NS-398 (NS398)

For research use only.

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

11 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.

Selleck's NS-398 (NS398) has been cited by 11 publications

1 Customer Review

  • (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 M1PRbWZ2dmO2aX;uJIF{e2G7 M2\ncWV3[Wy3YYTl[EBnd3JiaX7obYJqfGmxbjDv[kBEV1hvMjDjZZRidHm8ZXSgVGdGNTJicILv[JVkfGmxbjDmdo9uKEySUzDpcoR2[2WmIGLBW{AzPjRwNzDj[YxteyxiSVO1NF0xNjVizszN M1zjcVE1QThyNkW3
MDA-MB-231 cell MWnGeY5kfGmxbjDhd5NigQ>? NXPpXHp[WmWmdXP0bY9vKGmwIGDHSVIhdGW4ZXzzJIlvKE2GQT3NRk0zOzFiY3XscC=> M2XsVVE3PDhyMke3
SKBr3 cells NVfGTHE1TnWwY4Tpc44h[XO|YYm= MUKyOEBp M2\EOnJm\HWldHnvckBqdiCFWWCxPUBuWk6DIHX4dJJme3Orb36gbY4hW0uEckOgZ4VtdHNiYX\0[ZIhOjSqIHX4dI9{fXKnIITvJFI2fU1icnXsZZRqfmVidH:gZ49vfHKxbB?= NHK4OG4yPjR6MEK3Oy=>
SK-BR-3 cells NV;MUHZCS3m2b4TvfIlkcXS7IHHzd4F6 MkLDNlQhcA>? MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZkhemWuYYTpeoUhfG9iTmOzPVgtKEmFNUC9NE44OiEQvF2= NU[wdYcyOTdyOUWyNlE>
SKBR3 cells M2ThR2Z2dmO2aX;uJIF{e2G7 Ml23TY5pcWKrdHnvckBw\iCjcn;tZZRie2ViaX6gbJVu[W5iU1vCVlMh[2WubIOgZpkhfHKrdHnheIVlKHejdHXyJJJmdGWjc3WgZZN{[XluIFnDOVA:OC54ODFOwG0> Mm[1NVgzPzF3MUm=
RAW264.7 cells MWfGeY5kfGmxbjDhd5NigQ>? NHLITW5CdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgVGdGOiCycn;keYN1cW:wIHL5JGVKSSxiSVO1NF01NjhizszN MYiyNFAxPDV5Mh?=
PMA-Ion-stimulated human PBL MXzGeY5kfGmxbjDhd5NigQ>? NXGxNGpXPSEQvF2= M2K0TFIxKGh? M1jFeGlvcGmkaYTpc44hd2ZiQ1;YNkBmgHC{ZYPzbY9vKGmwIGDNRU1Kd25vc4TpcZVt[XSnZDDoeY1idiCSQlygZZQhPSC3TTDh[pRmeiB{MDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MkLHNlMxPDd{M{G=
HUVEC M2Ppc2Z2dmO2aX;uJIF{e2G7 NFHnWW8yQCCq NHS3coFCdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDh[4FqdnO2IG\FS2ZCNXO2aX31cIF1\WRiY3HwbYxt[XK7IHTp[oZmemWwdHnheIlwdiCrbjDIWXZGSyCjZoTldkAyQCCqcoOgZpkhdWG2cnnn[Ywh[XO|YYm= Mn;VNlMyOTB2N{W=
HUVEC M3\xS2Z2dmO2aX;uJIF{e2G7 NUfIXppNPDhiaB?= NGf3coRCdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDh[4FqdnO2IG\FS2ZCNXO2aX31cIF1\WRiY3XscEBxem:uaX\ldoF1cW:wIHnuJGhWXkWFIHHmeIVzKDR6IHjyd{BjgSCEcnTVJIlv[2:{cH;yZZRqd25iYYPzZZk> NEnGdWkzOzFzMES3OS=>
RAW264.7 cells NHjZTmlHfW6ldHnvckBie3OjeR?= M1\BUFI1KGh? M4Dq[2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKFCJRUKgdJJw\HWldHnvckBi\G2rbnnzeIVz\WRiMTDodkBxemmxcjD0c{BNWFNvY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{BjgSCHSVGsJGlEPTB;MD6wNFcxOSEQvF2= MXOyOFM3ODV4MR?=
HaCaT cells MXnGeY5kfGmxbjDhd5NigQ>? NGLHbIUzPCCq MmPtTY5pcWKrdHnvckBw\iCSR1WyJJBzd2S3Y4Tpc44hcW5iaIXtZY4hUGGFYWSgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFKLQTygTWM2OD1yLkCxJO69VQ>? MUKxOVM5PzZ2Mh?=
RAW264.7 cells NYTUW|dMTnWwY4Tpc44h[XO|YYm= MYfJcohq[mm2aX;uJI9nKFCJRUKgdJJw\HWldHnvckBqdiCOUGOtbY5lfWOnZDDtc5V{\SCUQWeyOlQvPyClZXzsd{whUUN3ME2wMlAxPyEQvF2= M{PKeFI2PDV|OECw
RAW264.7 cells MVnGeY5kfGmxbjDhd5NigQ>? NHXSfJkyPy1{MDDo MWrJcohq[mm2aX;uJI9nKEmITj3nZY1u[S:OUGOtbY5lfWOnZDDQS2UzKHC{b3T1Z5Rqd25iaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[W[2ZYKgNVchfG9iMkCgbJJ{KGK7IFXJRUBu\XSqb3SsJGlEPTB;MD6xJO69VQ>? NFH1fFMzPTB{N{mzNy=>
SK-BR-3 cells MmGxSpVv[3Srb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKEO\UES1NEBiem:vYYThd4Uh[WO2aY\peJkhcW5iU1utRnIuOyClZXzsd{whUUN3ME2wMlY5KM7:TR?= MUmxOlQ5ODJ5Nx?=
RAW264.7 cells MWfGeY5kfGmxbjDhd5NigQ>? NVfMbohZUW6qaXLpeIlwdiCxZjDDU3gzNW2nZHnheIVlKFCJRUKgdJJw\HWldHnvckBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCkeTDlcpp6dWViaX3teY5w[XO|YYmsJGlEPTB;MD6wOUDPxE1? M{nPWFE6OjN|NkS2
K562 cells NEfjT49HfW6ldHnvckBie3OjeR?= M1;tTlQh\GG7cx?= MUnJcohq[mm2aX;uJI9nKEORWEKgbY4hcHWvYX6gT|U3OiClZXzsd{Bie3Onc4Pl[EBieyCkbH;jb4Fl\SCxZjDBUWwyNUWWTzDwdo91\WmwLXTldIVv\GWwdDDldpl1cHKxaXSg[Iln\mW{ZX70bYF1cW:wIHHmeIVzKDRiZHH5d{BjgSCkZX76bYRqdmVic4ThbY5qdmdibXX0bI9l MXKxPVE4OjF2Nh?=
RAW264.7 cells MmTOSpVv[3Srb36gZZN{[Xl? M3rHfGlvcGmkaYTpc44hd2ZiQ1;YNkBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDifUBmdnq7bXWgbY1ufW6xYYPzZZktKEmFNUC9NE45OSEQvF2= MVWyNFA2PjV2OR?=

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID