EPZ-6438
Catalog #
27626-1
$195
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Description
EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 (Ki = 2.5 nM).
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Synonyms
E-7438; 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
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥99% by HPLC
Target(s)
EZH2
Formula
C34H44N4O4
MW
572.7 Da
Solubility
Soluble in EtOH
Biological Activity
EPZ-6438 is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and over 4,500-fold selectivity relative to 14 other HMTs.
CAS Registry #
1403254-99-8
Background
EPZ-6438 competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and also non-competitively binds to the binding sites of peptide or nucleosome substrate. EPZ-6438 selectively inhibits EZH2 with selectivity 35-fold greater than EZH1. Study results have suggested that EPZ-6438 exhibits dramatic and permanent anti-tumor activity in MRT models through synergistic effects of EPZ-6438-mediated EZH2 inhibition on several cancer pathways.
References
Knutson, SK, et al. PNAS 2013; 110(19): 7922-7927.
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