NS-398 (NS398)

For research use only.

Catalog No.S8433 Synonyms: N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide

8 publications

NS-398 (NS398) Chemical Structure

CAS No. 123653-11-2

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.

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Selleck's NS-398 (NS398) has been cited by 8 publications

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  • (C)Percentage of TUNEL-positive cell in B were calculated. Data are mean ± SEM; ** P < 0.01 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (D-G) ELISA of cytokines IL-1α (D), IL-1β (E), IL-6 (F), and TNF-α (G) in tSCI rats with or without NS-398 treatment. Data are mean ± SEM; * P < 0.05 or ** P < 0.01 versus the Sham group; # P <0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (H) The mean CBS score in tSCI rats was improved by NS-398 treatment. Data are mean ± SEM; ** P < 0.05 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group.

    Oncotarget, 2017, 8(50): 87658-87666. NS-398 (NS398) purchased from Selleck.

Purity & Quality Control

Choose Selective COX Inhibitors

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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RAW264.7 cells NGS4e2ZHfW6ldHnvckBie3OjeR?= NH[xVphGfmGudXH0[YQh\m:{IHnubIljcXSrb36gc4YhS0:[LUKgZ4F1[Wy7enXkJHBITS1{IIDyc4R2[3Srb36g[pJwdSCOUGOgbY5lfWOnZDDSRXchOjZ2LkegZ4VtdHNuIFnDOVA:OC53IN88US=> M160TFE1QThyNkW3
MDA-MB-231 cell MUPGeY5kfGmxbjDhd5NigQ>? M1:2UXJm\HWldHnvckBqdiCSR1WyJIxmfmWuczDpckBOTEFvTVKtNlMyKGOnbHy= M{H0VFE3PDhyMke3
SKBr3 cells NUDTenVrTnWwY4Tpc44h[XO|YYm= NILHTGYzPCCq NF;hfXRT\WS3Y4Tpc44hcW5iQ2nQNVkhdVKQQTDlfJBz\XO|aX;uJIlvKFONQoKzJINmdGy|IHHmeIVzKDJ2aDDlfJBwe3W{ZTD0c{AzPXWPIILlcIF1cX[nIITvJINwdnS{b3y= NYnLWm5{OTZ2OECyO|c>
SK-BR-3 cells MlrZR5l1d3SxeHnjbZR6KGG|c3H5 M{PRSVI1KGh? MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZkhemWuYYTpeoUhfG9iTmOzPVgtKEmFNUC9NE44OiEQvF2= M4foNVE4ODl3MkKx
SKBR3 cells M2jvbWZ2dmO2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGG{b33heIF{\SCrbjDoeY1idiCVS1LSN{Bk\WyuczDifUB1emm2aXH0[YQhf2G2ZYKgdoVt\WG|ZTDhd5NigSxiSVO1NF0xNjZ6IN88US=> M2rxdlE5OjdzNUG5
RAW264.7 cells NID1e5hHfW6ldHnvckBie3OjeR?= MV;BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhVFCVLXnu[JVk\WRiUFfFNkBxem:mdXP0bY9vKGK7IFXJRUwhUUN3ME20Mlgh|ryP MkTRNlAxODR3N{K=
PMA-Ion-stimulated human PBL Ml;sSpVv[3Srb36gZZN{[Xl? NVf0O457PSEQvF2= NH\BR3MzOCCq NVPqUWR4UW6qaXLpeIlwdiCxZjDDU3gzKGW6cILld5Nqd25iaX6gVG1CNUmxbj3zeIlufWyjdHXkJIh2dWGwIGDCUEBifCB3IIXNJIFnfGW{IEKwJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> M2nMWVI{ODR5MkOx
HUVEC M13xZ2Z2dmO2aX;uJIF{e2G7 M3HNelE5KGh? NX;yVW5sSW62aXHu[4lw\2WwaXOgZYN1cX[rdImgZYdicW6|dDDWSWdHSS2|dHnteYxifGWmIHPhdIltdGG{eTDkbYZn\XKnboTpZZRqd25iaX6gTHVXTUNiYX\0[ZIhOThiaILzJIJ6KG2jdILp[4VtKGG|c3H5 MYOyN|EyODR5NR?=
HUVEC MmjoSpVv[3Srb36gZZN{[Xl? MX[0PEBp NWPK[VBjSW62aXHu[4lw\2WwaXOgZYN1cX[rdImgZYdicW6|dDDWSWdHSS2|dHnteYxifGWmIHPlcIwheHKxbHnm[ZJifGmxbjDpckBJXV[HQzDh[pRmeiB2ODDodpMh[nliQoLkWUBqdmOxcoDvdoF1cW:wIHHzd4F6 MUSyN|EyODR5NR?=
RAW264.7 cells NFrRfHhHfW6ldHnvckBie3OjeR?= MUKyOEBp M4PTXGFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKFCJRUKgdJJw\HWldHnvckBi\G2rbnnzeIVz\WRiMTDodkBxemmxcjD0c{BNWFNvY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{BjgSCHSVGsJGlEPTB;MD6wNFcxOSEQvF2= NFTX[3MzPDN4MEW2NS=>
HaCaT cells MW\GeY5kfGmxbjDhd5NigQ>? NE\KSGszPCCq NGrBPGVKdmirYnn0bY9vKG:oIGDHSVIheHKxZIXjeIlwdiCrbjDoeY1idiCKYVPhWEBk\WyuczDh[pRmeiB{NDDodpMh[nliUlnBMEBKSzVyPUCuNFEh|ryP MW[xOVM5PzZ2Mh?=
RAW264.7 cells NFO0OJFHfW6ldHnvckBie3OjeR?= M1\kbGlvcGmkaYTpc44hd2ZiUFfFNkBxem:mdXP0bY9vKGmwIFzQV{1qdmS3Y3XkJI1wfXOnIGLBW|I3PC55IHPlcIx{NCCLQ{WwQVAvODB5IN88US=> M1rBTVI2PDV|OECw
RAW264.7 cells M{LVR2Z2dmO2aX;uJIF{e2G7 Mnf6NVcuOjBiaB?= M3\qbWlvcGmkaYTpc44hd2ZiSV\OMYdidW2jL1zQV{1qdmS3Y3XkJHBITTJicILv[JVkfGmxbjDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCjZoTldkAyPyC2bzCyNEBpenNiYomgSWlCKG2ndHjv[EwhUUN3ME2wMlEh|ryP NUfMWWh3OjVyMke5N|M>
SK-BR-3 cells MXXGeY5kfGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKEO\UES1NEBiem:vYYThd4Uh[WO2aY\peJkhcW5iU1utRnIuOyClZXzsd{whUUN3ME2wMlY5KM7:TR?= NHX0SXUyPjR6MEK3Oy=>
RAW264.7 cells MXLGeY5kfGmxbjDhd5NigQ>? MkjITY5pcWKrdHnvckBw\iCFT2iyMY1m\GmjdHXkJHBITTJicILv[JVkfGmxbjDpckBNWFNvc4TpcZVt[XSnZDDtc5V{\SCUQWeyOlQvPyClZXzsd{BjgSCnbor5cYUhcW2vdX7vZZN{[XluIFnDOVA:OC5yNTFOwG0> NXPJTY1ZOTl{M{O2OFY>
K562 cells NIPYWHdHfW6ldHnvckBie3OjeR?= MmTrOEBl[Xm| NVfsPYtOUW6qaXLpeIlwdiCxZjDDU3gzKGmwIHj1cYFvKEt3NkKgZ4VtdHNiYYPz[ZN{\WRiYYOgZoxw[2ujZHWgc4YhSU2OMT3FWG8heHKxdHXpck1l\XCnbnTlcpQh\XK7dHjyc4llKGSrZn\ldoVvfGmjdHnvckBi\nSncjC0JIRigXNiYomgZoVvgmmmaX7lJJN1[WmwaX7nJI1mfGixZB?= NF7JOmIyQTF5MkG0Oi=>
RAW264.7 cells MlS3SpVv[3Srb36gZZN{[Xl? NHXncZhKdmirYnn0bY9vKG:oIFPPXFIhcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZpkh\W68eX3lJIludXWwb3Hzd4F6NCCLQ{WwQVAvQDFizszN NWWyVoRMOjByNU[1OFk>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Myc; 

