IM-12

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).^1,2 It has been shown to reduce proliferation and increase differentiation of a ReNCell VM cell line derived from human ventral midbrain.² IM-12 is also reported to have a depolymerizing effect on in vitro tubulin assembly.³

WARNING This product is not for human or veterinary use.

1. Brennführer, A., Neumann, H., Pews-Davtyan, A., et al. Catalytic and stoichiometric synthesis of novel 3-aminocarbonyl-, 3-alkoxycarbonyl-, and 3-amino-4-indolylmaleimides. The Journal of Organic Chemistry 2009(1), 38-42 (2009).

2. Schmöle, A.C., Brennführer, A., Karapetyan, G., et al. Novel indolylmaleimide acts as GSK-3β inhibitor in human neural progenitor cells. Bioorg. Med. Chem. 18(18), 6785-6795 (2010).

3. Eisenlöffel, C., Schmöle, A.C., Pews-Davtyan, A., et al. Interference of a novel indolylmaleimide with microtubules induces mitotic arrest and apoptosis in human progenitor and cancer cells. Biochem. Pharmacol. 85(6), 763-771 (2013).