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產(chǎn)品名稱:

EPZ005687

 
產(chǎn)品編號: AS-0258 
別名: EPZ005687 抑制劑 
英文名: 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide 
CAS號: 1396772-26-1
分子式: C32H37N5O3 
分子量: 539.67 
EPZ005687
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.
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