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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 |
| Related Epigenetic Reader Domain Products |
|---|
| I-BET151
I-BET151 (GSK1210151A) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. |
| (+)-JQ1
(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. |
| I-BET-762
I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| CPI-0610
CPI-0610 is a novel BET protein bromodomain inhibitor. |
| RVX-208
Apabetalone (RVX-208) is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
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