Product Name: EPZ-005687
 CAT#: A-1415

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  Synonym:EPZ005687

EPZ-005687 Chemical Structure
EPZ-005687 chemical structure


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IUPAC/Chemical name: 1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide

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Biological Activity
EPZ-005687 is a selective EZH2 inhibitor.

A 10 mM (2 mg in 370 µl) solution of the EZH2 inhibitor EPZ-005687 (Cat. No. 2364) in anhydrous DMSO> EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against the closely related enzyme EZH1. The compound reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells.
Technical Data

Chemical Formula: C32H37N5O3
Molecular Weight: 539.67
Purity: >99%
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 3 years.

Reference
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
Nature Chemical Biology 8, 890–896 (2012) doi:10.1038/nchembio.1084
EZH2 catalyzes trimethylation of histone H3 lysine 27 (H3K27). Point mutations of EZH2 at Tyr641 and Ala677 occur in subpopulations of non-Hodgkin's lymphoma, where they drive H3K27 hypertrimethylation. Here we report the discovery of EPZ005687, a potent inhibitor of EZH2 (Ki of 24 nM). EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against the closely related enzyme EZH1. The compound reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells. These data suggest that genetic alteration of EZH2 (for example, mutations at Tyr641 or Ala677) results in a critical dependency on enzymatic activity for proliferation (that is, the equivalent of oncogene addiction), thus portending the clinical use of EZH2 inhibitors for cancers in which EZH2 is genetically altered.


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