NS-398 (NS398)

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

For research use only.

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

CAS No. 123653-11-2

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

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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 M{Llb2Z2dmO2aX;uJIF{e2G7 NIrN[ndGfmGudXH0[YQh\m:{IHnubIljcXSrb36gc4YhS0:[LUKgZ4F1[Wy7enXkJHBITS1{IIDyc4R2[3Srb36g[pJwdSCOUGOgbY5lfWOnZDDSRXchOjZ2LkegZ4VtdHNuIFnDOVA:OC53IN88US=> NVfkS5lMOTR7OEC2OVc>
MDA-MB-231 cell NIXqRlNHfW6ldHnvckBie3OjeR?= MoXMVoVlfWO2aX;uJIlvKFCJRUKgcIV3\Wy|IHnuJG1FSS2PQj2yN|Eh[2WubB?= M4K3eFE3PDhyMke3
SKBr3 cells MXjGeY5kfGmxbjDhd5NigQ>? MXKyOEBp NEXY[3ZT\WS3Y4Tpc44hcW5iQ2nQNVkhdVKQQTDlfJBz\XO|aX;uJIlvKFONQoKzJINmdGy|IHHmeIVzKDJ2aDDlfJBwe3W{ZTD0c{AzPXWPIILlcIF1cX[nIITvJINwdnS{b3y= NUDyfHF3OTZ2OECyO|c>
SK-BR-3 cells NWH0dYNbS3m2b4TvfIlkcXS7IHHzd4F6 MnH4NlQhcA>? MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZkhemWuYYTpeoUhfG9iTmOzPVgtKEmFNUC9NE44OiEQvF2= M3zWclE4ODl3MkKx
SKBR3 cells M3u0bWZ2dmO2aX;uJIF{e2G7 Mne4TY5pcWKrdHnvckBw\iCjcn;tZZRie2ViaX6gbJVu[W5iU1vCVlMh[2WubIOgZpkhfHKrdHnheIVlKHejdHXyJJJmdGWjc3WgZZN{[XluIFnDOVA:OC54ODFOwG0> MVSxPFI4OTVzOR?=
RAW264.7 cells MoO2SpVv[3Srb36gZZN{[Xl? MYHBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhVFCVLXnu[JVk\WRiUFfFNkBxem:mdXP0bY9vKGK7IFXJRUwhUUN3ME20Mlgh|ryP MWGyNFAxPDV5Mh?=
PMA-Ion-stimulated human PBL MnrhSpVv[3Srb36gZZN{[Xl? NUCwRpM3PSEQvF2= NXvqO2puOjBiaB?= MoDoTY5pcWKrdHnvckBw\iCFT2iyJIV5eHKnc4Ppc44hcW5iUF3BMWlwdi2|dHnteYxifGWmIHj1cYFvKFCETDDheEA2KHWPIHHmeIVzKDJyIHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MYOyN|A1PzJ|MR?=
HUVEC MWTGeY5kfGmxbjDhd5NigQ>? NEDidJAyQCCq NFmwNGNCdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDh[4FqdnO2IG\FS2ZCNXO2aX31cIF1\WRiY3HwbYxt[XK7IHTp[oZmemWwdHnheIlwdiCrbjDIWXZGSyCjZoTldkAyQCCqcoOgZpkhdWG2cnnn[Ywh[XO|YYm= M3;t[lI{OTFyNEe1
HUVEC MojLSpVv[3Srb36gZZN{[Xl? MXu0PEBp M{\lbWFvfGmjbnfpc4dmdmmlIHHjeIl3cXS7IHHnZYlve3RiVlXHSmEue3SrbYXsZZRm\CClZXzsJJBzd2yrZnXyZZRqd25iaX6gTHVXTUNiYX\0[ZIhPDhiaILzJIJ6KEK{ZGWgbY5kd3Kyb4LheIlwdiCjc4PhfS=> MofmNlMyOTB2N{W=
RAW264.7 cells Ml3ZSpVv[3Srb36gZZN{[Xl? NIXiToEzPCCq NYnFb3MzSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhVFCVLXnu[JVk\WRiUFfFNkBxem:mdXP0bY9vKGGmbXnubZN1\XKnZDCxJIhzKHC{aX;yJJRwKEySUz3jbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGK7IFXJRUwhUUN3ME2wMlAxPzBzIN88US=> NXKzVoFYOjR|NkC1OlE>
