UNC0224
Cat. No.:YN310103
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. |
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)