LY2090314

LY2090314 is a potent, selective small molecule inhibitor of glycogen synthase kinase-3 (GSK-3), targeting both GSK-3α and GSK-3β isoforms with nanomolar potency. Developed by Eli Lilly, it acts as an ATP-competitive inhibitor, preventing GSK-3-mediated phosphorylation of beta-catenin. This inhibition stabilizes beta-catenin and activates the Wnt/beta-catenin signaling pathway, leading to apoptosis in susceptible tumor cells. LY2090314 has demonstrated antineoplastic activity in preclinical models and was investigated for the treatment of various cancers including leukemia (acute myeloid leukemia and acute promyelocytic leukemia) and pancreatic cancer. Clinical development reached up to phase 2 trials but was discontinued for these indications.

Other names

ly2090314ly-2090314ly 2090314