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EPZ-005687 is a highly selective inhibitor of mutant EZH2, a histone methyltransferase (HMT) that exhibits point mutations at key residues Tyr641 and Ala677 in non-Hodgkin’s lymphoma and other cancers. EPZ-005687 displays anticancer chemotherapeutic activity through its inhibition of EZH2; this enzyme is responsible for methylation of lysine and arginine residues and controls gene transcription fidelity in cells. Inhibition of mutant EZH2 induces apoptosis.
| Cas No. | 1396772-26-1 |
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| Purity | ≥99% |
| Formula | C32H37N5O3 |
| Formula Wt. | 539.67 |
| IUPAC Name | 1-cyclopentyl-N-[(4, 6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl) phenyl]indazole-4-carboxamide |
| Solubility | DMSO 2 mg/mL (3.7 mM) Water Insoluble Ethanol Insoluble |
| Appearance | white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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Knutson SK, Wigle TJ, Warholic NM, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6. PMID: 23023262.