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: 123653-11-2

Selleck's NS-398 (NS398) has been cited by 14 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.80%
99.80

NS-398 (NS398) Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

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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. NS-398 stocks (5 mM) are dissolved in 0.1% dimethylsulfoxide (DMSO). 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


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