Setanaxib (GKT137831) - Moligand™, 10mM in DMSO , Inhibitor of cytochrome b-245 beta chain;Inhibitor of NADPH oxidase 1;Inhibitor of NADPH oxidase 4;Inhibitor of NADPH oxidase 5, CAS No.1218942-37-0, Inhibitor of cytochrome b-245 beta chain;Inhibitor of NADPH oxidase 1;Inhibitor of NADPH oxidase 4;Inhibitor of NADPH oxidase 5

CAS: 1218942-37-0 Cat. No.: S407890 Molecular Weight: 394.85 EC Number: 942-974-8 PubChem CID: 58496428

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

GKT831 | 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1,2-dihydro-5H-pyrazolo[4,3-c]pyridine-3,6-dione

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Setanaxib (GKT137831) 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 f
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. GKT137831 also prevents oxidative stress in response to hyperglycemia in human aortic endothelial cells.

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. 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. In diabetic apolipoprotein E-deficient mice, GKT137831 (60 mg/kg/d p.o.) attenuates diabetes mellitus-accelerated atherosclerosis. 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.
Cell Data

cell lines：

Concentrations：20 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Synonyms

GKT831 | 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1, 2-dihydro-5H-pyrazolo[4, 3-c]pyridine-3, 6-dione

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of cytochrome b-245 beta chain;Inhibitor of NADPH oxidase 1;Inhibitor of NADPH oxidase 4;Inhibitor of NADPH oxidase 5

Product Properties

• ALogP: 2.366
• HBD Count: 1
• Rotatable Bond: 3

Names and Identifiers

• Isomeric SMILES: CN1C(=O)C=C2C(=C1C3=CC(=CC=C3)N(C)C)C(=O)N(N2)C4=CC=CC=C4Cl
• Alternate CAS: 1218942-37-0
• PubChem CID: 58496428
• MeSH Entry Terms: 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo(4,3-c)pyridine-3,6(2H,5H)-dione;GKT-137831;GKT-831;GKT137831;setanaxib
• Molecular Weight: 394.85

Associated Targets(Human)

CYBB Tchem Cytochrome b-245 heavy chain (1 Activities)

Discover Target: CYBB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NOX1 Tchem NADPH oxidase 1 (1 Activities)

Discover Target: NOX1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NOX4 Tchem NADPH oxidase 4 (1 Activities)

Discover Target: NOX4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NOX5 Tchem NADPH oxidase 5 (1 Activities)

Discover Target: NOX5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• DMSO(mg / mL) Max Solubility: 78
• DMSO(mM) Max Solubility: 197.5433709
• Water(mg / mL) Max Solubility: ＜1

References

1. Xiaoyong Huang, Qianqian Li, Shaobo Yun, Xiaomin Ren, Sijie Wu, Jia Cheng.  (2025)  Psoralea corylifolia seed extract bakuchiol hijacks bacterial metabolism to induce oxygen-dependent membrane lipid peroxidation in methicillin-resistant Staphylococcus aureus.  BIOORGANIC CHEMISTRY,      [PMID:41151326] [10.1016/j.bioorg.2025.109154]