2-Propenamide, N-[4-[[(3-methoxy-2-pyrazinyl)amino]sulfonyl]phenyl]-3-(5-nitro-2-thienyl)-, (2E)-
Necrosulfonamide
CAS: 1360614-48-7
Molecular Formula: C18H15N5O6S2
2-Propenamide, N-[4-[[(3-methoxy-2-pyrazinyl)amino]sulfonyl]phenyl]-3-(5-nitro-2-thienyl)-, (2E)- - Names and Identifiers
2-Propenamide, N-[4-[[(3-methoxy-2-pyrazinyl)amino]sulfonyl]phenyl]-3-(5-nitro-2-thienyl)-, (2E)- - Physico-chemical Properties
| Molecular Formula | C18H15N5O6S2 |
| Molar Mass | 461.4716 |
| Density | 1.578±0.06 g/cm3(Predicted) |
| Melting Point | 200-204°C(dec.) |
| Solubility | Soluble in DMSO (up to 10 mg/ml) |
| Appearance | solid |
| Color | Yellow |
| pKa | 6.37±0.40(Predicted) |
| Storage Condition | -20℃ |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Physical and Chemical Properties | Bioactive necrsulfonamide is a specific and potent inhibitor of cell necrosis that exerts its effects by inhibiting MLKL. |
| Use | (E)-Necrosulfonamide is an inhibitor of necroptosis. Blocks mixed lineage kinase domain-like protein (MLKL), a critical substrate of receptor-interacting serine-threonine kinase 3 (RIP3) during necrosis. Prevents MLKL-RIP1-RIP3 necrosome complex from interacting with downstream necrosis effectors. Binds and inhibits gasdermin D. Inhibits pyroptosis. |
| Target | necrosis(MLKL) |
| In vitro study | Necrsulfonamide inhibits MLKL-mediated necrosis by preventing the function of the N-terminal CC region of MLKL. It inhibits necrosis downstream of RIP3 activation. Necrsulfonamide did not have any effect on TNF-α and Smac mimetic-induced apoptosis in Panc-1 cells that did not express RIP3, even at concentrations up to 5 μm. Necrsulfonamide is effective in inhibiting necrosis in human cells, but not in mouse cells. The species-specificity of necrsulfonamide may be due to the dependence of necrsulfonamide binding on the 86th cysteine of human MLKL, which is replaced by tryptophan in mouse MLKL. |
2-Propenamide, N-[4-[[(3-methoxy-2-pyrazinyl)amino]sulfonyl]phenyl]-3-(5-nitro-2-thienyl)-, (2E)- - Reference
| Reference Show more | 1. Teng J F, Mei Q B, Zhou X G, et al. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer[J]. MLA . Cancers. 2020, 12(1): 193.2. Yang W, Liu S, Li Y, et al. Pyridoxine induces monocyte-macrophages death as specific treatment of acute myeloid leukemia. Cancer Letters. 20203. Zhang J, Zhou B, Sun R, et al. The metabolite α-KG induces GSDMC-dependent pyroptosis through death receptor 6-activated caspase-8[J]. Cell Research. 2021: 1-18. |
2-Propenamide, N-[4-[[(3-methoxy-2-pyrazinyl)amino]sulfonyl]phenyl]-3-(5-nitro-2-thienyl)-, (2E)- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.167 ml | 10.835 ml | 21.67 ml |
| 5 mM | 0.433 ml | 2.167 ml | 4.334 ml |
| 10 mM | 0.217 ml | 1.083 ml | 2.167 ml |
| 5 mM | 0.043 ml | 0.217 ml | 0.433 ml |
Last Update：2024-01-02 23:10:35
2-Propenamide, N-[4-[[(3-methoxy-2-pyrazinyl)amino]sulfonyl]phenyl]-3-(5-nitro-2-thienyl)-, (2E)- - Cell Experiment
Cell lines: HT-29 cellsConcentrations: 1 μMIncubation Time: 8 or 12 hrsMethod: Necrosis inhibitors induce diverse effects on MLKL phosphorylation. HT-29 cells are treated with T/S/Z with or without necrosis inhibitors for 12 hr or 8 hr. The number of dead cells is determined by measuring released protease activity in culture medium. The whole-cell extracts are prepared and analyzed by western blotting. The final concentrations of 10 μM necrostatin-1 or 1 μM necrosulfonamide are used to block necrosis.
Last Update：2023-08-16 21:32:38
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Spot supply
Product Name: Necrosulfonamide Visit Supplier Webpage Request for quotationCAS: 1360614-48-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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