IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27.
IHMT-337 demonstrates excellent selectivity for EZH2 over a wide range of methyltransferases including EZH1, covalently binds to EZH2 at Cys663 residue in SET domain.
IHMT-337 showed comparable effects on H3K27me3 levels in different DLBCL cell lines in a dose-dependent manner, compared to EPZ6438 and GSK126.
IHMT-337 robustly impaired EZH2-dependent DLBCL cell proliferation with similar GI50s.
IHMT-337 (10 uM, 24 h) degrades EZH2 through CHIP E3 ligase-mediated proteasome pathway in both Pfeiffer and MDA-MB-231 cells.
IHMT-337 inhibits breast cancer cell proliferation by degrading EZH2, a CDK4 transcription factor.
IHMT-337 inhibits cell proliferation in different preclinical models in vitro and in vivo.
