Necrosulfonamide

SKU: orb1300359

Description

Necrosulfonamide is a selective small molecule inhibitor of MLKL that blocks necroptosis by disrupting the MLKL-RIP1-RIP3 complex. It is widely used in both in vitro and in vivo research to investigate programmed necrosis in contexts like inflammatory disease and ischemia-reperfusion injury.

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 1360614-48-7
• MW: 461.47
• Purity: >98%
• Formula: C₁₈H₁₅N₅O₆S₂
• SMILES: COc1nccnc1NS(=O)(=O)c1ccc(NC(=O)\C=C\c2ccc(s2)[N+]([O-])=O)cc1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 10 mg/ml)

Bioactivity

• Target IC50:
  PI3Kγ:5.9 (pIC50)|PI4Kβ:5.9 (pIC50)|PI4KA:8.0 (pIC50)|PI3Kβ:5.9 (pIC50)|PI3Kα:5.8 (pIC50)|PI4Kα:8.0 (pIC50)|PI3Kδ:6.4 (pIC50)|PI4KB:5.9 (pIC50)
• In Vitro:
  METHODS: FLAG-tagged RIP3-HT-29 cells were treated with Necrosulfonamide for 6 h, and the interaction between RIP1 and RIP3 was examined using a FLAG-tagged RIP3 pull-down assay. RESULTS: Necrosulfonamide, an inhibitor of necrosis downstream of RIP3, did not block the necrosis-induced interaction between RIP1 and RIP3.
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• Cell Research:
  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. (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

complex, (E)-Necrosulfonamide, Mixed Lineage Kinase, necrosis(MLKL), necrosome, necrosis, Necrosulfonamide, MLKs, inhibit, formation, Inhibitor, substrate, RIP3

Compound Identifiers

PubChem CID

1566236