Home MAPK Mixed Lineage Kinase inhibitor Necrosulfonamide For research use only.

Necrosulfonamide

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

Necrosulfonamide Chemical Structure

Necrosulfonamide Chemical Structure

CAS No. 1360614-48-7

Purity & Quality Control

Necrosulfonamide Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IEC-6 cells Function assay 10 μM 40 min Reduced cell viability was further aggravated by inhibition of MLKL using necrosulfonamide 29935529
MDA-MB-231 Cell viability assay 20 μM 48 h prevent cystine-starvation-induced cell death 29383104
Hs 578T Cell viability assay 20 μM 48 h prevent cystine-starvation-induced cell death 29383104
HCC 1937 Cell viability assay 20 μM 48 h prevent cystine-starvation-induced cell death 29383104
U937 Function assay 0-2.5 μM 20 h NSA reduced the ratio of PI positive cells in a concentration-dependent fashion independently of the way of cell death trigger (either TRAIL or STS) under caspase-compromised condition. 22860037
HeLa 20 nM Competitive binding affinity to Myc-tagged MLKL (unknown origin) transfected in human HeLa cells at 20 nM by Western blot analysis in presence of biotin-labeled positive probe ChEMBL
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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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pMLKL / MLKL 29500427
In Vivo
In vivo

Necrosulfonamide (NSA) is a small molecule that specifically inhibits necroptosis by targeting MLKL, the terminal executioner of necroptosis.
Animal Research Animal Models Male Wistar rats
Dosages 1.65 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 461.47 Formula

C18H15N5O6S2
CAS No. 1360614-48-7 SDF Download Necrosulfonamide SDF
Smiles COC1=NC=CN=C1NS(=O)(=O)C2=CC=C(C=C2)NC(=O)C=CC3=CC=C(S3)[N+](=O)[O-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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