EPZ005687
Catalog #
27624-1
$160
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Description
EPZ-005687 is a potent and selective inhibitor of EZH2.
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Synonyms
EPZ 005687; EPZ-005687; 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥98% by HPLC
Target(s)
EZH2
Formula
C32H37N5O3
MW
539.7 Da
Solubility
Soluble in DMSO
Biological Activity
Potent and selective EZH2 inhibitor with Ki of 24 nM. It exhibits 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
CAS Registry #
1396772-26-1
Background
EPZ005687 is a potent inhibitor of EZH2, an enzymatic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of histone H3 lysine 27 (H3K27), that inhibits EZH2 with Ki of 24 nM, which is 500-fold and 50-fold greater in selectivity than 15 other protein methyltransferases and closely related EZH1 respectively. EPZ005687 concentration-dependently inhibits the enzymatic activity of PRC2 with IC50 of 54 nM through binding to the S-adenosylmethionine (SAM) pocket of the EZH2 SET domain. Study results have shown that EPZ005687 reduces H3K27 methylation in a variety of lymphoma cells and induces apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells.
References
Knutson SK, et al. Nat Chem Biol. 2012 Nov;8(11):890-6.
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