BMH-21 | RNA Polymerase I inhibitor

CAS:
 896705-16-1
Catalog Number:
 10-5688

Available Options

SizePriceQuantity 
5mg$52.00
25mg$210.00

BMH-21 (896705-16-1) is 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

References/Citations:

  1. Colis et al. (2014), DNA intercalator BMH-21 inhibits RNA polymerase I independent DNA damage response; Oncotarget, 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 e12996
CAS:
896705-16-1
Catalog Number:
10-5688
Activity:
RNA Polymerase I inhibitor
Chemical Names:
N-[2-(Dimethylamino)ethyl]-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide
Molecular Weight:
360.42
Molecular Formula:

C21H20N4O2

Solubility:
Soluble in DMSO (13 mg/ml with warming)
Physical Properties:
Orange solid
Purity:

>98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee