Necrosulfonamide

製品コードS8251 バッチS825101

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C18H15N5O6S2

分子量 461.47 CAS No. 1360614-48-7
Solubility (25°C)* 体外 DMSO 92 mg/mL (199.36 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Necrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL).
in vitro

Necrosulfonamide inhibits MLKL-mediated Necrosis by blocking its N-terminal CC domain function. It blocks necrosis downstream of RIP3 activation. This compound has no effect on apoptosis induced by TNF-α plus Smac mimetic in non-RIP3-expressing Panc-1 cells, even at 5 μM concentration. The reason for the species specificity of this chemical is that the cysteine at residue 86 in human MLKL that is covalently modified by it is replaced by a tryptophan residue in mouse MLKL(mixed lineage kinase domain-like protein).

in vivo

Necrosulfonamide (NSA) is a small molecule that specifically inhibits necroptosis by targeting MLKL, the terminal executioner of this process.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HT-29 cells
濃度 1 μM
反応時間 8 or 12 hrs
実験の流れ

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 this compound are used to block necrosis.

動物実験 動物モデル Male Wistar rats
投薬量 1.65 mg/kg
投与方法 i.p.

参考

  • http://pubs.rsc.org/en/content/articlelanding/2014/md/c3md00278k#!divAbstract
  • https://pubmed.ncbi.nlm.nih.gov/22265413/
  • https://pubmed.ncbi.nlm.nih.gov/24703947/
  • https://pubmed.ncbi.nlm.nih.gov/32936609/

カスタマーフィードバック

Data from [Data independently produced by , , Biochim Biophys Acta, 2018, 1865(3):522-531]

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2018, 503(3):1550-1556]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

SIGLEC12 mediates plasma membrane rupture during necroptotic cell death [ Nature, 2025, 10.1038/s41586-025-09741-1] PubMed: 41225007
STING induces ZBP1-mediated necroptosis independently of TNFR1 and FADD [ Nature, 2025, 647(8090):735-746] PubMed: 40834903
Cytosolic cytochrome c represses ferroptosis [ Cell Metab, 2025, S1550-4131(25)00149-4] PubMed: 40233758
Harnessing the FGFR2/NF2/YAP signaling-dependent necroptosis to develop an FGFR2/IL-8 dual blockade therapeutic strategy [ Nat Commun, 2025, 16(1):4128] PubMed: 40319089
MLKL‒OPTN axis regulates herpesvirus-induced neurological sequelae [ Clin Transl Med, 2025, 15(6):e70353] PubMed: 40490945
The cancer-associated SF3B1K700E spliceosome mutation confers enhanced sensitivity to BV-6-induced cytotoxicity [ Cell Death Dis, 2025, 16(1):476] PubMed: 40595498
Androgen receptor inhibition sensitizes glioblastoma stem cells to temozolomide by the miR-1/miR-26a-1/miR-487b signature mediated WT1 and FOXA1 silencing [ Cell Death Discov, 2025, 11(1):248] PubMed: 40399259
O-GlcNAcylation of glutaminase isoform KGA inhibits ferroptosis through activation of glutaminolysis in hepatoblastoma [ Cell Death Discov, 2025, 11(1):160] PubMed: 40204725
Neuregulin-1 prevents death from a normally lethal respiratory viral infection [ PLoS Pathog, 2025, 21(4):e1013124] PubMed: 40267147
WTX-L/β-arrestin2/LCN2 axis controls vulnerability to ferroptosis in gastric cancer [ iScience, 2025, 28(3):111964] PubMed: 40109379

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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