GKT137831

Catalog No.S7171

GKT137831 Chemical Structure

Molecular Weight(MW): 394.85

GKT137831 is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectivelyl; ~10-fold selectivity towards NOX1, 4 and 5 over NOX2, does not inhibit XO or scavange ROS/RNS.

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4 Customer Reviews

  • Serum markers of liver injury and liver pathology in mice fed control (Ctrl) or ethanol (EtOH) for four weeks with or without GKT137831 for the last two weeks. (A) Light microscopy with hematoxylin & eosin staining shows accumulation of lipid droplets (arrows) and necrosis (arrowheads) in the liver of ethanol-fed mice, which was attenuated by GKT137831 treatment. (B) Serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities. Serum ALT and AST activities were measured by using Infinity ALT and AST Reagents. Scale bar: 20μM. Results are mean ± SD (n=6). Results for bars that do not share a letter differed significantly among groups (P <0.05). Significant differences among groups are determined by ANOVA followed by Tukey’s test.

    Biochim Biophys Acta, 2016, 1861(1 Pt A):2912-2921. . GKT137831 purchased from Selleck.

    (C) Indicated macrophages were treated with LPS (100 ng/mL) in the absence or presence of GKT137831 (1 μmol/L) for 24 h. PKM2 mRNA and lactate levels were assayed (n = 3, *, p < 0.05 versus LPS group).

    Mol Med, 2016. GKT137831 purchased from Selleck.

  • A549 cells were treated with GKT137831 (20 µM) or NAC (25 µM) after transfection with NOX4 plasmid for 48 h. Nrf2 expression was analyzed by western blotting (B). NOX4-overexpressed A549 cells were pretreated with MG132 (25 µM) after the addition of NAC or GKT137831 (C).

    Exp Cell Res, 2017, 352(2):245-254. GKT137831 purchased from Selleck.

    AGE3-BSA-induced apoptosis in A7r5 cells was mediated by NAD(P)H oxidase. (a) Cultured A7r5 cells were incubated in calcification medium containing cBSA, or AGE3-BSA (100 µg/mL) in the presence or absence of NAD(P)H oxidase inhibitors including GKT137831 (20 µM) or VAS2870 (10 µM) for three days. Apoptosis was evaluated by TUNEL assay, as described in the Method section. Cells in the culture were identified by nuclear staining with Hoechst, and evaluated under a fluorescence microscope; (b) For quantification, Hoechst and TUNEL double positive cells were counted in 10 random microscopic fields at 200× magnification, and expressed as percent TUNEL positive cells in a culture. Statistical significance of the results was analyzed by one-way ANOVA followed by LDS post-hoc test. Statistical significance was denoted as follows, ** p < 0.001 vs. AGE3-BSA.

    Int J Mol Sci, 2016, 17(9). pii: E1567. GKT137831 purchased from Selleck.

Purity & Quality Control

Choose Selective NADPH-oxidase Inhibitors

Biological Activity

Description GKT137831 is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectivelyl; ~10-fold selectivity towards NOX1, 4 and 5 over NOX2, does not inhibit XO or scavange ROS/RNS.
Targets
NOX1 [1]
(Cell-based assay)
NOX4 [1]
(Cell-based assay)
110 nM(Ki) 140 nM(Ki)
In vitro

GKT137831 attenuates hypoxia-induced H(2)O(2) release, cell proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs. [2] GKT137831 also prevents oxidative stress in response to hyperglycemia in human aortic endothelial cells. [3]

In vivo In WT and SOD1mut mice, GKT137831 (60 mg/kg i.g.) blocks liver fibrosis and downregulates markers of oxidative stress, inflammation, and fibrosis. [1] GKT137831 (60 mg/kg/d p.o.) also attenuates chronic hypoxia–induced right ventricular hypertrophy, vascular remodeling, lung cell proliferation, and hypoxic alterations in lung PPARγ and TGF-β1 expression in mouse model of chronic hypoxia exposure. [2] In diabetic apolipoprotein E-deficient mice, GKT137831 (60 mg/kg/d p.o.) attenuates diabetes mellitus-accelerated atherosclerosis. [3] Moreover, in angII-infused c-hNox4Tg mice, GKT137831 abolishes the increase in oxidative stress, suppresses Akt-mTOR and NF-κB signaling pathway and attenuates cardiac remodeling. [4]

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: Hypoxic HPASMC and HPAECs
  • Concentrations: 20 μM
  • Incubation Time: 72 hours
  • Method:

    Hypoxic HPASMC and HPAEC proliferation is determined using MTT assay, by Western blotting to detect proliferating cell nuclear antigen (PCNA) expression, or by manual cell counting after Trypan blue staining. Amplex Red Hydrogen Peroxide/Peroxidase Assay Kit is used to measure H2O2 released into the culture media from HPAECs or HPASMCs. After exposure to control or hypoxic environments for 72 hours, Amplex Red reagent is added, and the cells are returned to control or hypoxic environments for an additional hour before fluorescence measurements.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Mouse models of liver fibrosis
  • Formulation: corn oil
  • Dosages: 60 mg/kg daily
  • Administration: i.g.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL warmed (197.54 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO+2% Tween 80+30% PEG 300+ddH2O
9mg/mL

* 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 394.85
Formula

C21H19ClN4O2

CAS No. 1218942-37-0
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02010242 Completed Type 2 Diabetes Mellitus With Diabetic Nephropathy Genkyotex Innovation SAS October 2013 Phase 2

Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID