EB-47 dihydrochloride
Cat. No.:YN310096
CAS No. :1190332-25-2
产品名称: | EB-47 dihydrochloride |
CAS No.: | 1190332-25-2 |
Chemical Name: | 5′-deoxy-5′-[4-[2-[(2,3-dihydro-1-oxo-1H-isoindol-4-yl)amino]-2-oxoethyl]-1-piperazinyl]-5′-oxo-adenosine, dihydrochloride |
Synonyms: | EB 47 |
分子量: | 610.45 |
分子式: | C₂₄H₂₉Cl₂N₉O₆ |
SMILES: | O=C1NCC2=C(C=CC=C21)NC(CN3CCN(CC3)C([C@H]4O[C@H]([C@@H]([C@@H]4O)O)N5C6=C(N=C5)C(N)=NC=N6)=O)=O.[H]Cl.[H]Cl |
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: | EB-47 dihydrochloride 是一种有效的PARP-1/ARTD-1选择性抑制剂,IC50值为 45 nM,对 ARTD5 的IC50值为 410 nM,表现出温和的效果。EB-47 模拟底物 NAD+,从烟酰胺延伸至腺苷亚区结合。 |
IC50和靶点: | |
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Jagtap, P.G., Southan, G.J., Baloglu, E., et al.The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: Potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)Bioorg. Med. Chem. Lett.14(1),81-85(2004)
Haikarainen, T., Narwal, M., Joensuu, P., et al.Evaluation and structural basis for the inhibition of tankyrases by PARP inhibitorsACS Med. Chem. Lett.5(1),18-22(2013)
Venkannagari, H., Fallarero, A., Feijs, K.L.H., et al.Activity-based assay for human mono-ADP-ribosyltransferases ARTD7/PARP15 and ARTD10/PARP10 aimed at screening and profiling inhibitorsEur. J. Pharm. Sci.49(2),148-156(2013)
Ferraris, D.V.Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinicJ. Med. Chem.53(12),4561-4584(2010)