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Cat. No. Name Size Price Add Cart
KI2263EPZ0056875 mg$432
EPZ00568725 mg$1552

Chemical Characteristic

Product NameEPZ005687
SynonymsN/A
CAS No.1396772-26-1
Molecular Weight 539.67
FormulaC32H37N5O3
Chemical Name1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide
Smilesn1(ncc2c(cc(cc12)c1ccc(cc1)CN1CCOCC1)C(=O)NCc1c(=O)[nH]c(cc1C)C)C1CCCC1
Chemical Structure

Biological activities

EPZ005687 is a potent and selective small-molecule inhibitor of enhancer of zeste homolog 2 (EZH2). EPZ005687 inhibits polycomb-repressive complex 2 (PRC2) enzymatic activity with an IC50 of 54 nM. EPZ005687 inhibits PRC2 by competitively binding the S-adenosylmethionine (SAM)-binding site with a Ki of 24 nM. EPZ005687 specifically inhibits H3K27 methylation in lymphoma cells. EPZ005687 decreases proliferation in mutant but not wild-type EZH2 lymphoma cells.[1] EPZ005687 decreases cell proliferation in two non-Hodgkin's lymphoma (NHL) cell lines with activating mutations but not in a cell line containing wild-type EZH2. [2]

References

[1] Knutson SK, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012, 8(11): 890-896.
[2] Kotz J, et al. EZH2 moves. Science-Business eXchange. 2012, 18: 1-2.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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