EPZ6438
EPZ-6438 is an inhibitor of EZH2, a histone methyltransferase (HMT) responsible for methylation of lysine and arginine residues and controls gene transcription fidelity in cells. EPZ-6438 displays anticancer chemotherapeutic activity in in vivo models by inducing regression of malignant or atypical teratoid rhabdoid tumors containing altered or mutant SWI/SNF ATP-dependent chromatin remodelers.
References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/1892150
Cas No. |
1403254-99-8 |
---|---|
Purity |
≥99% |
Formula |
C34H44N4O4 |
Formula Wt. |
572.74 |
IUPAC Name |
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide |
Synonym |
E7438 |
Solubility |
In DMSO |
Appearance |
white powder |
Knutson SK, Warholic NM, Wigle TJ, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. PMID: 23620515.