NS-398 (NS398)

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

NS-398 (NS398) Chemical Structure

Molecular Weight(MW): 314.36

NS-398 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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Biological Activity

Description NS-398 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 NHKxbXpHfW6ldHnvckBie3OjeR?= MWrFeoFtfWG2ZXSg[o9zKGmwaHnibZRqd25ib3[gR29ZNTJiY3H0ZYx6gmWmIGDHSU0zKHC{b3T1Z5Rqd25iZoLvcUBNWFNiaX7keYNm\CCUQWegNlY1NjdiY3XscJMtKEmFNUC9NE42KM7:TR?= M1TwPFE1QThyNkW3
MDA-MB-231 cell MoSySpVv[3Srb36gZZN{[Xl? NIKzeFlT\WS3Y4Tpc44hcW5iUFfFNkBt\X[nbIOgbY4hVUSDLV3CMVI{OSClZXzs NHmycpgyPjR6MEK3Oy=>
SKBr3 cells NELVNFFHfW6ldHnvckBie3OjeR?= MnjWNlQhcA>? MW\S[YR2[3Srb36gbY4hS1mSMUmgcXJPSSCneIDy[ZN{cW:wIHnuJHNMSnJ|IHPlcIx{KGGodHXyJFI1cCCneIDvd5Vz\SC2bzCyOZVOKHKnbHH0bZZmKHSxIHPvcpRzd2x? NH\UPVcyPjR6MEK3Oy=>
SK-BR-3 cells MmX2R5l1d3SxeHnjbZR6KGG|c3H5 NV2zeZQ6OjRiaB?= NUHqcGhZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvQmKtN{Bk\WyuczDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7IILlcIF1cX[nIITvJG5UOzl6LDDJR|UxRTBwN{Kg{txO NV;3VWFjOTdyOUWyNlE>
SKBR3 cells MkTwSpVv[3Srb36gZZN{[Xl? NV7aV|d4UW6qaXLpeIlwdiCxZjDhdo9u[XSjc3WgbY4hcHWvYX6gV2tDWjNiY3XscJMh[nlidILpeIlifGWmIIfheIVzKHKnbHXhd4Uh[XO|YYmsJGlEPTB;MD62PEDPxE1? MXSxPFI4OTVzOR?=
RAW264.7 cells NHywd3BHfW6ldHnvckBie3OjeR?= M13iZmFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCOUGOtbY5lfWOnZDDQS2UzKHC{b3T1Z5Rqd25iYomgSWlCNCCLQ{WwQVQvQCEQvF2= NWO0UpN7OjByMES1O|I>
PMA-Ion-stimulated human PBL MYfGeY5kfGmxbjDhd5NigQ>? NWnHbZdyPSEQvF2= MofzNlAhcA>? NX7uTpJpUW6qaXLpeIlwdiCxZjDDU3gzKGW6cILld5Nqd25iaX6gVG1CNUmxbj3zeIlufWyjdHXkJIh2dWGwIGDCUEBifCB3IIXNJIFnfGW{IEKwJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NHzqNlkzOzB2N{KzNS=>
HUVEC NFLYXGNHfW6ldHnvckBie3OjeR?= Mm[0NVghcA>? NWPBW|RSSW62aXHu[4lw\2WwaXOgZYN1cX[rdImgZYdicW6|dDDWSWdHSS2|dHnteYxifGWmIHPhdIltdGG{eTDkbYZn\XKnboTpZZRqd25iaX6gTHVXTUNiYX\0[ZIhOThiaILzJIJ6KG2jdILp[4VtKGG|c3H5 M4G1NVI{OTFyNEe1
HUVEC NWPMOGJXTnWwY4Tpc44h[XO|YYm= NGPFV4E1QCCq MXHBcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCjZ3HpcpN1KF[HR1\BMZN1cW23bHH0[YQh[2WubDDwdo9tcW[ncnH0bY9vKGmwIFjVWmVEKGGodHXyJFQ5KGi{czDifUBDemSXIHnuZ49zeG:{YYTpc44h[XO|YYm= NIrncYIzOzFzMES3OS=>
