GSK126

GSK126 is a **highly selective, small molecule inhibitor of the enhancer of zeste homolog 2 (EZH2) methyltransferase**, a histone methyltransferase and epigenetic regulator involved in gene silencing. GSK126 is S-adenosyl-methionine-competitive, with an in vitro IC50 of 9.9–17.4 nM and demonstrates preclinical antineoplastic activity by blocking the methylation of histone H3 (H3K27me3), suppressing tumor cell proliferation, and inducing apoptosis in multiple myeloma (MM), lymphoma, and other cancer cell models. GSK126 also impacts cell migration, angiogenesis, lipid metabolism, and immune cell function in the tumor microenvironment. Despite promising preclinical results, the drug's first-in-human phase I trial was terminated due to insufficient clinical activity and dose-limiting toxicity. GSK126 was originally developed by GSK for the treatment of refractory non-Hodgkin lymphoma, multiple myeloma, and various solid tumors, but is now primarily used as a chemical probe or tool compound in laboratory research[1][3][4][7][9].

Other names

EZH2 inhibitorEZH-2 inhibitorEZH 2 inhibitor(S)-1-(sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamideCAS#1346574-57-9