MS436
- Product Name
- MS436
- CAS No.
- 1395084-25-9
- Chemical Name
- MS436
- Synonyms
- MS436;CS-1882;MS436(95%);MS 436, >=98%;MS-436; MS 436;MS436 USP/EP/BP;5-Dimethoxy-4-hydroxy cinnamaldehyde;(E)-4-[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;4-[(1E)-2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
- CBNumber
- CB12677056
- Molecular Formula
- C18H17N5O3S
- Formula Weight
- 383.42
- MOL File
- 1395084-25-9.mol
MS436 Property
- 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)
N-Bromosuccinimide Price
- Product number
- 5173
- Product name
- MS436
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $184
- Updated
- 2021/12/16
- Product number
- 5173
- Product name
- MS436
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $753
- Updated
- 2021/12/16
- Product number
- A612095
- Product name
- 4-[(1E)-2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
- Packaging
- 10mg
- Price
- $185
- Updated
- 2021/12/16
- Product number
- Y1865
- Product name
- MS436
- Packaging
- 10mg
- Price
- $218.75
- Updated
- 2021/12/16
- Product number
- CS-1729
- Product name
- MS436
- Purity
- 99.13%
- Packaging
- 5mg
- Price
- $90
- Updated
- 2021/12/16
MS436 Chemical Properties,Usage,Production
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
-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.
MS436 Preparation Products And Raw materials
Raw materials
Preparation Products
MS436 Suppliers
View Lastest Price from MS436 manufacturers
- Product
- (E)-4-((2-AMINO-4-HYDROXY-5-METHYLPHENYL)DIAZENYL)-N-(PYRIDIN-2-YL)BENZENESULFONAMIDE 1395084-25-9
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 20kg
- Release date
- 2019-09-03