Drug intelligence / Profile preview

dichlororibofuranosylbenzimidazole

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

Dichlororibofuranosylbenzimidazole (DRB) is a synthetic small molecule nucleoside analog that functions primarily as an inhibitor of RNA polymerase II transcription. It acts by terminating transcription prematurely through selective inhibition of RNA synthesis. DRB is also a potent and specific ATP-competitive inhibitor of casein kinase II (CSNK2A1), with an IC₅₀ around 6 μM. In research settings, it is used to study mechanisms of cellular regulation including transcription elongation and cell cycle progression. Sensitivity to DRB in cells depends on factors such as DSIF (DRB sensitivity-inducing factor), NELF (negative elongation factor), and P-TEFb (positive transcription elongation factor b). It has been reported to induce apoptosis and G1/S cell cycle arrest in some models[2][3][4][5].

Other names
5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole5,6-dichlorobenzimidazole riboside5,6-dichlorobenzimidazole 1-beta-D-ribofuranoside5,6-dichloro-1-.beta.-D-ribofuranosylbenzimidazole
02

Targets

Pol II (RNA polymerase II elongation factors)CK2 (Casein kinase II subunit alpha)

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