Home Neuronal Signaling COX inhibitor NS-398 (NS398) For research use only.

NS-398 (NS398)

Synonyms: N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide

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

NS-398 (NS398) Chemical Structure

NS-398 (NS398) Chemical Structure

CAS No. 123653-11-2

Purity & Quality Control

NS-398 (NS398) Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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 14980657
MDA-MB-231 cell Function assay Reduction in PGE2 levels in MDA-MB-231 cell 16480277
SKBr3 cells Function assay 24 h Reduction in CYP19 mRNA expression in SKBr3 cells after 24h exposure to 25uM relative to control 16480277
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 17095221
SKBR3 cells Function assay Inhibition of aromatase in human SKBR3 cells by tritiated water release assay, IC50=0.68 μM 18271519
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 20004572
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 23047231
HUVEC Function assay 18 h Antiangiogenic activity against VEGFA-stimulated capillary differentiation in HUVEC after 18 hrs by matrigel assay 23110475
HUVEC Function assay 48 h Antiangiogenic activity against VEGFA-stimulated cell proliferation in HUVEC after 48 hrs by BrdU incorporation assay 23110475
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 24360561
HaCaT cells Function assay 24 h Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA, IC50=0.01 μM 15387642
RAW264.7 cells Function assay Inhibition of PGE2 production in LPS-induced mouse RAW264.7 cells, IC50=0.007 μM 25453800
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 25027933
SK-BR-3 cells Function assay Inhibition of CYP450 aromatase activity in SK-BR-3 cells, IC50=0.68 μM 16480277
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 19233646
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 19172146
RAW264.7 cells Function assay Inhibition of COX2 in mouse RAW264.7 cells by enzyme immunoassay, IC50=0.81 μM 20056549
Click to View More Cell Line Experimental Data

Biological Activity

Description NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively.
Targets
COX-2 [1]
(Cell-free assay)
3.8 μM
In vitro
In vitro

NS-398 inhibits COX-2 enzyme activity in a concentration dependent manner, the IC50 being 3.8 μM, whereas NS-398 at 100μM has no effect on COX-1 activity[1]. At 10 μM, NS-398 treatment results in increased production of COX-2 and the pro-inflammatory cytokine. NS-398 (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. NS-398 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 NS-398 is mediated by NF-kB transcription factor activation. NS-398 induces NF-kB and down-regulates Ikβ-α protein expression in LNCaP C4-2b cells[2].
Cell Research Cell lines human prostate carcinoma cell line LNCaP and the LNCaP subline C4-2b
Concentrations 10 μM
Incubation Time 24, 48, 72 h
Method

1×106 cells are plated in six well cluster plates with 2 ml of medium for 24 h. At time point 0, medium was removed, cells were carefully washed with phosphate buffered saline (PBS) and serum free(SF), phenol-red free medium containing 0.5 μg/ml BSA was added. Incubations are continued for an additional 72 h with or without increasing NS-398 concentrations.  Cells and culture medium are harvested at 24 h time intervals. Dead cells are removed by gentle washing with PBS and cell number determined by direct counting using trypan blue dye exclusion to identify viable cells. DMSO (0.1%) is added to control cultures.
Experimental Result Images 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
In Vivo
In vivo

NS398 could inhibit Cox-2 expression induced by acoustic injury and could attenuate noise-induced hearing threshold shifts and cochlear hair cell loss. The inhibition of Cox-2 by NS398 could attenuate Noise-induced hearing loss（NIHL）and related hair cell damage.[3].
Animal Research Animal Models CD1 mice
Dosages 20 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 314.36 Formula

C13H18N2O5S
CAS No. 123653-11-2 SDF Download NS-398 (NS398) SDF
Smiles CS(=O)(=O)NC1=C(C=C(C=C1)[N+](=O)[O-])OC2CCCCC2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 62 mg/mL ( (197.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy NS-398 (NS398) | NS-398 (NS398) supplier | purchase NS-398 (NS398) | NS-398 (NS398) cost | NS-398 (NS398) manufacturer | order NS-398 (NS398) | NS-398 (NS398) distributor