product name BMH-21
Description: BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription. BMH-21 intercalated into dsDNA and had binding preference towards GC-rich DNA sequences. BMH-21 had wide cytotoxic activities against human cancer cell lines, and acted in p53-independent manner, widely considered as a mediator of many cytotoxic agents. BMH-21 inhibited transcription of RNA polymerase I (Pol I) by binding to ribosomal (r) DNA that caused Pol I blockade and degradation of the large catalytic subunit of Pol I, RPA194.
References: Cancer Cell. 2014 Jan 13;25(1):77-90; J Med Chem. 2014 Jun 12;57(11):4950-61.
360.41
Formula
C21H20N4O2
CAS No.
896705-16-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (13.9 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (5.5 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1941180
| In Vitro |
In vitro activity: BMH-21 causes proteasome-dependent destruction of RPA194, the large catalytic subunit protein of Pol I holocomplex. In U2OS cancer cell line, BMH-21 results in degradation of RPA194 and translocation of NCL with IC50 of 0.05 μM and 0.07 μM, respectively. By causing nucleolar stress, BMH-21 also shows potent inhibition on cell viability. Kinase Assay: Cell Assay: The cells (U2OS osteosarcoma cells) are maintained at 37 °C in a humidified atmosphere containing 5% CO2. U2OS osteosarcoma cells are cultured in DMEM supplemented with 15% fetal bovine serum. Cells are plated in 96-well plates at a density of 10000 cells/well in triplicate and incubated for 48 h with the compounds. Viability is determined using WST-1 cell proliferation reagent. |
|---|---|
| In Vivo | BMH-21 reduces tumor growth in mouse xenografts. |
| Animal model | |
| Formulation & Dosage | |
| References | Cancer Cell. 2014 Jan 13;25(1):77-90; J Med Chem. 2014 Jun 12;57(11):4950-61. |
