DRB
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
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- 2. Bangming Jin, Jiamei Zhu, et al. "MEN1is a regulator of alternative splicing and prevents R-loop-induced genome instability through suppression of RNA polymerase II elongation." Nucleic Acids Res. 2023 Aug 25;51(15):7951-7971. PMID: 37395406
- 3. Qian Fang, Geng G Tian, et al. "YTHDF1 phase separation triggers the fate transition of spermatogonial stem cells by activating the IκB-NF-κB-CCND1 axis." Cell Rep. 2023 Apr 25;42(4):112403. PMID: 37060562
- 4. Chi Hin Wong, Chi Han Li, et al. "The Establishment of CDK9/ RNA PolII/H3K4me3/DNA Methylation Feedback Promotes HOTAIR Expression by RNA Elongation Enhancement in Cancer." bioRxiv. 2019 October 21.
Storage | Store at -20°C |
M.Wt | 319.1 |
Cas No. | 53-85-0 |
Formula | C12H12Cl2N2O4 |
Synonyms | NSC 401575,Benzimidazole |
Solubility | insoluble in EtOH; insoluble in H2O; ≥12.6 mg/mL in DMSO |
Chemical Name | 5,6-dichloro-1-β-D-ribofuranosyl-1H-benzimidazole |
SDF | Download SDF |
Canonical SMILES | O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N2C=NC3=C2C=C(Cl)C(Cl)=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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