Necrosulfonamide

• CAT Number: I001390
• CAS Number: 1360614-48-7
• Molecular Formula: C18H15N5O6S2
• Molecular Weight: 461.467
• Purity: ≥95%
• Synonyms: (Z)-N-(4-(N-(3-methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophen-2-yl)acrylamide
• Target: Mixed Lineage Kinase
• Solubility: DMSO ≥ 28 mg/mL
• Storage: Store at +4C
• IUPAC Name: (E)-N-[4-[(3-methoxypyrazin-2-yl)sulfamoyl]phenyl]-3-(5-nitrothiophen-2-yl)prop-2-enamide
• InChI: InChI=1S/C18H15N5O6S2/c1-29-18-17(19-10-11-20-18)22-31(27,28)14-6-2-12(3-7-14)21-15(24)8-4-13-5-9-16(30-13)23(25)26/h2-11H,1H3,(H,19,22)(H,21,24)/b8-4+
• InChIKey: FNPPHVLYVGMZMZ-XBXARRHUSA-N
• SMILES: COC1=NC=CN=C1NS(=O)(=O)C2=CC=C(C=C2)NC(=O)C=CC3=CC=C(S3)[N+](=O)[O-]

Necrosulfonamide is a pharmacological inhibitor of MLKL with IC50 values of 124 nM in human HT-29.target: MLKL IC50 : 124 nM.In vitro: Necrosulfonamide significantly decreases BV6/DAC-induced cell death in MV4-11 cells. Treating cells with necrosulfonamide or knocking down MLKL expression arrests necrosis at a specific step at which RIP3 formed discrete punctae in cells. necrosulfonamide had no effect on apoptosis induced by TNF-α plus Smac mimetic in non-RIP3-expressing Panc-1 cells. Complete inhibition was observed at NSA concentration of 0.5 M. NSA is also an effective inhibitor of the necroptotic pathway induced by STS in the presence of caspase inhibitor.