DRB

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. They are expressed in all known eukaryotes. With cyclin, CDK shows kinase activity. CDKs are serine-threonine kinases . 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) . DRB inhibited influenza virus multiplication in the chorioallantoic membrane in vitro . DRB inhibited a HeLa protein kinase whihc phosphorylated an RNA polymerase II-derived peptide . DRB can also inhibit HIV transcription (IC50 = ~4 μM) by targeting elongation enhanced by the HIV-encoded transactivator Tat.

Product information

CAS Number: 53-85-0

Molecular Weight: 319.14

Formula: C12H12Cl2N2O4

Chemical Name: (2R,3R,4S,5R)-2-(5,6-dichloro-1H-1,3-benzodiazol-1-yl)-5-(hydroxymethyl)oxolane-3,4-diol

Smiles: OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=NC2C=C(Cl)C(Cl)=CC1=2

InChiKey: XHSQDZXAVJRBMX-DDHJBXDOSA-N

InChi: InChI=1S/C12H12Cl2N2O4/c13-5-1-7-8(2-6(5)14)16(4-15-7)12-11(19)10(18)9(3-17)20-12/h1-2,4,9-12,17-19H,3H2/t9-,10-,11-,12-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.