Activating the Wnt/β-Catenin Pathway for the Treatment of Melanoma – Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3
Fig 1
LY2090314 is a GSK inhibitor which elevated Wnt signaling in melanoma cell lines.
A. Structure of LY2090314. B. Riluzole (▲), LY2090314 (■) and BIA (●) activated the TCF/LEF luminescent reporter in A375 cells following 5 hours of drug exposure. C. LY2090314 (20nM) decreased phosphorylation of GSK3α/β in A375 cells and increased β-catenin and Axin2 protein levels as determined by Western blot. D. LY2090314 (20nM) treatment of A375 cells increased Axin2 gene expression in a time dependent manor. E. Uncomplexed β-catenin IP experiments reveal a large increase in β-catenin protein following LY2090314 (20nM) treatment for 48 hours.