Name: MS436
Price: 281.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    MS436 is a potent and selective small-molecule inhibitor of BRD4 with Ki values of ＜0.085μM and 0.34μM, respectively for BrD1 and BrD2 [1].BRD4 plays a role in gene transcription and is a drug target for cancer and inflammation. It has two bromodomains. MS436 is a diazobenzene compound, it is designed from the SAR studies to have higher selectivity. In vitro fluorescent anisotropy assay shows MS436 has about 10-fold higher affinity of BrD1 over BrD2. MS436 binds to BRD4 through a set of water-mediated interaction and this is the molecular basis for the binding affinity. MS436 also has activity to CBP BrD. In RAW264.7 cells, MS436 can block NF-κB-directed NO production and block the expression of proinflammatory cytokine interleukin (IL)-6 induced by LPS [1].
    
    [1] Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM. Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J Med Chem. 2013 Nov 27;56(22):9251-64.
- Properties
  - Alternative Name
    
    4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide
    
    CAS Number
    
    1395084-25-9
    
    Molecular Formula
    
    C18H17N5O3S
    
    Molecular Weight
    
    383.42
    
    Appearance
    
    A solid
    
    Purity
    
    99.21%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥19.15 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

MS436

MS436

Background

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