NOX1 Inhibitor

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

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.

Prochlorperazine dimaleate is an orally active phenothiazine-type dopamine D2 receptor (D2R) antagonist. Prochlorperazine exhibits anti-cancer activity in vitro against various cancer cell lines. Prochlorperazine dimaleate exhibits IC₅₀ values of 6.4 μM, 4.5 μM and 2.3 μM for NOX1, NOX2 and NOX5, respectively. Prochlorperazine dimaleate has antedesmosidic activity against dengue virus (DENV). Prochlorperazine dimaleate can be used for research on nausea, vomiting, migraine, and schizophrenia.

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.

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.

AMPAR modulator-12 is a blood-brain barrier-permeable AMPAR positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances AMPAR-mediated currents, promotes excitatory postsynaptic transmission and restores AMPAR function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression.

NoxA1ds is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC₅₀=20 nM). NoxA1ds inhibits NOX1-derived O^2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds can be used in the study of hypertension, atherosclerosis and tumors.

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.

Fluoflavine (ML-090) is a selective NOX1 inhibitor and reactive oxygen species inhibitor. Fluoflavine reduces reactive oxygen species production, NOX1-mediated downstream signaling events, and oxygen-glucose deprivation-induced retinal ganglion cell death. Fluoflavine inhibits NADPH oxidase activity and pathological retinal neovascularization induced by oxygen-induced retinopathy in the retinas of ischemic mice. Fluoflavine can be used in studies related to retinal ischemia-reperfusion injury and proliferative retinopathy.

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.

NoxA1ds TFA is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC₅₀=20 nM). NoxA1ds TFA inhibits NOX1-derived O^2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds TFA can be used in the study of hypertension, atherosclerosis and tumors.

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.

ML171 analog 1 (Crop ID: SR-03000000698-1 SID: 57287906) is a NOX1 inhibitor. ML171 analog 1 can be used in cancer research.