Home Immunology & Inflammation NADPH-oxidase inhibitor - Ferroptosis inhibitor - ROS inhibitor Setanaxib (GKT137831) For research use only.

Setanaxib (GKT137831)

Synonyms: GKT831

Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.

Setanaxib (GKT137831) Chemical Structure

Setanaxib (GKT137831) Chemical Structure

CAS: 1218942-37-0

Selleck's Setanaxib (GKT137831) has been cited by 64 publications

Purity & Quality Control

Batch: Purity: 99.91%
99.91

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HPAECs Proliferation assay 0.1-20 μM 24 h no significant effect on proliferation 22904198
HPASMCs Proliferation assay 0.1-20 μM 24 h attenuated cell proliferation 22904198
Click to View More Cell Line Experimental Data

Biological Activity

Description Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.
Targets
Ferroptosis [5] NOX1 [1]
(Cell-based assay)		 NOX4 [1]
(Cell-based assay)
110 nM(Ki) 140 nM(Ki)
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Mouse models of liver fibrosis
Dosages 60 mg/kg daily
Administration i.g.

Chemical lnformation & Solubility

Molecular Weight 394.85 Formula

C21H19ClN4O2
CAS No. 1218942-37-0 SDF Download Setanaxib (GKT137831) SDF
Smiles CN1C(=O)C=C2C(=C1C3=CC(=CC=C3)N(C)C)C(=O)N(N2)C4=CC=CC=C4Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (197.54 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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