell proliferation or differentiation, via inhibition of glycogen synthase kinase 3 beta (GSK-3β).

Definition

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.

References

[1]. schmöle 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.