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 |
| InChI | 1S/C18H17N5O3S/c1-12-10-16(15(19)11-17(12)24)22-21-13-5-7-14(8-6-13)27(25,26)23-18-4-2-3-9-20-18/h2-11,24H,19H2,1H3,(H,20,23) |
| InChIKey | DZTGIRNXWSZBIM-UHFFFAOYSA-N |
| SMILES | O=S(C(C=C1)=CC=C1/N=N/C2=C(N)C=C(O)C(C)=C2)(NC3=NC=CC=C3)=O |
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.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H315-H319-H335 |
| Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501 |
| WGK Germany | WGK 3 |
| Storage Class | 11 - Combustible Solids |
