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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Cited by 1 Publication

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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 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 MojmSpVv[3Srb36gZZN{[Xl? NUfsTlRDTX[jbIXheIVlKG[xcjDpcohq[mm2aX;uJI9nKEORWD2yJINifGGueYrl[EBRT0VvMjDwdo9lfWO2aX;uJIZzd21iTGDTJIlv\HWlZXSgVmFYKDJ4ND63JINmdGy|LDDJR|UxRTBwNTFOwG0> M{SzNlE1QThyNkW3
MDA-MB-231 cell MorLSpVv[3Srb36gZZN{[Xl? NXHybHJkWmWmdXP0bY9vKGmwIGDHSVIhdGW4ZXzzJIlvKE2GQT3NRk0zOzFiY3XscC=> Ml3UNVY1QDB{N{e=
SKBr3 cells M1;xfmZ2dmO2aX;uJIF{e2G7 NVHU[GpZOjRiaB?= M17S[3Jm\HWldHnvckBqdiCFWWCxPUBuWk6DIHX4dJJme3Orb36gbY4hW0uEckOgZ4VtdHNiYX\0[ZIhOjSqIHX4dI9{fXKnIITvJFI2fU1icnXsZZRqfmVidH:gZ49vfHKxbB?= MnnPNVY1QDB{N{e=
SK-BR-3 cells NH;H[5FEgXSxdH;4bYNqfHliYYPzZZk> NUHRNo5bOjRiaB?= MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZkhemWuYYTpeoUhfG9iTmOzPVgtKEmFNUC9NE44OiEQvF2= NGnMU48yPzB7NUKyNS=>
SKBR3 cells M4PRPGZ2dmO2aX;uJIF{e2G7 NX3HN2FmUW6qaXLpeIlwdiCxZjDhdo9u[XSjc3WgbY4hcHWvYX6gV2tDWjNiY3XscJMh[nlidILpeIlifGWmIIfheIVzKHKnbHXhd4Uh[XO|YYmsJGlEPTB;MD62PEDPxE1? NVn2WVMxOTh{N{G1NVk>
RAW264.7 cells MmTHSpVv[3Srb36gZZN{[Xl? NFLhT5pCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgVGdGOiCycn;keYN1cW:wIHL5JGVKSSxiSVO1NF01NjhizszN M3fEW|IxODB2NUey
PMA-Ion-stimulated human PBL MoT3SpVv[3Srb36gZZN{[Xl? NGLlfHk2KM7:TR?= MYWyNEBp NYj3[2RHUW6qaXLpeIlwdiCxZjDDU3gzKGW6cILld5Nqd25iaX6gVG1CNUmxbj3zeIlufWyjdHXkJIh2dWGwIGDCUEBifCB3IIXNJIFnfGW{IEKwJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NE\ze3AzOzB2N{KzNS=>
HUVEC NXPhU3o6TnWwY4Tpc44h[XO|YYm= NIfO[WQyQCCq MUXBcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCjZ3HpcpN1KF[HR1\BMZN1cW23bHH0[YQh[2GyaXzsZZJ6KGSrZn\ldoVvfGmjdHnvckBqdiCKVW\FR{Bi\nSncjCxPEBpenNiYomgcYF1emmpZXygZZN{[Xl? MorUNlMyOTB2N{W=
HUVEC MorZSpVv[3Srb36gZZN{[Xl? NWO4dYpbPDhiaB?= MlTIRY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliYXfhbY5{fCCYRVfGRU1{fGmvdXzheIVlKGOnbHygdJJwdGmoZYLheIlwdiCrbjDIWXZGSyCjZoTldkA1QCCqcoOgZpkhSnKmVTDpcoNwenCxcnH0bY9vKGG|c3H5 NGi0VHIzOzFzMES3OS=>
RAW264.7 cells NE\3XXRHfW6ldHnvckBie3OjeR?= NF3Uc40zPCCq M4jFe2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKFCJRUKgdJJw\HWldHnvckBi\G2rbnnzeIVz\WRiMTDodkBxemmxcjD0c{BNWFNvY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{BjgSCHSVGsJGlEPTB;MD6wNFcxOSEQvF2= M4[2d|I1OzZyNU[x
HaCaT cells NFLOfXJHfW6ldHnvckBie3OjeR?= NGDPNXUzPCCq M3vpSGlvcGmkaYTpc44hd2ZiUFfFNkBxem:mdXP0bY9vKGmwIHj1cYFvKEijQ3HUJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCUSVGsJGlEPTB;MD6wNUDPxE1? NEfINooyPTN6N{[0Ni=>
RAW264.7 cells MVXGeY5kfGmxbjDhd5NigQ>? NUXnOWpKUW6qaXLpeIlwdiCxZjDQS2UzKHC{b3T1Z5Rqd25iaX6gUHBUNWmwZIXj[YQhdW:3c3WgVmFYOjZ2LkegZ4VtdHNuIFnDOVA:OC5yMEeg{txO MUOyOVQ2OzhyMB?=
RAW264.7 cells NW\ZWo1mTnWwY4Tpc44h[XO|YYm= M1n3XVE4NTJyIHi= MmL5TY5pcWKrdHnvckBw\iCLRl6t[4FudWFxTGDTMYlv\HWlZXSgVGdGOiCycn;keYN1cW:wIHnuJI1wfXOnIGLBW|I3PC55IHPlcIx{KGGodHXyJFE4KHSxIEKwJIhzeyCkeTDFTWEhdWW2aH;kMEBKSzVyPUCuNUDPxE1? NVPOfGhJOjVyMke5N|M>
SK-BR-3 cells MVnGeY5kfGmxbjDhd5NigQ>? M1q2WWlvcGmkaYTpc44hd2ZiQ2nQOFUxKGG{b33heIF{\SCjY4Tpeol1gSCrbjDTT{1DWi1|IHPlcIx{NCCLQ{WwQVAvPjhizszN MUWxOlQ5ODJ5Nx?=
RAW264.7 cells MUjGeY5kfGmxbjDhd5NigQ>? MVTJcohq[mm2aX;uJI9nKEORWEKtcYVlcWG2ZXSgVGdGOiCycn;keYN1cW:wIHnuJGxRWy2|dHnteYxifGWmIH3veZNmKFKDV{K2OE44KGOnbHzzJIJ6KGWweont[UBqdW23bn;hd5NigSxiSVO1NF0xNjB3IN88US=> NGK5OIoyQTJ|M{[0Oi=>
K562 cells MkDTSpVv[3Srb36gZZN{[Xl? NY[xPXBtPCCmYYnz NEPlcJNKdmirYnn0bY9vKG:oIFPPXFIhcW5iaIXtZY4hUzV4MjDj[YxteyCjc4Pld5Nm\CCjczDicI9kc2GmZTDv[kBCVUxzLVXUU{Bxem:2ZXnuMYRmeGWwZHXueEBmenm2aILvbYQh\GmoZnXy[Y51cWG2aX;uJIFnfGW{IESg[IF6eyCkeTDi[Y57cWSrbnWgd5RicW6rbnegcYV1cG:m MUOxPVE4OjF2Nh?=
RAW264.7 cells NYryfpNQTnWwY4Tpc44h[XO|YYm= M3S5bWlvcGmkaYTpc44hd2ZiQ1;YNkBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDifUBmdnq7bXWgbY1ufW6xYYPzZZktKEmFNUC9NE45OSEQvF2= NHSwUHMzODB3NkW0PS=>

... 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
  • 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
in solvent
Synonyms N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID