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> 产品中心 > 抑制剂 & 激动剂 > Epigenetics > Histone Methyltransferase

EPZ005687

Cat. No.:YN310271

  • CAS No. :1396772-26-1

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    • 产品名称: EPZ005687
      CAS No.: 1396772-26-1
      Chemical Name: 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide
      Synonyms:EPZ005687;1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide;1H-Indazole-4-carboxamide, 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)pheny
      分子量:539.67
      分子式:C₃₂H₃₇N₅O₃
      SMILES:O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC5=C2C=NN5C6CCCC6
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: EPZ005687 是一种有效的,选择性的EZH2抑制剂,Ki值为 24 nM,对其选择性是对 EZH1 的 50 倍,对其他 15 种甲基转移酶的 500 倍。
      IC50和靶点: [{name:"EZH2:24 nM (Ki)"}]
      In Vitro:
      In Vivo:
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      Solvent & Solubility:
    • Knutson, S.K., Wigle, T.J., Warholic, N.M., et al.A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cellsNat. Chem. Biol.8(11),890-896(2012)

      Wigle, T.J., and Copeland, R.A.Drugging the human methylome: An emerging modality for reversible control of aberrant gene transcriptionCurr. Opin. Chem. Biol.17(3),369-378(2013)

      Konze, K.D., Ma, A., Li, F., et al.An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1ACS Chem. Biol.8(6),1324-1334(2013)

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