An RNA polymerase I inhibitor; inhibits expression of the 47S rRNA transcript (IC50 = 60 nM)

BMH-21 – 10 mg

Brand:
Cayman
CAS:
896705-16-1
Storage:
-20
UN-No:
Non-Hazardous - /

BMH-21 is an inhibitor of RNA polymerase I.{41313} It binds to GC-rich sequences in DNA and ribosomal DNA (rDNA) and inhibits RNA polymerase I transcription in vitro. It inhibits expression of the 47S rRNA transcript (IC50 = 60 nM), disrupts the structure of the nucleolus, and leads to removal of the RNA polymerase complex from rDNA by inducing dissociation and destruction of RPA194 through a proteasome-dependent mechanism. BMH-21 also activates p53 in the nanomolar range.{41312} It reduces viability of several cancer cell lines but not of non-cancerous cells (IC50s = 0.7, 1.9, ≥40, and 2.7 µM for A375, human diploid fibroblasts, primary human melanocytes, and HIMEC cells, respectively). BMH-21 intercalates with DNA but does not induce DNA damage via the ataxia-telangiectasia mutated (ATM) kinase pathway. BMH-21 (25 mg/kg) inhibits tumor growth in melanoma and colon cancer mouse xenograft models.{41313}  

 

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Description

An RNA polymerase I inhibitor; inhibits expression of the 47S rRNA transcript (IC50 = 60 nM), disrupts the structure of the nucleolus, and leads to removal of the RNA polymerase complex from rDNA by inducing dissociation and destruction of RPA194 through a proteasome-dependent mechanism; activates p53 in the nanomolar range; reduces viability of several cancer cell lines but not of non-cancerous cells (IC50s = 0.7, 1.9, ≥40, and 2.7 µM for A375, human diploid fibroblasts, primary human melanocytes, and HIMEC cells, respectively); inhibits tumor growth in melanoma and colon cancer mouse xenograft models when used at a dose of 25 mg/kg

Formal name: N-[2-(dimethylamino)ethyl]-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide

Synonyms: 

Molecular weight: 360.4

CAS: 896705-16-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|DNA Damage and Repair

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