NOX4
NOX4 is a constitutively active NADPH oxidase that generates H2O2 and requires p22^phox^ for ROS production[1]. Mechanistically, isolated NOX4 directs most electron flux toward H2O2, and its high oxygen K~m~ supports oxygen-sensitive redox signaling[2]. Compared with NOX1 and NOX2, NOX4 preferentially forms H2O2 through its enlarged E-loop, which controls ROS product specificity[3]. Under hypoxia, HIF-1 induces NOX4 expression, linking NOX4 to oxygen-response pathways[4]. In fibrosis models, NOX4 mediates TGF-β1-induced fibroblast-to-myofibroblast differentiation through Smad2/3 activation[5]. In idiopathic pulmonary fibrosis, pulmonary fibroblasts show increased NOX4 expression, and NOX4 mediates TGF-β1-induced myofibroblast differentiation[6]. Therefore, NOX4 research should prioritize isoform-specific H2O2 biology, hypoxia signaling, and TGF-β-driven fibrotic remodeling rather than generalized ROS measurement.
References:
- [1]. Martyn KD, et al. Functional analysis of Nox4 reveals unique characteristics compared to other NADPH oxidases. Cell Signal. 2006 Jan;18(1):69-82. [Content Brief]
- [2]. Nisimoto Y, et al. Nox4: a hydrogen peroxide-generating oxygen sensor. Biochemistry. 2014 Aug 12;53(31):5111-20. [Content Brief]
- [3]. Takac I, et al. The E-loop is involved in hydrogen peroxide formation by the NADPH oxidase Nox4. J Biol Chem. 2011 Apr 15;286(15):13304-13. [Content Brief]
- [4]. Diebold I, et al. The NADPH oxidase subunit NOX4 is a new target gene of the hypoxia-inducible factor-1. Mol Biol Cell. 2010 Jun 15;21(12):2087-96. [Content Brief]
- [5]. Cucoranu I, et al. NAD(P)H oxidase 4 mediates transforming growth factor-beta1-induced differentiation of cardiac fibroblasts into myofibroblasts. Circ Res. 2005 Oct 28;97(9):900-7. [Content Brief]
- [6]. Amara N, et al. NOX4/NADPH oxidase expression is increased in pulmonary fibroblasts from patients with idiopathic pulmonary fibrosis and mediates TGFbeta1-induced fibroblast differentiation into myofibroblasts. Thorax. 2010 Aug;65(8):733-8. [Content Brief]
All Product Categories
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NOX4 Related Products (13)
Related Products (13)
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Setanaxib
0 ImagesSynonyms: GKT137831; GKT831Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.
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GLX351322
0 ImagesGLX351322 is an inhibitor of NADPH oxidase 4 (Nox4), and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μM.
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APX-115
0 ImagesSynonyms: Ewha-18278APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.
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GKT136901
0 ImagesGKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.
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APX-115 free base
0 ImagesSynonyms: Ewha-18278 free base; Isuzinaxib free baseAPX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base effectively prevents kidney injury.
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GK-136901
0 ImagesCat. No.: HY-124487CAS No.: 1062624-71-8GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a Ki of 160 nM for Nox1 and 165 nM for Nox4. GK-136901 potently blocks high glucose-induced intracellular reactive oxygen species production, p38-MAPK phosphorylation, and upregulation of TGF-β1/2 and fibronectin (fibronectin) in renal cells. GK-136901 also inhibits the proliferation of mouse pulmonary vascular cells under hypoxic conditions. GK-136901 is applicable to the research on the pathogenesis of type 2 diabetic nephropathy, high glucose-related renal lesions and pulmonary hypertension.
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NADPH oxidase-IN-1
0 ImagesNADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy.
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Mulberrofuran G
0 ImagesCat. No.: HY-N3239CAS No.: 87085-00-5Mulberrofuran G is a NOX inhibitor (IC50: 6.9 μM) and tyrosinase inhibitor. Mulberrofuran G exhibits anti-inflammatory, antioxidant, antiviral, antitumor, and neuroprotective effects. Mulberrofuran G can be used in the research of tumors, nervous system diseases, and other conditions.
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Hidrosmin
0 ImagesCat. No.: HY-105946CAS No.: 115960-14-0
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Niazirin
0 ImagesNiazirin is an orally active antioxidant. Niazirin can be isolated from Moringa oleifera Lam. Niazirin reduces the production levels of ROS and MDA, while increasing the levels of superoxide dismutase SOD and glutathione peroxidase GPx. Niazirin also abolishes high glucose-induced PKCζ activation and inhibits Nox4 protein expression. Niazirin exhibits excellent free radical scavenging activity. Niazirin significantly inhibits high glucose-induced proliferation of vascular smooth muscle cells. Niazirin can be used in the research of diabetic atherosclerosis.
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NOX5-IN-1
0 ImagesCat. No.: HY-174817NOX5-IN-1 (Compound 13) is a selective NADPH oxidase 5 (NOX5) inhibitor with an IC50s of 0.30 μM. NOX5-IN-1 significantly inhibits NOX5-dependent production of ROS in freestyle293 cells (EC50: 0.86 μM). NOX5-IN-1 can be used for NOXs related diseases research, such as cardiovascular, cancer and neuroinflammation.
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NOX5-IN-2
0 ImagesCat. No.: HY-174818NOX5-IN-2 (Compound 17) is a selective NADPH oxidase 5 (NOX5) inhibitor with an IC50s of 0.70 μM. NOX5-IN-2 significantly inhibits NOX5-dependent production of ROS in freestyle293 cells (EC50: 1.8 μM). NOX5-IN-2 can be used for NOXs related diseases research, such as cardiovascular, cancer and neuroinflammation.
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GLX481372
0 ImagesCat. No.: HY-148936CAS No.: 1990478-58-4GLX481372 is a NADPH Oxidase (NOX) inhibitor. GLX481372 potently inhibits NOX4/5 activities with IC50 values of 0.68 and 0.57 μM. GLX481372 also has weak inhibitory activity against NOX1, NOX2, and NOX3, with IC50 values of 7, 16 and 3.2 μM respectively. GLX481372 can inhibit ROS production. GLX481372 can be used for the researches of inflammation, cardiovascular and metabolic disease, such as diabetes.
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