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GKT137831 (Setanaxib) attenuated hypoxia-induced H(2)O(2) release, proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs in vitro.
In vivo GKT137831 inhibited hypoxia-induced increases in TGF-β1 and reductions in PPARγ expression and attenuated RVH and pulmonary artery wall thickness but not increases in RVSP or muscularization of small arterioles.Targeting Nox4 with GKT137831 provides a novel strategy to attenuate hypoxia-induced alterations in pulmonary vascular wall cells that contribute to vascular remodeling and RVH, key features involved in PH pathogenesis. GKT137831, attenuated liver fibrosis and ROS production in both SOD1mu and WT mice as well as messenger RNA expression of fibrotic and NOX genes. Treatment with GKT137831 suppressed ROS production and NOX and fibrotic gene expression, but not Rac1 activity, in SOD1mut and WT HSCs.
FASEB J. 2021 Apr;35(4):e21531.
Inhibition of NADPH oxidase 4 attenuates lymphangiogenesis and tumor metastasis in breast cancer
GKT137831 (Setanaxib) purchased from AbMole
J Sex Med. 2021 Dec;18(12):1970-1983.
NOX1/4 Inhibitor GKT-137831 Improves Erectile Function in Diabetic Rats by ROS Reduction and Endothelial Nitric Oxide Synthase Reconstitution
GKT137831 (Setanaxib) purchased from AbMole
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Source | Cell Physiol Biochem (2018). Figure 5. GKT137831 |
| Method | DCF assays | |
| Cell Lines | AML12 cells | |
| Concentrations | 0.2, 1 and 5 μM | |
| Incubation Time | 1 h | |
| Results | Importantly, the application of GKT137381 dose-dependently decreased the percentage of PA-induced apoptosis in cultured AML12 cells |
| Molecular Weight | 394.85 |
| Formula | C21H19ClN4O2 |
| CAS Number | 1218942-37-0 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related NADPH Oxidase Products |
|---|
| Apocynin
Apocynin is a nADPH-oxidase inhibitor. |
| ML171
ML171 is a potent and selective inhibitor of NADPH-oxidase with IC50s of 0.25 μM, 5 μM, 3μM, 5 μM and 5.5 μM for NOX1, NOX2, NOX3, NOX4 and xanthine oxidase, respectively. ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay. |
| VAS2870
VAS2870 is a cell-permeable and specific NADPH oxidase (NOX) inhibitor that effectively suppresses growth factor-mediated ROS liberation in VSMC. |
| APX-115
APX-115 is a potent, orally active inhibitor of pan NADPH oxidase (Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. |
| GLX351322
GLX351322 is an NADPH oxidase 4 inhibitor, which inhibits hydrogen peroxide production from tetracycline inducible NOX4-overexpressing cells with IC50 of 5 uM. |
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