EPZ005687
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.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1892145
| Cas No. |
1396772-26-1 |
|---|---|
| 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 |
| Appearance |
white powder |
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.
