MS436

SKU: orb1307320

Description

MS436 is a potent and selective small-molecule inhibitor targeting the bromodomains of BRD4. It is widely used in biochemical and cellular research to probe BET protein function and has demonstrated activity in both in vitro assays and in vivo models of inflammation and cancer.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1395084-25-9
• MW: 383.42
• Purity: 97.95%
• Formula: C₁₈H₁₇N₅O₃S
• SMILES: Cc1cc(\N=N\c2ccc(cc2)S(=O)(=O)Nc2ccccn2)c(N)cc1O
• Target: Epigenetic Reader Domain
• Solubility: DMSO:40 mg/mL (104.32 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.61 mM)

Bioactivity

• Target IC50:
  BRD4(1):<0.085 μM(Ki)|BRD4(2):0.34 μM(Ki)
• In Vivo:
  MS436 exhibits low nanomolar affinity (Ki=30-50 nM) for the first bromodomain of BRD4. In mouse macrophages with NF-κB-directed expression, MS436 inhibits BRD4 activity, reducing the levels of NO and IL-6.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRD4 (2), BRD4 (1), Inhibitor, EpigeneticReaderDomain, Epigenetic Reader Domain, MS436, MS-436, MS 436, inhibit

Compound Identifiers

PubChem CID

135566899