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BMH 21
- Soluble in 0.1N HCl(aq)
- MF: C21H20N4O2
- MW: 360.41
Description
BMH 21 is an inhibitor of RNA polymerase I transcription that binds GC-rich ribosomal DNA and induces proteasome-mediated degradation of the Pol I subunit RPA194. It activates nucleolar stress and p53-linked responses in tumor cells.
RNA polymerase I drives ribosomal RNA synthesis and supports high ribosome biogenesis in proliferating cancer cells. BMH 21 is useful for studying nucleolar stress, rDNA transcription inhibition and Pol I-targeted anticancer mechanisms.
Key Features
- RNA polymerase I transcription inhibitor
- Reported IC50 values: 0.05 µM for RPA194 degradation and 0.07 µM for nucleolin translocation
- Intercalates GC-rich rDNA without classical DNA-damage signaling
- Induces nucleolar stress and p53 pathway activation
Applications
- RNA polymerase I pharmacology
- Ribosome biogenesis and nucleolar stress studies
- Cancer cell transcriptional vulnerability assays
- p53 activation and rDNA transcription research
More Information
| Parent CAS No. | 896705-16-1 |
|---|---|
| Chemical Name | N-(2-(dimethylamino)ethyl)-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide |
| SMILES | N1C2=C(C=C3C=CC=CC3=C2)C(=O)N2C=CC=C(C(NCCN(C)C)=O)C=12 |
| MFCD | N.A. |
| InChi | InChI=1S/C21H20N4O2/c1-24(2)11-9-22-20(26)16-8-5-10-25-19(16)23-18-13-15-7-4-3-6-14(15)12-17(18)21(25)27/h3-8,10,12-13H,9,11H2,1-2H3,(H,22,26) |
| InChiKey | BXYDVWIAGDJBEC-UHFFFAOYSA-N |
| CID | 3508054 |
| Short Description | RNAP1 inhibitor |
References
- L. Colis et al.Design, synthesis, and structure-activity relationships of pyridoquinazolinecarboxamides as RNA polymerase I inhibitors. J Med Chem. 2014 Jun 12;57(11):4950-61.
- K. Peltonen et al. Identification of novel p53 pathway activating small-molecule compounds reveals unexpected similarities with known therapeutic agents. PLoS One. 2010 Sep 27;5(9):e12996.
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