Name: Necrosulfonamide
Brand: Selleck Chemicals
SKU: S8251
Availability: InStock
Rating: 5 (116 reviews)

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Quality Control

Batch: Purity: 99.09%

99.09

Related Targets	ERK p38 MAPK K-Ras Raf JNK MEK Ras S6 Kinase MAP4K TAK1
Other Mixed Lineage Kinase Inhibitors	URMC-099 GW806742X GNE-3511

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	461.47	Formula	C₁₈H₁₅N₅O₆S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1360614-48-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=NC=CN=C1NS(=O)(=O)C2=CC=C(C=C2)NC(=O)C=CC3=CC=C(S3)[N+](=O)[O-]

Mechanism of Action

Targets/IC₅₀/Ki	necrosis(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.
References	[1] http://pubs.rsc.org/en/content/articlelanding/2014/md/c3md00278k#!divAbstract [2] https://pubmed.ncbi.nlm.nih.gov/22265413/ [3] https://pubmed.ncbi.nlm.nih.gov/24703947/ [4] https://pubmed.ncbi.nlm.nih.gov/32936609/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pMLKL / MLKL		29500427

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Necrosulfonamide Mixed Lineage Kinase inhibitor

Chemical Structure

Molecular Weight: 461.47