PubMed: 31410206     


A549 and H1299 cells treated with 10058-F4 and AZD5153 for 48 hours as indicated concentration and c-myc and GAPDH were detected by western blotting. Images are representatives of three independent experiments. 

p-CHK1 / CHK1 ; 

PubMed: 29636547     


Western Blot analysis of OVCAR3 cells treated with increasing concentrations of AZD5153 (2 hour treatment).

LEF1 / active-β-catenin / CXCR4 / Cleaved Caspase 3 ; 

PubMed: 30304769     


Western blot analysis of MYC, active β−catenin, CXCR4, CD45/PTPRC, MYB, and LEF1 in UP-ALL13 cells treated in vitro with vehicle or AZD5153 (50–500 nM) for 18 h. Cleaved caspase 3 is used as a marker of apoptosis. β-actin is shown as loading control.

31410206 29636547 30304769
Growth inhibition assay
Cell viability; 

PubMed: 30304769     


Effect of BRD4 inhibition on the viability of UP-ALL13 and the T-ALL cell lines CUTLL1, DND41, MOLT-16, and SKW3/KE-37. Viability was evaluated after 24 h of incubation with increasing doses of AZD5153. 

30304769
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].

Protocol

Cell Research:[2]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[3]
- Collapse
  • Animal Models: CD1 mice
  • Dosages: 20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 62 mg/mL (197.22 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 314.36
Formula

C13H18N2O5S

CAS No. 123653-11-2
Storage powder
in solvent
Synonyms N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide
Smiles CS(=O)(=O)NC1=C(C=C(C=C1)[N+](=O)[O-])OC2CCCCC2

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID