Art. -Nr.: HY-12298

Setanaxib

(Synonyms: GKT137831; GKT831)

31 Cited Publications

Kundenbewertung

Based on 31 publication(s) in Google Scholar

Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with K_is of 140 and 110 nM, respectively.

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Reinheit: 99.81%
CAS. Nr.: 1218942-37-0
Formel: C₂₁H₁₉ClN₄O₂
Molecular Weight:394.85

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Setanaxib Chemical Structure

CAS. Nr.: 1218942-37-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (31)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with K_is of 140 and 110 nM, respectively.

IC₅₀ & Target

NOX1

NOX4

Alle NADPH Oxidase Isoform-spezifische Produkte anzeigen :

In Vitro

Setanaxib (GKT137831) is a potent Nox1/4 inhibitor (K_is=140±40/110±30 nM)^[1]. Administration of Setanaxib (GKT137831) throughout the 72-hour period of normoxia or hypoxia exposure attenuates HPASMC proliferation under normoxic conditions at the 20 μM concentration but had no effect on proliferation in normoxic HPAECs. In the prevention paradigm, Setanaxib (GKT137831) attenuates hypoxia-induced HPASMC and HPAEC proliferation at 5 and 20 μM. Complementary assays of cell proliferation measuring the expression of PCNA or manual cell counting confirmed that Setanaxib (GKT137831) attenuates hypoxia-induced pulmonary vascular cell proliferation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

During the last half of CCl₄ injections, some mice are treated with Setanaxib (GKT137831) daily. CCl₄-induced liver fibrosis is more pronounced in SOD1mu compared to WT mice. Liver fibrosis in both SOD1mu and WT mice is attenuated by Setanaxib (GKT137831) treatment. The increased hepatic α-SMA expression is markedly decreased in SOD1mu mice treated with Setanaxib (GKT137831), to a level similar to that of WT mice given the NOX1/4 inhibitor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1218942-37-0
Appearance Solid
Molecular Weight 394.85
Formel C₂₁H₁₉ClN₄O₂
Color White to yellow
SMILES

O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C3=CC=CC(N(C)C)=C3)N4C)=CC4=O
Synonyms

GKT137831; GKT831
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (31)

All Cell Imaging/StainingHistological Imaging/StainingApoptosis AnalysisELISAWB

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Journal Impact Factor

Signal Transduct Target Ther

Suppression of ITPKB degradation by Trim25 confers TMZ resistance in glioblastoma through ROS homeostasis. [Abstract]

2024 Mar 4;9(1):58. PMID: 38438346

Setanaxib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Mar 4;9(1):58. [Abstract]

T98G-R cells stably expressing Ctrl or ITPKB shRNAs were treated with 100 μM TMZ and/or 10 μM NOX1/4 inhibitor GKT137831 ROS was measured using the DCFDA assay.

Setanaxib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Mar 4;9(1):58. [Abstract]

For cell apoptosis, T98G-R cells were treated with 500 μM TMZ and/or 10 μM NOX1/4 inhibitor GKT137831, and assessed by the Annexin V-FITC apoptosis kit.
Nature

Emergence of large-scale cell death through ferroptotic trigger waves. [Abstract]

2024 Jul;631(8021):654-662. PMID: 38987590
Redox Biol

BNP protects against diabetic cardiomyopathy by promoting Opa1-mediated mitochondrial fusion via activating the PKG-STAT3 pathway. [Abstract]

2023 Jun:62:102702. PMID: 37116257
Redox Biol

PM2.5 increases susceptibility to acute exacerbation of COPD via NOX4/Nrf2 redox imbalance-mediated mitophagy. [Abstract]

2023 Feb:59:102587. PMID: 36608590

Setanaxib purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Feb:59:102587. [Abstract]

Treated with or without GKT137831 (60 mg/kg) or Mito-TEMPO (i. p.) to mice, Lung tissue was stained with hematoxylin and eosin (H&E).

Setanaxib purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Feb:59:102587. [Abstract]

The levels of the inflammatory cytokines TNF-α, IL-1 and IL-6 were obviously reduced in the GKT137831 (25 μM) and Mito-TEMPO treatment groups by ELISA assay.

