Transcription inhibitor, CK2 inhibitor / A classic inhibitor of transcription by RNA polymerase II. A relatively selective inhibitor of Cdk9 (IC50=3 μM), the kinase of the positive transcription elongation factor b (P-TEF-b) required for processive transcription elongation by RNA polymerase II.1,2 Also inhibits casein kinase II, IC50=4-10 μM. 3 Suppresses the SIRT1/CK2α pathway and enhances the radiosensitivity of human cancer cells.4 Kinase-independent activities of Cdk9 such as glucocorticoid receptor modulation are not inhibited by DRB.5
Biochemicals & reagents
53-85-0
5,6-Dichlorobenzimidazole riboside; NSC 401575
1) Baumli et al. (2010), Halogen bonds form the basis for selective P-TEFb inhibition by DRB; Chem.Biol., 17 931 2) Yamaguchi et al. (1998), Interplay between positive and negative elongation factors: drawing a new view of DRB; Genes Cells, 3 9 3) Zandomeni (1989), Kinetics of inhibition by 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole; Biochem.J., 262 469 4) Wang et al. (2014), Inhibition of P-TEFb by DRB suppresses SIRT1/CK2α pathway and enhances radiosensitivity of human cancer cells; Anticancer Res., 34 6981 5) Zhu et al. (2014), A kinase-independent activity of Cdk9 modulates glucocorticoid receptor-mediated gene induction; Biochemistry, 53 1753
-20°C
TARGET: Kinase; RNA -- PATHWAY: Transcription; Cell cycle -- DISEASE AREA: Cancer