MS436

Catalog No.S7305

MS436 Chemical Structure

Molecular Weight(MW): 383.42

MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.

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Biological Activity

Description MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.
Targets
BRD4 (1) [1] BRD4 (2) [1]
<0.085 μM(Ki) 0.34 μM(Ki)
In vitro

MS436 exhibits low nanomolar affinity with preference for the first bromodomain over the second. MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages without siginificanty inhibition on cell viability. [1]

Protocol

Kinase Assay:[1]
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Fluorescence Anisotropy Binding Assay:

Binding affinity of the newly synthesized diazobenzene compounds for various bromodoamins is assessed in a fluorescence anisotropy competition assay using a fluorescein isothiocyanate (FITC)-labeled MS417 as an assay probe. Competition experiments are performed with a BrD protein (0.25–1 µM) and the fluorescent probe (80 nM), and increasing concentration of unlabeled competing ligand in a PBS buffer (pH 7.4) in total volume of 80 µL Measurements are obtained after a 1 hour incubation of the fluorescent ligand and the protein at 25°C with Safire 2 microplate reader. In a competition-binding assay, fluorescent ligand concentration is ≤ 2Kd, and protein concentration was set at which 50-80% of fluorescent ligand is bound. Dissociation constant of a competing ligand is calculated with the correction to Cheng-Prussoff equation introduced by Nicolovska-Coleska and colleagues. Assuming one-site competitive binding model, the equation used to calculate Ki’s from IC50 values recovered from fitting data using Prism.
Cell Research:[1]
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  • Cell lines: Murine macrophage RAW264.7 cells
  • Concentrations: ~100 μM
  • Incubation Time: 24 hours
  • Method: Murine macrophage RAW264.7 cells are plated at a density of 10000 cells per well in a 96-well plate and incubated at 37 °C for 18 h. The cells are then treated with the diazobenzene bromodomain inhibitors up to 100 μL for 24 hours. At the end of the 24 hr incubation, 10 μL of the MTT solution (4 mg/ml) is added to each well and incubated at 37°C for 4 h. 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. The final concentration of DMSO is adjusted to 0.05% (v/v). The extent of the reduction is measured by the absorbance at 570/630 nm using EnVison 2104 Multilabel Reader.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 55 mg/mL (143.44 mM)
Ethanol 1 mg/mL warmed (2.6 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 383.42
Formula

C18H17N5O3S

CAS No. 1395084-25-9
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID