Share this post on:

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.

GSK-2830371