Setanaxib
Based on 31 publication(s) in Google Scholar
Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 1218942-37-0
- Formula: C21H19ClN4O2
- Molecular Weight:394.85
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Publications Citing Use of MedChemExpress (MCE) Setanaxib
More- Signal Transduct Target Ther. 2024 Mar 4;9(1):58. [Abstract]
- Nature. 2024 Jul;631(8021):654-662. [Abstract]
- Redox Biol. 2023 Jun:62:102702. [Abstract]
- Redox Biol. 2023 Feb:59:102587. [Abstract]
- Basic Res Cardiol. 2022 Apr 25;117(1):24. [Abstract]
- Mol Syst Biol. 2021 Oct;17(10):e10480. [Abstract]
- Biomed Pharmacother. 2025 Apr 28:187:118108. [Abstract]
- Biomed Pharmacother. 2017 Feb:86:32-40. [Abstract]
- Antioxidants (Basel). 2022 Mar 8;11(3):513. [Abstract]
- Cell Mol Life Sci. 2023 Apr 21;80(5):127. [Abstract]
- Antioxid Redox Signal. 2019 May 20;30(15):1831-1848. [Abstract]
- Cell Biol Toxicol. 2023 Oct;39(5):2207-2225. [Abstract]
- Am J Chin Med. 2019;47(5):1113-1131. [Abstract]
- Immunology. 2021 Aug;163(4):493-511. [Abstract]
- Int J Mol Sci. 2025 Jul 15;26(14):6759. [Abstract]
- J Cell Mol Med. 2021 Jan;25(2):1012-1023. [Abstract]
- J Cell Mol Med. 2020 Feb;24(4):2552-2565. [Abstract]
- J Cell Physiol. 2021 Feb;236(2):1469-1480. [Abstract]
- Sci Rep. 2026 Mar 5;16(1):12283. [Abstract]
- Sci Rep. 2025 Jan 17;15(1):2342. [Abstract]
- Aging (Albany NY). 2022 Jul 13;14(17):6905-6916. [Abstract]
- Mol Cell Endocrinol. 2016 Dec 5:437:268-279. [Abstract]
- Viruses. 2021 Sep 12;13(9):1814. [Abstract]
- Vascul Pharmacol. 2021 Jun:138:106860. [Abstract]
- Toxicol Appl Pharmacol. 2020 Apr 17;397:115013. [Abstract]
- Arch Biochem Biophys. 2017 Feb 15:616:1-12. [Abstract]
- Surgery. 2020 Mar;167(3):620-627. [Abstract]
- PLoS One. 2026 Jun 24;21(6):e0352151. [Abstract]
- Biochem Biophys Res Commun. 2025 Dec 15:792:152981. [Abstract]
- Universidad De Salamanca. 2023
- Acta Neurochir Suppl. 2020:127:47-54. [Abstract]
Customer Validation & Images
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Cell Imaging/Staining
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Apoptosis Analysis
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Histological Imaging/Staining
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ELISA
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Biological Activity
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NOX1 |
NOX4 |
Setanaxib (GKT137831) is a potent Nox1/4 inhibitor (Kis=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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1218942-37-0
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Appearance Solid
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Molecular Weight 394.85
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Formula C21H19ClN4O2
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Color White to yellow
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SMILES
O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C3=CC=CC(N(C)C)=C3)N4C)=CC4=O
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Synonyms
GKT137831; GKT831
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (31)
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Journal Impact Factor
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Most Recent
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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.
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Nature
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.
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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
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.
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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
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.
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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
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
2025 Dec 15:792:152981. PMID: 41242297 -
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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
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
Purity & Documentation
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Data Sheet (285 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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