Setanaxib purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Feb:59:102587. [Abstract]

GKT137831 (25 μM) or Mito-TEMPO treatment obviously improved the NOX4/Nrf2 redox imbalance compared with the CS + PM2.5 group.
Basic Res Cardiol

NADPH oxidase 4 contributes to TRPV4-mediated endothelium-dependent vasodilation in human arterioles by regulating protein phosphorylation of TRPV4 channels. [Abstract]

2022 Apr 25;117(1):24. PMID: 35469044
Mol Syst Biol

Multistability maintains redox homeostasis in human cells. [Abstract]

2021 Oct;17(10):e10480. PMID: 34612597
Biomed Pharmacother

Enhanced tumor suppressive effect of a new HDAC inhibitor in bladder cancer in vitro and in vivo. [Abstract]

2025 Apr 28:187:118108. PMID: 40300392
Biomed Pharmacother

Rutin protects endothelial dysfunction by disturbing Nox4 and ROS-sensitive NLRP3 inflammasome. [Abstract]

2017 Feb:86:32-40. PMID: 27936392

Setanaxib purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2017 Feb:86:32-40. [Abstract]

Effect of Rutin on TXNIP, NLRP3 and caspase-1 proteins expression. HUVECs or Nox4-overexpressed HUVECs are incubated indicated rutinor GKT for 48 h under indicated glucose condition. Bands of western blotting are analyzed by densitometry.
Antioxidants (Basel)

Combined Activity of the Redox-Modulating Compound Setanaxib (GKT137831) with Cytotoxic Agents in the Killing of Acute Myeloid Leukemia Cells. [Abstract]

2022 Mar 8;11(3):513. PMID: 35326163
Cell Mol Life Sci

NOX4-derived ROS are neuroprotective by balancing intracellular calcium stores. [Abstract]

2023 Apr 21;80(5):127. PMID: 37081190
Antioxid Redox Signal

Tanshinone IIA Activates Nuclear Factor-Erythroid 2-Related Factor 2 to Restrain Pulmonary Fibrosis via Regulation of Redox Homeostasis and Glutaminolysis. [Abstract]

2019 May 20;30(15):1831-1848. PMID: 30105924

Setanaxib purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2019 May 20;30(15):1831-1848. [Abstract]

The western blot assay shows that Tan-IIA and GKT137831 inhibit Smad3 activation in response to TGF-β1 by dephosphorylation.
Cell Biol Toxicol

Effects of SIDT2 on the miR-25/NOX4/HuR axis and SIRT3 mRNA stability lead to ROS-mediated TNF-α expression in hydroquinone-treated leukemia cells. [Abstract]

2023 Oct;39(5):2207-2225. PMID: 35302183
Am J Chin Med

Salvia miltiorrhiza Restrains Reactive Oxygen Species-Associated Pulmonary Fibrosis via Targeting Nrf2-Nox4 Redox Balance. [Abstract]

2019;47(5):1113-1131. PMID: 31352786
Immunology

NLR family pyrin domain containing 3 (NLRP3) and caspase 1 (CASP1) modulation by intracellular Cl- concentration. [Abstract]

2021 Aug;163(4):493-511. PMID: 33835494
Int J Mol Sci

Aβ40 Improves Cerebrovascular Endothelial Function via NOX4-Dependent Hydrogen Peroxide Release. [Abstract]

2025 Jul 15;26(14):6759. PMID: 40725005
J Cell Mol Med

Salvianolate ameliorates oxidative stress and podocyte injury through modulation of NOX4 activity in db/db mice. [Abstract]

2021 Jan;25(2):1012-1023. PMID: 33332718
J Cell Mol Med

SIRT3, PP2A and TTP protein stability in the presence of TNF-α on vincristine-induced apoptosis of leukaemia cells. [Abstract]

2020 Feb;24(4):2552-2565. PMID: 31930676
J Cell Physiol

IRE1α/NOX4 signaling pathway mediates ROS-dependent activation of hepatic stellate cells in NaAsO2 -induced liver fibrosis. [Abstract]

2021 Feb;236(2):1469-1480. PMID: 32776539
Sci Rep

NOX1/4 drives hepatic iron and lipid dysregulation, redox imbalance, and inflammation in ethanol-fed mice. [Abstract]

2026 Mar 5;16(1):12283. PMID: 41786915
Sci Rep

20-HETE mediates Ang II-induced cardiac hypertrophy via ROS and Ca2+ signaling in H9c2 cells. [Abstract]

2025 Jan 17;15(1):2342. PMID: 39825084
Aging (Albany NY)

NOX4 promotes Kupffer cell inflammatory response via ROS-NLRP3 to aggravate liver inflammatory injury in acute liver injury. [Abstract]

2022 Jul 13;14(17):6905-6916. PMID: 35832027
Mol Cell Endocrinol

Andrographolide ameliorates diabetic nephropathy by attenuating hyperglycemia-mediated renal oxidative stress and inflammation via Akt/NF-κB pathway. [Abstract]

2016 Dec 5:437:268-279. PMID: 27378149
Viruses

A Bioluminescent 3CLPro Activity Assay to Monitor SARS-CoV-2 Replication and Identify Inhibitors. [Abstract]

2021 Sep 12;13(9):1814. PMID: 34578395
Vascul Pharmacol

Serotonin and chronic hypoxic pulmonary hypertension activate a NADPH oxidase 4 and TRPM2 dependent pathway for pulmonary arterial smooth muscle cell proliferation and migration. [Abstract]

