BMH-21
RNA polymerase I inhibitor / A planar heterocyclic DNA intercalator that inhibits RNA polymerase I (Pol I), IC50 = 0.6 µM in U2OS cells, but not Pols II or III, blocking transcription elongation without inducing the DNA damage response.1-3 Inhibition disengages Pol I from chromatin, resulting in proteasome-dependent destruction of Pol I subunit RPA194.4 At nanomolar concentrations it also activates p53 in A375 cells.5
Biochemicals & reagents
896705-16-1
1 Colis et al. (2014), DNA intercalator BMH-21 inhibits RNA polymerase I independent DNA damage response; Oncotarget, 5 4361 2 Jacobs et al. (2022), RNA Polymerase I is Uniquely Vulnerable to the Small-Molecule Inhibitor BMH-21; Cancers (Basel), 14 5544 3 Jacobs et al. (2022), The small-molecule BMH-21 directly inhibits transcription elongation and DNA occupancy of RNA polymerase I in vivo and in vitro; J. Biol. Chem, 298 101450 4 Wei et al. (2018), Small-molecule targeting of RNA Polymerase I Activates a Conserved Transcription Elongation Checkpoint; Cell Rep. 23 404 5 Peltonen et al. (2010), Identification of novel p53 pathway activating small-molecule compounds reveals unexpected similarities with known therapeutic reagents; PLoS One 5 e12996
-20°C
TARGET: RNA; DNA; Transcription factor -- PATHWAY: p53; Transcription -- RESEARCH AREA: Cellular stress -- DISEASE AREA: Cancer