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Chemical Structure : IHMT-337
Catalog No.: PC-49674Not For Human Use, Lab Use Only.
IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27.
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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.
| M.Wt | 561.08 | |
| Formula | C31H33ClN4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Husheng Mei, et al. Signal Transduct Target Ther. 2023 Jan 16;8(1):18.
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