NADPH oxidase

Apocynin is a NADPH oxidase inhibitor

Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells.

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.

GKT137831 is a first in class inhibitor targeting NOX1 and NOX4 enzymes.

APX-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.

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

GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption. GSK2795039 reduces apoptosis.

APX-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.

VAS 3947 is a selective inhibitor of NADPH oxidase (NOX), demonstrating significant antiplatelet activity. In addition to its role as an NOX inhibitor, VAS 3947 induces apoptosis through the activation of the unfolded protein response (UPR), primarily driven by protein aggregation and misfolding. This compound is valuable for research focused on oxidative stress and its implications in cardiovascular diseases.

6-Aminonicotinamide is a competitive inhibitor of glucose-6-phosphate dehydrogenase (G6PD) with a Ki value of 0.46 μM. This powerful antimetabolite of nicotinamide induces ATP depletion, enhancing the efficacy of DNA-crosslinking chemotherapy agents such as Cisplatin. Its ability to modulate metabolic pathways makes it a valuable tool in cancer research and therapeutic applications.

CPP11G is a selective inhibitor of NADPH oxidase 2 (Nox2), exhibiting an IC50 of 20 μM. This compound is valuable for the investigation of inflammatory diseases, such as vasculitis and atherosclerosis, as well as conditions characterized by Nox2 overactivation, including ischemia-reperfusion injury. Its potential applications in research can aid in understanding the role of Nox2 in various pathological processes.

VAS2870 is a selective inhibitor of NADPH oxidase (NOX), primarily targeting NOX1 and NOX2 isoforms. This compound exhibits strong antioxidant properties and effectively reduces reactive oxygen species (ROS) production. VAS2870 is widely utilized in research related to oxidative stress, inflammation, and various pathological conditions associated with NOX activity.

GKT136901 is a selective and orally active inhibitor of NADPH oxidases NOX1 and NOX4, exhibiting inhibition constants (Kis) of 160 nM and 165 nM, respectively. This compound also serves as a direct scavenger of peroxynitrite, contributing to its anti-inflammatory properties. GKT136901 is particularly useful in research focused on diabetic nephropathy, stroke, and neurodegenerative diseases, providing valuable insights into oxidative stress-related pathologies.

NoxA1ds is a selective inhibitor of NADPH oxidase 1 (NOX1), with an IC50 of 20 nM. It effectively inhibits NOX1-derived superoxide production in HT-29 human colon cancer cells. Additionally, NoxA1ds reduces VEGF-induced migration of human pulmonary artery endothelial cells under hypoxic conditions in vitro. This reagent is valuable for research into hypertension, atherosclerosis, and cancer biology.

NADPH oxidase-IN-1 is an orally active inhibitor of NADPH oxidase (Nox), specifically targeting Nox2 and Nox4 with IC50 values of 1.9 μM and 2.47 μM, respectively. This compound is notable for its ability to penetrate the blood-brain barrier, making it relevant for studies involving neuronal inflammation. NADPH oxidase-IN-1 effectively suppresses the production of pro-inflammatory cytokines and inhibits LPS-mediated microglial migration, demonstrating promising in vivo efficacy for potential therapeutic applications in neuroinflammatory conditions.

GKT136901 hydrochloride is a highly selective and orally active inhibitor of NADPH oxidase isozymes NOX1 and NOX4, exhibiting inhibition constants of 160 nM and 165 nM, respectively. This compound also functions as a direct scavenger of peroxynitrite, enhancing its therapeutic potential. GKT136901 hydrochloride is primarily utilized in research settings focusing on diabetic nephropathy, stroke, and neurodegenerative diseases, while also demonstrating notable anti-inflammatory properties.

GLX481304 is a selective inhibitor of Nox2 and Nox4, exhibiting an IC50 of 1.25 μM. This compound effectively suppresses reactive oxygen species (ROS) production in isolated mouse cardiomyocytes and enhances cardiac contractility. GLX481304 is applicable in research focused on ischemic heart injury, providing valuable insights into oxidative stress-related pathophysiology.

