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NS-398 (NS398) COX inhibitor

Name: NS-398 (NS398)
Brand: Selleck Chemicals
SKU: S8433
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S8433

NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) is a selective inhibitor of cyclooxygenase-2 (COX-2), with IC50 values for human recombinant COX-1 and -2 of 75 and 1.77 μM, respectively.

Chemical Structure

Molecular Weight: 314.36

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.80%

99.80

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel GluR MAO Beta Amyloid NMDAR P2 Receptor Trk receptor Serotonin Transporter Notch Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor BChE Adenosine Deaminase CCK receptor MT Receptor
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
RAW264.7 cells	Function assay			Evaluated for inhibition of COX-2 catalyzed PGE-2 production from LPS induced RAW 264.7 cells, IC50=0.5 μM
MDA-MB-231 cell	Function assay			Reduction in PGE2 levels in MDA-MB-231 cell
SKBr3 cells	Function assay		24 h	Reduction in CYP19 mRNA expression in SKBr3 cells after 24h exposure to 25uM relative to control
SK-BR-3 cells	Cytotoxicity assay		24 h	Cytotoxicity against human SK-BR-3 cells after 24 hrs by MTT assay relative to NS398, IC50=0.72 μM
SKBR3 cells	Function assay			Inhibition of aromatase in human SKBR3 cells by tritiated water release assay, IC50=0.68 μM
RAW264.7 cells	Function assay			Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production by EIA, IC50=4.8 μM
PMA-Ion-stimulated human PBL	Function assay	5 μM	20 h	Inhibition of COX2 expression in PMA-Ion-stimulated human PBL at 5 uM after 20 hrs by Western blot analysis
HUVEC	Function assay		18 h	Antiangiogenic activity against VEGFA-stimulated capillary differentiation in HUVEC after 18 hrs by matrigel assay
HUVEC	Function assay		48 h	Antiangiogenic activity against VEGFA-stimulated cell proliferation in HUVEC after 48 hrs by BrdU incorporation assay
RAW264.7 cells	Function assay		24 h	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS-challenge measured after 24 hrs by EIA, IC50=0.00701 μM
HaCaT cells	Function assay		24 h	Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA, IC50=0.01 μM
RAW264.7 cells	Function assay			Inhibition of PGE2 production in LPS-induced mouse RAW264.7 cells, IC50=0.007 μM
RAW264.7 cells	Function assay		17-20 h	Inhibition of IFN-gamma/LPS-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by EIA method, IC50=0.1 μM
SK-BR-3 cells	Function assay			Inhibition of CYP450 aromatase activity in SK-BR-3 cells, IC50=0.68 μM
RAW264.7 cells	Function assay			Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay, IC50=0.05 μM
K562 cells	Function assay		4 days	Inhibition of COX2 in human K562 cells assessed as blockade of AML1-ETO protein-dependent erythroid differentiation after 4 days by benzidine staining method
RAW264.7 cells	Function assay			Inhibition of COX2 in mouse RAW264.7 cells by enzyme immunoassay, IC50=0.81 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	314.36	Formula	C₁₃H₁₈N₂O₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	123653-11-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide			Smiles	CS(=O)(=O)NC1=C(C=C(C=C1)[N+](=O)[O-])OC2CCCCC2

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (197.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.100mg/ml (9.86mM)	Taking the 1 mL working solution as an example, add 50 μL of 62 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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+ %

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.

Mechanism of Action

Targets/IC₅₀/Ki	COX-2 ^[1] (Cell-free assay) 3.8 μM
In vitro	NS-398 (NS398) inhibits COX-2 enzyme activity in a concentration dependent manner, the IC50 being 3.8 μM, whereas at 100μM it has no effect on COX-1 activity^[1]. At 10 μM, this compound treatment results in increased production of COX-2 and the pro-inflammatory cytokine. It (10 μM) induces apoptosis in LNCaP cells, but not in the more aggressive, androgen-unresponsive C4-2b cells. The C4-2b cells are observed to continue to proliferate when treated with NS-398 and continues to retain malignant phenotype characteristics. Its treatment results in C4-2b cell differentiation into an unusual neuroendocrinelike cell. These neuroendocrine-like cells produces both epithelial (cytokeratin 18 and prostate specific antigen) and neuronal (neuron-specific enolase and chromogranin A) proteins. Furthermore, this C4-2b cellular response to it is mediated by NF-kB transcription factor activation. It induces NF-kB and down-regulates Ikβ-α protein expression in LNCaP C4-2b cells^[2].
In vivo	NS398 could inhibit Cox-2 expression induced by acoustic injury and attenuate noise-induced hearing threshold shifts and cochlear hair cell loss. The inhibition of Cox-2 by this compound could attenuate noise-induced hearing loss (NIHL) and related hair cell damage.^[3].
References	[1] https://pubmed.ncbi.nlm.nih.gov/8140262/ [2] https://pubmed.ncbi.nlm.nih.gov/11876163/ [3] https://pubmed.ncbi.nlm.nih.gov/26934825/

Applications

Methods	Biomarkers	Images	PMID
Western blot	c-Myc p-CHK1 / CHK1 LEF1 / active-β-catenin / CXCR4 / Cleaved Caspase 3		31410206
Growth inhibition assay	Cell viability		30304769

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