EPZ-5676

• CAT Number: I001465
• CAS Number: 1380288-87-8
• Molecular Formula: C₃₀H₄₂N₈O₃
• Molecular Weight: 562.71
• Purity: ≥95%
• Synonyms: (2R,3S,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol
• Target: Histone Methyltransferase
• Solubility: DMSO: ≥ 47.8 mg/mL
• Storage: 3 years -20C powder
• IC50: 80 pM (Ki value) [1]
• IUPAC Name: (2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol
• InChI: InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17-,19+,22-,25-,26-,29-/
• InChIKey: LXFOLMYKSYSZQS-LURJZOHASA-N
• SMILES: CC(C)(C)C1=CC2=C(NC(CC[[email protected]]3C[[email protected]@H](N(C[[email protected]@H]4[[email protected]@H](O)[[email protected]@H](O)[[email protected]](N5C(N=CN=C6C6N)=C6N=C5)O4)C(C)C)C3)=N2)C=C1

EPZ-5676(CAT: I001465), also known as Tazemetostat, is a potent and selective inhibitor of the histone methyltransferase enhancer of zeste homolog 2 (EZH2). It is extensively studied for its role in epigenetic modulation, particularly in cancers with EZH2 gain-of-function mutations, such as non-Hodgkin’s lymphoma and certain solid tumors. By inhibiting EZH2, EPZ-5676 reduces H3K27 trimethylation, reactivating tumor suppressor genes and altering cancer cell proliferation. Its specificity and efficacy make it a valuable tool in exploring EZH2-related pathways, advancing research in cancer epigenetics, and developing targeted therapies. EPZ-5676 is also used in preclinical and clinical studies to investigate its therapeutic potential in diverse malignancies.