Necrosulfonamide


Catalog No. size PriceQuantity
M6702-2 2mg solid $213
M6702-10 10mg solid $836

Description

Cas:1360614-48-7

          432531-71-0     

Product Information

Necrosulfonamide is a novel inhibitor of MLKL (mixed lineage kinase domain-like). Necrosulfonamide is a cell-permeable inhibitor that covalently modifies Cys88 and blocks human MLKL adaptor function. Necrosulfonamide Attenuates Spinal Cord Injury via Necroptosis Inhibition.

 

Chemical Formula: C18H15N5O6S2

 

Exact Mass: 461.0464

 

Molecular Weight: 461.467 

 

Elemental Analysis: C, 46.85; H, 3.28; N, 15.18; O, 20.80; S, 13.89

 

Synonym: 

 

Necrosulfonamide

MLKL inhibitor

Necrosis Inhibitor III

Mixed Lineage Kinase Domain-Like Protein Inhibitor

Necrosome Inhibitor II

 

Chemical Name:

N-(4-(N-(3-Methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophene-2-yl)acrylamide

 

InChi Key:

FNPPHVLYVGMZMZ-XBXARRHUSA-N

 

InChi Code:  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+

 

Smiles Code:

O=C(NC1=CC=C(S(=O)(NC2=NC=CN=C2OC)=O)C=C1)/C=C/C3=CC=C([N+]([O-])=O)S3

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >95% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in 1:50 DMF:PBS (pH 7.2); DMSO; DMF

Shelf Life:>2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

Necrosulfonamide specifically blocks necrosis downstream of RIP3 activation. Necrosulfonamide inhibits MLKL-mediated necrosis by blocking Its N-terminal CC domain function.

 

 

References

 

  1. Chen S, Lv X, Hu B, Shao Z, Wang B, Ma K, Lin H, Cui M. RIPK1/RIPK3/MLKL-mediated necroptosis contributes to compression-induced rat nucleus pulposus cells death. Apoptosis. 2017 May;22(5):626-638. doi: 10.1007/s10495-017-1358-2. PubMed PMID: 28289909.

 

  1. Zhao W, Feng H, Sun W, Liu K, Lu JJ, Chen X. Tert-butyl hydroperoxide (t-BHP) induced apoptosis and necroptosis in endothelial cells: Roles of NOX4 and mitochondrion. Redox Biol. 2017 Apr;11:524-534. doi: 10.1016/j.redox.2016.12.036. Epub 2017 Jan 5. PubMed PMID: 28088644; PubMed Central PMCID: PMC5237803.

 

  1. Filipczak PT, Thomas C, Chen W, Salzman A, McDonald JD, Lin Y, Belinsky SA. TSC2 Deficiency Unmasks a Novel Necrosis Pathway That Is Suppressed by the RIP1/RIP3/MLKL Signaling Cascade. Cancer Res. 2016 Dec 15;76(24):7130-7139. Epub 2016 Oct 18. PubMed PMID: 27756752.

 

  1. Liu X, Zhou M, Mei L, Ruan J, Hu Q, Peng J, Su H, Liao H, Liu S, Liu W, Wang H, Huang Q, Li F, Li CY. Key roles of necroptotic factors in promoting tumor growth. Oncotarget. 2016 Apr 19;7(16):22219-33. doi: 10.18632/oncotarget.7924. PubMed PMID: 26959742; PubMed Central PMCID: PMC5008357.

 

  1. Mulay SR, Desai J, Kumar SV, Eberhard JN, Thomasova D, Romoli S, Grigorescu M, Kulkarni OP, Popper B, Vielhauer V, Zuchtriegel G, Reichel C, Brasen JH, Romagnani P, Bilyy R, Munoz LE, Herrmann M, Liapis H, Krautwald S, Linkermann A, Anders HJ. Cytotoxicity of crystals involves RIPK3-MLKL-mediated necroptosis. Nat Commun. 2016 Jan 28;7:10274. doi: 10.1038/ncomms10274. PubMed PMID: 26817517; PubMed Central PMCID: PMC4738349.

 

Products are for research use only. Not for human use.

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