BMH-21

SKU: orb1223725

Description

BMH-21 is a RNA polymerase I inhibitor with wide and potent antitumorigenic activity across NCI60 cancer cell lines with mean GI50 of 160 nM, interacts with GC-Rich rDNA, potently and rapidly represses RNA polymerase I (Pol I) transcription; inhibits the expression of 47S rRNA transcript with IC50 of 60 nM, blocks transcription of the rRNA precursor without affecting rRNA maturation, and causes segregation of nucleolar proteins; causes proteasome-mediated degradation of RPA194 (Pol I catalytic subunit); activates p53 and inhibits TP53 null and mutant cell lines with GI50 of 110 and 205 nM, respectively.

Key Properties

• CAS Number: 896705-16-1
• MW: 360.4091
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₀N₄O₂
• SMILES: O=C(C1=CC=CN2C1=NC3C=C(C=CC=C4)C4=CC3C2=O)NCCN(C)C
• Target: DNA/RNA Synthesis
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  BMH-21 (50 mg/kg; i.p.; daily; for 6 days) inhibits HCT116 colon cancer tumor growth In vivo. Animal model: 6-week old athymic NCr nu/nu mice, with HCT116 colorectal carcinoma xenograft. Dosage: 50 mg/kg. Administration: Intraperitoneal injection, daily, for 6 days. Result: Significantly inhibited HCT116 colon cancer tumor growth.
• In Vitro:
  BMH-21 binds ribosomal DNA and inhibits Pol I transcription. BMH-21 inhibits RNA polymerase I independent of DNA damage response. BMH-21 intercalates into double strand (ds) DNA and has binding preference towards GC-rich DNA sequences. BMH-21 (1 μM; 3 hours) acts in a DNA damage independent manner to activate nucleolar stress and RPA194 degradation. Cell Viability Assay Cell line: U2OS cells. Concentration: 0 μM, 0.1 μM, 1 μM, 10 μM Incubation time: 48 hours. Result: Decreased the viability of cells at concentrations that activated the DNA damage response. Western blot analysis. Cell line: A375 cells. Concentration: 1 μM. Incubation time: 3 hours. Result: Degraded RPA194 with blocked ATM and DNA-PKcs activity.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMH21

Quick Database Links

Gene Symbol

DNA/RNA Synthesis