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.
|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 .|
|Incubation time||48 hours|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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.
|Related DNA/RNA Synthesis Products|
Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.
Uridine is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond.
Rifampin is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.