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BMH-21

Cat. No. M3892

BMH-21 Structure
Size Price Availability Quantity
10mg USD 70 In stock
50mg USD 200 In stock
100mg USD 350 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

BMH-21 binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription. Despite DNA intercalation, BMH-21 does not cause phosphorylation of H2AX, a key biomarker activated in DNA damage stress.BMH-21 inhibits RNA polymerase I (Pol I) transcription, causes the degradation of Pol I catalytic subunit RPA194, and has potent anticancer activity. BMH-21 has wide and potent antitumorigenic activity across NCI60 cancer cell lines and represses tumor growth in vivo. BMH-21 binds GC-rich sequences, which are present at a high frequency in ribosomal DNA genes, and potently and rapidly represses RNA polymerase I (Pol I) transcription. BMH-21 causes proteasome-dependent destruction of RPA194, the large catalytic subunit protein of Pol I holocomplex, and this correlates with cancer cell killing.

Protocol
Cell Experiment
Cell lines U2OS osteosarcoma cells
Preparation method Maintaining the cells at 37 °C in a humidified atmosphere containing 5% CO2. Culturing U2OS osteosarcoma cells in DMEM supplemented with 15% fetal bovine serum. Plating cells in 96-well plates at a density of 10000 cells/well in triplicate and incubated for 48 h with the compounds. Using WST-1 cell proliferation reagent to determine viability .
Concentrations ~5 μM
Incubation time 48 hours
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 360.41
Formula C21H20N4O2
CAS Number 896705-16-1
Purity >99%
Solubility
Storage at -20°C
References

Small molecule BMH-compounds that inhibit RNA polymerase I and cause nucleolar stress.
Peltonen K, et al. Mol Cancer Ther. 2014 Nov;13(11):2537-46. PMID: 25277384.

DNA intercalator BMH-21 inhibits RNA polymerase I independent of DNA damage response.
Colis L, et al. Oncotarget. 2014 Jun 30;5(12):4361-9. PMID: 24952786.

A targeting modality for destruction of RNA polymerase I that possesses anticancer activity.
Peltonen K, et al. Cancer Cell. 2014 Jan 13;25(1):77-90. PMID: 24434211.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BMH-21 supplier, DNA/RNA Synthesis, inhibitors

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