| 货号 | 10010302-10mg |
| 描述 | DRB is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II (IC50 range of 4-10 µM)1, Cdk7 (IC50 = ~20 µM)2,3, Cdk8 (IC50 = ~20 µM)3, and Cdk9 (IC50 = 3 µM).4 Through inhibition of certain CTD kinases, DRB inhibits an elongation step during RNA polymerase II transcription5,6, which can trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.7 DRB can also inhibit HIV transcription (IC50 = ~4 µM) by targeting elongation enhanced by the HIV-encoded transactivator Tat.8 |
| 别名 | NSC 401575;Benzimidazole; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Zandomeni, R.O. Kinetics of inhibition by 5,6-dichloro-1-β-D-ribofuranosylbenzimidazole on calf thymus casein kinase II. Biochemistry Journal 262, 469-473 (1989). 2.Yankulov, K.,Yamashita, K.,Roy, R., et al. The transcriptional elongation inhibitor 5,6-dichloro-1-β-D-ribofuranosylbenzimidazole inhibits transcription factor IIH-associated protein kinase. The Journal of Biological Chemisty 270(41), 23922-23925 (1995). 3.Rickert, P.,Corden, J.L., and Lees, E. Cyclin C/CDK8 and cyclin H/CDK7/p36 are biochemically distinct CTD kinases. Oncogene 18, 1093-1102 (1999). 4.Schang, L.M. Cyclin-dependent kinases as cellular targets for antiviral drugs. Journal of Antimicrobial Chemotherapy 50, 779-792 (2002). 5.Zandomeni, R.,Zandomeni, M.C.,Shugar, D., et al. Casein kinase type II is involved in the inhibition by 5,6-dichloro-1-β-D-ribofuranosylbenzimidazole of specific RNA polymerase II transcription. The Journal of Biological Chemisty 261(7), 3414-3419 (1986). 6.Yamaguchi, Y.,Wada, T., and Handa, H. Interplay between positive and negative elongation factors: drawing a new view of DRB. Genes to Cells 3, 9-15 (1998). 7.te Poele, R.H.,Okorokov, A.L., and Joel, S.P. RNA synthesis block by 5,6-dichloro-1-β-D-ribofuranosylbenzimidazole (DRB) triggers p53-dependent apoptosis in human colon carcinoma cells. Oncogene 18, 5765-5772 (1999). 8.Marciniak, R.A., and Sharp, P.A. HIV-1 tat protein promotes formation of more-processive elongation complexes. EMBO Journal 10(13), 4189-4196 (1991). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 319.1 |
| 分子式 | C12H12Cl2N2O4 |
| CAS号 | 53-85-0 |
| 稳定性 | ≥ 2 years |
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