MS436 , 10mMinDMSO , 1395084-25-9
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
Pack Size | Price | Stock | Quantity |
1ml | RMB559.20 | In Stock |
|
others | Enquire |
PRODUCT Properties
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 |
Description and Uses
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.
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.