DRB
(Synonyms: 二氯苯并咪唑呋喃型核糖苷,NSC 401575,Benzimidazole) 目录号 : GC17015
A CTD kinase inhibitor
Cas No.:53-85-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
5, 6-dichloro-1-β-D-ribofuranosylbenzimidazole (DRB) is a transcriptional elongation inhibitor.
Cyclin-dependent kinases (CDKs) belong to a family of protein kinases involved in regulating the cell cycle, transcription, mRNA processing, and the differentiation of nerve cells.[1] They are expressed in all known eukaryotes. With cyclin, CDK shows kinase activity. CDKs are serine-threonine kinases [1].
DRB inhibited the activity of several carboxyl-terminal domain (CTD) kinases including casein kinase II, Cdk7, Cdk8, and Cdk9 with the IC50 of 4-10 μM, ~20 μM, ~20 μM, and 3 μM) [2-5]. In HeLa cells, DRB (75 μM) inhibited 60-75% of nuclear heterogeneous RNA (hnRNA) synthesis. DRB (75 μM) reduced the appearance of labeled cytoplasmic poly(A)-containing messenger RNA (mRNA) by approximately 95%. DRB inhibited the initiation of hnRNA chains, but did not directly interfere with labeling of poly(A) [6]. DRB inhibited influenza virus multiplication in the chorioallantoic membrane in vitro [7]. DRB inhibited a HeLa protein kinase whihc phosphorylated an RNA polymerase II-derived peptide [8]. DRB can also inhibit HIV transcription (IC50 = ~4 μM) by targeting elongation enhanced by the HIV-encoded transactivator Tat.
References:
[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] Sehgal P B, Darnell J E, Tamm I. The inhibition of DRB (5, 6-dichloro-1-β-d-ribofuranosylbenzimidazole) of hnRNA and mRNA production in HeLa cells[J]. Cell, 1976, 9(3): 473-480.
[6] Tamm I, Tyrrell D A J. Influenza virus multiplication in the chorioallantoic membrane in vitro: kinetic aspects of inhibition by 5, 6-dichloro-1-β-D-ribofuranosylbenzimidazole[J]. The Journal of experimental medicine, 1954, 100(6): 541.
[7] Stevens A, Maupin M K. 5, 6-Dichloro-1-β-d-ribofuranosylbenzimidazole inhibits a HeLa protein kinase that phosphorylates an RNA polymerase II-derived peptide[J]. Biochemical and biophysical research communications, 1989, 159(2): 508-515.
| Cas No. | 53-85-0 | SDF | |
| 别名 | 二氯苯并咪唑呋喃型核糖苷,NSC 401575,Benzimidazole | ||
| 化学名 | 5,6-dichloro-1-β-D-ribofuranosyl-1H-benzimidazole | ||
| Canonical SMILES | O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N2C=NC3=C2C=C(Cl)C(Cl)=C3 | ||
| 分子式 | C12H12Cl2N2O4 | 分子量 | 319.1 |
| 溶解度 | ≥ 12.6mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1338 mL | 15.6691 mL | 31.3381 mL |
| 5 mM | 0.6268 mL | 3.1338 mL | 6.2676 mL |
| 10 mM | 0.3134 mL | 1.5669 mL | 3.1338 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet