MS436 is a potent and selective BRD4 bromodomain inhibitor (Ki = 30 - 50 nM for BrD1). MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages. MS436 exhibits 10-fold selectivity for BrD1 over BrD2. MS436 blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50 values are 3.8 and 4.9 μM, respectively).
| Cell Experiment | |
|---|---|
| Cell lines | Murine macrophage RAW264.7 cells |
| Preparation method | Plating Murine macrophage RAW264.7 cells at a density of 10000 cells per well in a 96-well plate and incubating at 37 °C for 18 h. Then treating the cells with the diazobenzene bromodomain inhibitors up to 100 μL for 24 hours. Adding 10 μL of the MTT solution (4 mg/ml) to each well and incubating at 37°C for 4 h at the end of the 24 hr incubation. The supernatants are then removed and the cells were solubilized in 100 μL of 100% DMSO. The diazobenzene compounds are first dissolved in DMSO then diluted with culture medium to concentrations that ranged from 0.28 to 50000 nM.Adjusting the final concentration of DMSO is to 0.05% (v/v). Mearsuring the extent of the reduction by the absorbance at 570/630 nm using EnVison 2104 Multilabel Reader. |
| Concentrations | ~100 μM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 383.42 |
| Formula | C18H17N5O3S |
| CAS Number | 1395084-25-9 |
| Form | Solid |
| 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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