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UNC0224

Cat. No.:YN310103

  • CAS No. :1197196-48-7

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    • 产品名称: UNC0224
      CAS No.: 1197196-48-7
      Chemical Name: 7-[3-(dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine
      Synonyms:UNC-0224, UNC0224, UNC 0224
      分子量:485.67
      分子式:C₂₆H₄₃N₇O₂
      SMILES:CN1CCC(NC2=C3C=C(OC)C(OCCCN(C)C)=CC3=NC(N4CCN(C)CCC4)=N2)CC1
      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: UNC0224 是一种有效的选择性的组蛋白甲基转移酶G9a抑制剂,Ki为 2.6 nM,IC50值为 15 nM,Kd为 23 nM。UNC0224 还有效抑制GLP,IC50值为 20-58 nM。UNC0224 对 SET7/9,SET8/PreSET7,PRMT3 和 JMJD2E 无活性。
      IC50和靶点: [{name:"EHMT1/GLP/KMT1D:20-58 nM (IC50)"},{name: "G9a:15 nM (IC50)"},{name: "G9a:2.6 nM (Ki)"},{name: "G9a:23 nM (Kd)"}]
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • Tachibana, M., Sugimoto, K., Nozaki, M., et al.G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesisGenes Dev.16(14),1779-1791(2002)

      Wagschal, A., Sutherland, H.G., Woodfine, K., et al.G9a histone methyltransferase contributes to imprinting in the mouse placentaMol. Cell Biol.28(3),1104-1113(2008)

      Thomas, L.R., Miyashita, H., Cobb, R.M., et al.Functional analysis of histone methyltransferase G9a in B and T lymphocytesJ. Immunol.181(1),485-493(2008)

      Liu, F., Chen, X., Allali-Hassani, A., et al.Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9aJ. Med. Chem.52(24),7950-7953(2009)

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