RAW264.7 cells M4\NUGZ2dmO2aX;uJIF{e2G7 MXKyOEBp NHm3VnJCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViUlHXNlY1NjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBNWFNvaX7keYNm\CCSR1WyJJBzd2S3Y4Tpc44h[WSvaX7pd5RmemWmIEGgbJIheHKrb4KgeI8hVFCVLXPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB{NDDodpMh[nliRVnBMEBKSzVyPUCuNFA4ODFizszN NWSwfndtOjR|NkC1OlE>
HaCaT cells NGPadYpHfW6ldHnvckBie3OjeR?= NWPkO5p{OjRiaB?= M4\o[WlvcGmkaYTpc44hd2ZiUFfFNkBxem:mdXP0bY9vKGmwIHj1cYFvKEijQ3HUJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCUSVGsJGlEPTB;MD6wNUDPxE1? NGHhUlQyPTN6N{[0Ni=>
RAW264.7 cells NFziWHhHfW6ldHnvckBie3OjeR?= M2rEOWlvcGmkaYTpc44hd2ZiUFfFNkBxem:mdXP0bY9vKGmwIFzQV{1qdmS3Y3XkJI1wfXOnIGLBW|I3PC55IHPlcIx{NCCLQ{WwQVAvODB5IN88US=> MX:yOVQ2OzhyMB?=
RAW264.7 cells MkDPSpVv[3Srb36gZZN{[Xl? MX6xO{0zOCCq M13Rb2lvcGmkaYTpc44hd2ZiSV\OMYdidW2jL1zQV{1qdmS3Y3XkJHBITTJicILv[JVkfGmxbjDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCjZoTldkAyPyC2bzCyNEBpenNiYomgSWlCKG2ndHjv[EwhUUN3ME2wMlEh|ryP M{joV|I2ODJ5OUOz
SK-BR-3 cells M3vVZWZ2dmO2aX;uJIF{e2G7 NYfiOHNiUW6qaXLpeIlwdiCxZjDDXXA1PTBiYYLvcYF1[XOnIHHjeIl3cXS7IHnuJHNMNUKULUOgZ4VtdHNuIFnDOVA:OC54ODFOwG0> MXOxOlQ5ODJ5Nx?=
RAW264.7 cells NHvVepBHfW6ldHnvckBie3OjeR?= M3m3PWlvcGmkaYTpc44hd2ZiQ1;YNk1u\WSrYYTl[EBRT0V{IIDyc4R2[3Srb36gbY4hVFCVLYP0bY12dGG2ZXSgcY92e2ViUlHXNlY1NjdiY3XscJMh[nliZX76fY1mKGmvbYXuc4F{e2G7LDDJR|UxRTBwMEWg{txO MoP4NVkzOzN4NE[=
K562 cells MnT2SpVv[3Srb36gZZN{[Xl? MkW0OEBl[Xm| MWHJcohq[mm2aX;uJI9nKEORWEKgbY4hcHWvYX6gT|U3OiClZXzsd{Bie3Onc4Pl[EBieyCkbH;jb4Fl\SCxZjDBUWwyNUWWTzDwdo91\WmwLXTldIVv\GWwdDDldpl1cHKxaXSg[Iln\mW{ZX70bYF1cW:wIHHmeIVzKDRiZHH5d{BjgSCkZX76bYRqdmVic4ThbY5qdmdibXX0bI9l Mo\QNVkyPzJzNE[=
RAW264.7 cells NYDMOI86TnWwY4Tpc44h[XO|YYm= NH;q[2hKdmirYnn0bY9vKG:oIFPPXFIhcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZpkh\W68eX3lJIludXWwb3Hzd4F6NCCLQ{WwQVAvQDFizszN MVuyNFA2PjV2OR?=

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: CD1 mice
  • Formulation: Normal saline
  • 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
Synonyms N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID