| Identification | Back Directory | [Name]
MS436 | [CAS]
1395084-25-9 | [Synonyms]
MS436
CS-1882
MS436(95%)
MS 436, >=98%
MS-436; MS 436
MS436 USP/EP/BP
(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
(E)-4-((2-AMINO-4-HYDROXY-5-METHYLPHENYL)DIAZENYL)-N-(PYRIDIN-2-YL)BENZENESULFONAMIDE
Benzenesulfonamide, 4-[(1E)-2-(2-amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinyl-
4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide
4-[(1E)-2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide MS436
MS436 4-[(1E)-2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide | [Molecular Formula]
C18H17N5O3S | [MDL Number]
MFCD27992062 | [MOL File]
1395084-25-9.mol | [Molecular Weight]
383.42 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [Uses]
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]
Store at -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. |
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| Company Name: |
China Langchem Inc.
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0086-21-58956006 |
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www.is0513.com/ShowSupplierProductsList19141/0.htm |
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