NOX4 Inhibitor

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

GLX351322 is an inhibitor of NADPH oxidase 4 (Nox4), and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC₅₀ of 5 μM.

APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with K_i values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.

GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with K_is 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.

APX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with K_i 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.

GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a K_i 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.

NADPH 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.

Mulberrofuran 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.

Hidrosmin, a flavonoid, is derived from Diosmin (HY-N0178). hidrosmin exerts a beneficial effect against diabetic nephropathy (DN) by reducing inflammation, oxidative stress, and senescence pathways. Hidrosmin can be used for the research of venous insufficiency and diabetes mellitus.

Niazirin 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.

NOX5-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.

NOX5-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.

GLX481372 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.