EPZ6438
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1403254-99-8
≥98%
A crystalline solid
C34H44N4O4
572.7
n-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2h-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide, tazemetostat
- MSDS: View or download
An EZH2 inhibitor (IC50 = 11 nM); inhibits mutant EZH2, including EZH2A677G, EZH2A687V, and EZH2Y641F, and EZH2Y641S (IC50s = 2, 2, 14, and 4 nM, respectively); selective for wild-type and mutant EZH2 over EZH1 (IC50 = 392 nM) and a variety of other histone methyltransferases (IC50s = >50 or >100 µM for all); reduces H3K27me3 levels in various lymphoma cell lines expressing wild-type or mutant EZH2 (IC50s = 2-8 and 2-22 nM, respectively); inhibits proliferation of various lymphoma cell lines expressing wild-type or mutant EZH2 (IC50s = 0.099-6.2 and 0.00049-5.8 µM, respectively); induces insulin production and glucose-stimulated insulin secretion in human pancreatic exocrine cells isolated from juvenile patients with type 1 diabetes or adults without diabetes at 1 µM; reduces H3K27me3 levels and induces insulin secretion and glucose-stimulated insulin secretion in human pancreatic ductal epithelial cells in vitro
