BMH-21 is a first-in-class DNA intercalator that binds to high-frequency GC-rich sequences in ribosomal DNA genes and can effectively and rapidly inhibit the transcription of RNA polymerase I (Pol I), leading to degradation of the Pol I catalytic subunit RPA194 and non-phosphorylation of histone H2AX. H2AX is not phosphorylated.BMH-21 has broad and potent antitumor activity in NCI60 cancer cell line and inhibits tumor growth in vivo.
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Source | Oncol Rep (2017). Figure 2. BMH-21 |
| Method | Apoptosis assay | |
| Cell Lines | SKOV3 cells | |
| Concentrations | 1, 2 and 4 μM | |
| Incubation Time | 24 h | |
| Results | The results showed that the levels of BAX and cleaved caspase-3 increased in BMH-21 treated cells, compared with the control group |
| 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 | |
| Molecular Weight | 360.41 |
| Formula | C21H20N4O2 |
| CAS Number | 896705-16-1 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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