1139875-74-3

GSK3β inhibitor XVIII is an inhibitor of glycogen synthase kinase 3β (GSK3β; IC₅₀ = 64 nM). It induces expression of a luciferase reporter in HEK293 cells expressing wild-type Wnt (EC₅₀ = ~1.25 μM) but not in cells expressing a β-catenin/TCF binding site-mutant Wnt. GSK3β inhibitor XVIII increases β-catenin accumulation in the nucleus of HEK293 cells. It induces proliferation of R7T1 β-cells (EC₅₀ = 1,143 nM), an effect that can be blocked by the COX and Wnt signaling inhibitor sulindac , and rat primary β-cells.

GSK-3β inhibitor 8, a thiophenacil derivative, is an effective and selective inhibitor of GSK-3β (IC50=64 nM). GSK-3β inhibitor 8 negatively regulated Wnt signaling pathway and stimulated β cell proliferation[1][2].

GSK-3β: 64 nM (IC₅₀)

[1] Wang W, et al. Identification of small-molecule inducers of pancreatic beta-cell expansion. Proc Natl Acad Sci U S A. 2009 Feb 3;106(5):1427-32. DOI:10.1073/pnas.0811848106