2021 Jun:138:106860. PMID: 33794383
Toxicol Appl Pharmacol

Arsenic trioxide-induced p38 MAPK and Akt mediated MCL1 downregulation causes apoptosis of BCR-ABL1-positive leukemia cells. [Abstract]

2020 Apr 17;397:115013. PMID: 32305283
Arch Biochem Biophys

CFTR impairment upregulates c-Src activity through IL-1β autocrine signaling. [Abstract]

2017 Feb 15:616:1-12. PMID: 28088327
Surgery

NOX4 overexpression is a poor prognostic factor in patients undergoing curative esophagectomy for esophageal squamous cell carcinoma. [Abstract]

2020 Mar;167(3):620-627. PMID: 31889545
PLoS One

Inhibition of SUR1-TRPM4 attenuates astrocyte swelling and reactivity under oxygen-glucose deprivation/reoxygenation. [Abstract]

2026 Jun 24;21(6):e0352151. PMID: 42340956
Biochem Biophys Res Commun

Regorafenib promotes ferroptosis in acute myeloid leukemia by upregulating NOX4. [Abstract]

2025 Dec 15:792:152981. PMID: 41242297
Universidad De Salamanca

2023
Acta Neurochir Suppl

Nox2 and Nox4 Participate in ROS-Induced Neuronal Apoptosis and Brain Injury During Ischemia-Reperfusion in Rats. [Abstract]

2020:127:47-54. PMID: 31407062

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (316.58 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5326 mL

12.6630 mL

25.3261 mL

5 mM

0.5065 mL

2.5326 mL

5.0652 mL

10 mM

0.2533 mL

1.2663 mL

2.5326 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

Monolayers of HPAECs and HPASMCs are propagated in culture and placed in normoxic (21% O₂, 5% CO₂) or hypoxic (1% O₂, 5% CO₂) conditions for 72 hours. Setanaxib (GKT137831) (0.1-20 μM), or vehicle (1% DMSO) are added to the culture medium at the onset (prevention regimen) or during the last 24 hours (intervention regimen) of a 72-hour hypoxia exposure regimen^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Specific pathogen-free, wild-type (WT) C57BL/6J mice are used. For the carbon tetrachloride (CCl₄) model of liver fibrosis, 6 week old male mice are injected intraperitoneally with CCl₄, which is diluted 1:3 in corn oil, or with vehicle (corn oil) at a dose of 0.5 μL/g of body weight twice a week for a total of 12 injections. During the last half of CCl₄ treatment, mice are treated with 60 mg/kg of the NOX1/4 inhibitor Setanaxib (GKT137831) or vehicle by intragastric injection daily. Mice are sacrificed 48 hours after the last CCl₄ injection. For the bile duct ligation (BDL) model, 6 week old male mice are anesthetized. After laparotomy, the common bile duct is ligated twice and the abdomen closed. The sham operation is performed similarly without BDL. From 11 days after operation, mice are treated with 60 mg/kg of the NOX1/4 inhibitor Setanaxib (GKT137831) or vehicle by daily intragastric lavage. Mice are sacrificed 21 days after operation. Serum levels of alanine aminotransferase (ALT) are measured with a commercial kit.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Aoyama T, et al. Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Hepatology. 2012 Dec;56(6):2316-27. [Content Brief]

[2]. Green DE, et al. The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation. Am J Respir Cell Mol Biol. 2012 Nov;47(5):718-26. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5326 mL	12.6630 mL	25.3261 mL	63.3152 mL
	5 mM	0.5065 mL	2.5326 mL	5.0652 mL	12.6630 mL
	10 mM	0.2533 mL	1.2663 mL	2.5326 mL	6.3315 mL
	15 mM	0.1688 mL	0.8442 mL	1.6884 mL	4.2210 mL
	20 mM	0.1266 mL	0.6332 mL	1.2663 mL	3.1658 mL
	25 mM	0.1013 mL	0.5065 mL	1.0130 mL	2.5326 mL
	30 mM	0.0844 mL	0.4221 mL	0.8442 mL	2.1105 mL
	40 mM	0.0633 mL	0.3166 mL	0.6332 mL	1.5829 mL
	50 mM	0.0507 mL	0.2533 mL	0.5065 mL	1.2663 mL
	60 mM	0.0422 mL	0.2111 mL	0.4221 mL	1.0553 mL
	80 mM	0.0317 mL	0.1583 mL	0.3166 mL	0.7914 mL
	100 mM	0.0253 mL	0.1266 mL	0.2533 mL	0.6332 mL

Keywords

Setanaxib

31 Cited Publications

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Setanaxib

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Publications Citing Use of MedChemExpress (MCE) Setanaxib

Alle NADPH Oxidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (31)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Setanaxib Related Classifications

HY-12298 Related Classifications