NS-398 (NS398)

Catalog No.S8433 Batch:S843301

Print

Technical Data

Formula

C13H18N2O5S
Molecular Weight 314.36 CAS No. 123653-11-2
Solubility (25°C)* In vitro DMSO 62 mg/mL (197.22 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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].
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 Assay:

[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.  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 Study:

[3]
  • Animal Models

    CD1 mice

  • Dosages

    20 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2017, 8(50): 87658-87666]

Selleck's NS-398 (NS398) has been cited by 15 publications

Embryo-derive TNF promotes decidualization via fibroblast activation [ Elife, 2023, 12e82970] PubMed: 37458359
Embryo-derive TNF promotes decidualization via fibroblast activation [ Elife, 2023, 12e82970] PubMed: 37458359
COX-2 is required to mediate crosstalk of ROS-dependent activation of MAPK/NF-κB signaling with pro-inflammatory response and defense-related NO enhancement during challenge of macrophage-like cell line with Giardia duodenalis [ PLoS Negl Trop Dis, 2022, 16(4):e0010402] PubMed: 35482821
Celecoxib impairs primary human myoblast proliferation and differentiation independent of cyclooxygenase 2 inhibition [ Physiol Rep, 2022, 10(21):e15481] PubMed: 36325583
PP2 Ameliorates Renal Fibrosis by Regulating the NF-κB/COX-2 and PPARγ/UCP2 Pathway in Diabetic Mice [ Oxid Med Cell Longev, 2021, 2021:7394344] PubMed: 34580604
Cancer-associated fibroblasts educate normal fibroblasts to facilitate cancer cell spreading and T-cell suppression [ Mol Oncol, 2021, 10.1002/1878-0261.13077] PubMed: 34379869
NS398 as a potential drug for autosomal-dominant polycystic kidney disease: Analysis using bioinformatics, and zebrafish and mouse models [ J Cell Mol Med, 2021, 25(20):9597-9608] PubMed: 34551202
Oxidized-LDL inhibits testosterone biosynthesis by affecting mitochondrial function and the p38 MAPK/COX-2 signaling pathway in Leydig cells [ Cell Death Dis, 2020, 11(8):626] PubMed: 32796811
Cyclooxygenase-2 Inhibition Reduces Autophagy of Macrophages Enhancing Extraintestinal Pathogenic Escherichia coli Infection. [ Front Microbiol, 2020, 17;11:708] PubMed: 32362888
Enhanced Effect of IL-1 β-Activated Adipose-Derived MSCs (ADMSCs) on Repair of Intestinal Ischemia-Reperfusion Injury via COX-2-PGE 2 Signaling [ Stem Cells Int, 2020, 17;2020:2803747] PubMed: 32377202

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.