GSK503

GSK503 is a potent and selective small molecule inhibitor of the Enhancer of zeste homolog 2 (EZH2) methyltransferase, an enzyme responsible for the trimethylation of histone H3 at lysine 27 (H3K27me3). Developed by GSK, this research compound demonstrates high potency against both wild-type and mutant forms of EZH2, with significant selectivity over EZH1 and other histone methyltransferases. In preclinical models, GSK503 has shown efficacy in reducing H3K27me3 levels, impairing cancer cell proliferation, and suppressing tumor growth and metastasis, particularly in melanoma, diffuse large B-cell lymphoma (DLBCL), and multiple myeloma. It is primarily used as a chemical probe in epigenetic research and has not advanced to clinical trials.

Other names

CAS 1346572-63-1CAS1346572-63-1CAS-1346572-63-1