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EPZ005687
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EPZ005687图片
CAS NO:1396772-26-1
规格:98%
分子量:539.67
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
EZH2 inhibitor,potent and selective
CAS:1396772-26-1
分子式:C32H37N5O3
分子量:539.67
纯度:98%
存储:Store at -20°C

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 a value of inhibition constantKiof 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 a value of 50% inhibition concentration IC50of 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.


Reference


?[1].Knutson SK, Wigle TJ, Warholic NM, Sneeringer CJ, Allain CJ, Klaus CR, Sacks JD, Raimondi A, Majer CR, Song J, Scott MP, Jin L, Smith JJ, Olhava EJ, Chesworth R, Moyer MP, Richon VM, Copeland RA, Keilhack H, Pollock RM, Kuntz KW. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6.