LY-2090314 is a diazepinoindole compound with substituents at positions 2, 7, and 9: piperidin-1-ylcarbonyl, 4-(imidazo[1,2-a]pyridin-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl, and fluoro, respectively. It is a potent ATP-competitive inhibitor of GSK-3 with IC50 values of 1.5 nM (GSK-3α) and 0.9 nM (GSK-3β). In clinical development for advanced/metastatic cancer, it acts as an apoptosis inducer, antineoplastic agent, Wnt signalling activator, and tau-protein kinase inhibitor. It is classified as an imidazopyridine, diazepinoindole, monofluorobenzene, piperidinecarboxamide, urea, and maleimide.
