MS436
Synonym(s):(E)-4-[2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide;4-[(1E)-2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide;MS 436;MS-436
- CAS NO.:1395084-25-9
- Empirical Formula: C18H17N5O3S
- Molecular Weight: 383.42
- MDL number: MFCD27992062
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-01 14:32:37
What is MS436?
Description
MS436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated Ki of 30-50 nM) with preference for the first bromodomain over the second. MS436 effectively 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 ?M, respectively). MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression.
The Uses of MS436
MS 436 is a potent bromodomain inhibitor, binding to BRD4 and more tightly to subdomain BD1 than BD2. These domains play a key role in inflammatory gene expression, mitosis and viral/host interaction. Applications involving innhibition of bromodomains include decrease in cell proliferation for leukemia and destruction of tumor cells.
Biological Activity
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].
storage
-20°C
References
[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 of MS436
Boiling point: | 673.7±65.0 °C(Predicted) |
Density | 1.42±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | insoluble in H2O; insoluble in EtOH; ≥19.15 mg/mL in DMSO |
form | solid |
pka | 9.25±0.36(Predicted) |
color | Pink to red |
Safety information for MS436
Computed Descriptors for MS436
New Products
Bromine 99.5% AR (4 x 500ml) Fehling's Solution No. B Amino Acid Kit of 23 items set Ammonium Molybdate Reagent Solution Beam's Reagent Solution Ehrlich's Reagent For detection of urobillinogen 4-Hydroxy Carbazole 4-((2-isopropoxyethoxy)methyl)phenol 2 – Methoxy – 5- Sulfamoyl Benzoic acid Amino Salicylic Acid. U.S.P. 1,2,3,4-Tetrahydrocarbazol-4-one Acetone Isobutryl oxime ester Curcuma aromatica Oil Curry leaf Extract Terminalia bellirica Extract Aloe vera extract 200x Withania somnifera (Ashwagandha Extract) Citrus bioflavonoids Extract (S)-4-(4-(5-(Aminomethyl)-2-Oxooxazolidin-3-Yl)Phenyl)Mo Ethyl N-[[2-[[[4-(Aminoiminomethyl)Phenyl]Amino]Methyl] 5-Nitrosalicylaldehyde 5-(Difluoromethoxy)-2-Mercapto-1H-Benzimidazole- IP/BP/ Cypermethric Acid Chloride Methyl Di Chloride (Mdc)Related products of tetrahydrofuran
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