Necrosulfonamide

Catalog No.S8251 Batch:S825101

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Technical Data

Formula

C18H15N5O6S2
Molecular Weight 461.47 CAS No. 1360614-48-7
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Necrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL).
Targets
necrosis(MLKL) [1]
In vitro

Necrosulfonamide inhibits MLKL-mediated Necrosis by blocking its N-terminal CC domain function. It blocks necrosis downstream of RIP3 activation. Necrosulfonamide 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 necrosulfonamide is that the cysteine at residue 86 in human MLKL that is covalently modified by necrosulfonamide is replaced by a tryptophan residue in mouse MLKL(mixed lineage kinase domain-like protein)[2].
In vivo

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

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    HT-29 cells

  • Concentrations

    1 μM

  • Incubation Time

    8 or 12 hrs

  • Method

    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.
Animal Study:

[4]
  • Animal Models

    Male Wistar rats

  • Dosages

    1.65 mg/kg

  • Administration

    i.p.

Customer Product Validation

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's Necrosulfonamide has been cited by 102 publications

MRE11 liberates cGAS from nucleosome sequestration during tumorigenesis [ Nature, 2024, 625(7995):585-592] PubMed: 38200309
Combined targeting of GPX4 and BCR-ABL tyrosine kinase selectively compromises BCR-ABL+ leukemia stem cells [ Mol Cancer, 2024, 23(1):240] PubMed: 39465372
SLC13A3 is a major effector downstream of activated β-catenin in liver cancer pathogenesis [ Nat Commun, 2024, 15(1):7522] PubMed: 39215042
NR4A1 depletion inhibits colorectal cancer progression by promoting necroptosis via the RIG-I-like receptor pathway [ Cancer Lett, 2024, 585:216693] PubMed: 38301909
Macroautophagy/autophagy promotes resistance to KRASG12D-targeted therapy through glutathione synthesis [ Cancer Lett, 2024, 604:217258] PubMed: 39276914
TCP1 expression alters the ferroptosis sensitivity of diffuse large B-cell lymphoma subtypes by stabilising ACSL4 and influences patient prognosis [ Cell Death Dis, 2024, 15(8):611] PubMed: 39174525
Haemolysins are essential to the pathogenicity of deep-sea Vibrio fluvialis [ iScience, 2024, 27(5):109558] PubMed: 38650982
Cetylpyridinium chloride triggers paraptosis to suppress pancreatic tumor growth via the ERN1-MAP3K5-p38 pathway [ iScience, 2024, 27(8):110598] PubMed: 39211547
Circ-CDK8 regulates SLC7A11-mediated ferroptosis by inhibiting miR-615-5p to promote progression in oral squamous cell carcinomas [ Front Pharmacol, 2024, 15:1432520] PubMed: 39170701
The cell fate regulator DACH1 modulates ferroptosis through affecting P53/SLC25A37 signaling in fibrotic disease [ Hepatol Commun, 2024, 8(3)e0396] PubMed: 38437058

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.