HaCaT cells NIix[m5HfW6ldHnvckBie3OjeR?= M2e4NVI1KGh? Mm\pTY5pcWKrdHnvckBw\iCSR1WyJJBzd2S3Y4Tpc44hcW5iaIXtZY4hUGGFYWSgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFKLQTygTWM2OD1yLkCxJO69VQ>? NYjkUFJnOTV|OEe2OFI>
RAW264.7 cells NEHnRpRHfW6ldHnvckBie3OjeR?= Mn6yTY5pcWKrdHnvckBw\iCSR1WyJJBzd2S3Y4Tpc44hcW5iTGDTMYlv\HWlZXSgcY92e2ViUlHXNlY1NjdiY3XscJMtKEmFNUC9NE4xODdizszN NVHscllHOjV2NUO4NFA>
RAW264.7 cells MlrTSpVv[3Srb36gZZN{[Xl? MXexO{0zOCCq Ml;OTY5pcWKrdHnvckBw\iCLRl6t[4FudWFxTGDTMYlv\HWlZXSgVGdGOiCycn;keYN1cW:wIHnuJI1wfXOnIGLBW|I3PC55IHPlcIx{KGGodHXyJFE4KHSxIEKwJIhzeyCkeTDFTWEhdWW2aH;kMEBKSzVyPUCuNUDPxE1? M2\iSVI2ODJ5OUOz
SK-BR-3 cells Mn20SpVv[3Srb36gZZN{[Xl? NFzYZY5KdmirYnn0bY9vKG:oIFPZVFQ2OCCjcn;tZZRie2ViYXP0bZZqfHliaX6gV2suSlJvMzDj[YxteyxiSVO1NF0xNjZ6IN88US=> MY[xOlQ5ODJ5Nx?=
RAW264.7 cells Mnv3SpVv[3Srb36gZZN{[Xl? MnfITY5pcWKrdHnvckBw\iCFT2iyMY1m\GmjdHXkJHBITTJicILv[JVkfGmxbjDpckBNWFNvc4TpcZVt[XSnZDDtc5V{\SCUQWeyOlQvPyClZXzsd{BjgSCnbor5cYUhcW2vdX7vZZN{[XluIFnDOVA:OC5yNTFOwG0> NWexXm93OTl{M{O2OFY>
K562 cells NVWzOlRJTnWwY4Tpc44h[XO|YYm= M3S0[|Qh\GG7cx?= NG\wc2hKdmirYnn0bY9vKG:oIFPPXFIhcW5iaIXtZY4hUzV4MjDj[YxteyCjc4Pld5Nm\CCjczDicI9kc2GmZTDv[kBCVUxzLVXUU{Bxem:2ZXnuMYRmeGWwZHXueEBmenm2aILvbYQh\GmoZnXy[Y51cWG2aX;uJIFnfGW{IESg[IF6eyCkeTDi[Y57cWSrbnWgd5RicW6rbnegcYV1cG:m MWexPVE4OjF2Nh?=
RAW264.7 cells NV\2bWdLTnWwY4Tpc44h[XO|YYm= M1nIcmlvcGmkaYTpc44hd2ZiQ1;YNkBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDifUBmdnq7bXWgbY1ufW6xYYPzZZktKEmFNUC9NE45OSEQvF2= NIjCWWgzODB3NkW0PS=>
Assay
Methods Test Index PMID
Western blot c-Myc ; p-CHK1 / CHK1 ; LEF1 / active-β-catenin / CXCR4 / Cleaved Caspase 3 31410206 29636547 30304769
Growth inhibition assay Cell viability 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 (from reference)

Cell Research:[2]
  • 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.
Animal Research:[3]
  • Animal Models: CD1 mice
  • Dosages: 20 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 314.36
Formula

C13H18N2O5S

CAS No. 123653-11-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CS(=O)(=O)NC1=C(C=C(C=C1)[N+](=O)[O-])OC2CCCCC2

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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.

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