Fluoflavine is a selective inhibitor of NOX1 and reactive oxygen species (ROS) production. This compound effectively reduces ROS levels, NOX1-mediated signaling pathways, and prevents retinal ganglion cell death induced by oxygen-glucose deprivation. In preclinical studies, Fluoflavine has demonstrated the ability to inhibit NADPH oxidase activity and mitigate pathological retinal neovascularization in models of oxygen-induced retinopathy. It is a valuable tool for investigating retinal ischemia-reperfusion injury and proliferative retinopathy.

NOX2-IN-2 diTFA is a potent inhibitor of NOX2, specifically targeting the p47phox-p22phox protein-protein interaction with a Ki of 0.24 μM. This compound effectively inhibits reactive oxygen species (ROS) production derived from NOX2 in cellular environments. It is valuable for research applications focused on oxidative stress and related signaling pathways.

8-Hydroxycoumarin is an important intermediate in the microbial transformation of quinolones. It serves as a valuable building block in organic synthesis and is utilized in research focusing on metabolic pathways of various compounds. Its unique structural properties enable exploration in pharmacology and biochemistry, facilitating the study of enzymatic processes and potential therapeutic agents.

NOX2-IN-3 is a selective inhibitor of NADPH Oxidase 2 (NOX2). This compound has been shown to enhance the sensitivity of tumor cells to MRTX1133, indicating its potential role in cancer research. NOX2-IN-3 may be valuable for studies focused on oxidative stress and its implications in tumor biology.

YF-Mo1 is a selective inhibitor of the carbonyl reductase 1 (CBR1), exhibiting an IC50 value of 1.1 μM. This compound demonstrates potential in modulating CBR1 activity, which is significant in metabolic processes and drug metabolism. YF-Mo1 is valuable for research exploring the role of CBR1 in various physiological and pathological conditions, offering insights into metabolic therapies and drug interactions.

Saikosaponin bk1 is a specific binder for the dehydrogenase domain of NADPH oxidase 5 (NOX5), exhibiting hepatoprotective properties. It forms stable interactions with the NOX5 enzyme derived from Cylindrospermum stagnale, making it a valuable tool in studies of oxidative stress. This compound is particularly relevant in research focused on COVID-19 and alcoholic liver injury, contributing to the understanding of these conditions at a molecular level.

N-Benzyl-N-demethylpronqodine A is an inhibitor of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1), exhibiting an IC50 value of 83.3 nM. This compound plays a significant role in the study of redox biology and the mechanisms of cellular response to oxidative stress. Its application includes investigating the implications of NQO1 inhibition in various disease models, facilitating research in cancer biology and drug metabolism.

NOX2-IN-2 is a potent inhibitor of NOX2, specifically targeting the p47phox-p22phox protein-protein interaction with a Ki of 0.24 μM. This compound effectively reduces reactive oxygen species (ROS) production mediated by NOX2 in cellular contexts. NOX2-IN-2 is ideal for research applications focused on oxidative stress, inflammation, and related signaling pathways.

TSR-011-isomer is a potent anaplastic lymphoma kinase (ALK) inhibitor with an IC50 of 6 nM. This compound demonstrates significant biological activity by undergoing metabolic hydrolysis and NADPH-dependent metabolism, facilitating its clearance in biological systems. TSR-011-isomer is suitable for research focused on ALK-driven cancers, making it a valuable tool for studies in cancer biology and targeted therapy development.

CBR1-IN-3 is a potent inhibitor of carbonyl reductase 1 (CBR1), exhibiting an IC50 value of 0.034 μM. This compound serves as a valuable research tool for studies focusing on the modulation of carbonyl metabolites in various biological systems. Its ability to effectively inhibit CBR1 makes it suitable for investigating the enzyme's role in drug metabolism and potential therapeutic applications.

Diapocynin, a dimeric derivative of Apocynin, functions as a potent NADPH oxidase inhibitor. This compound exhibits significant anti-inflammatory, neuroprotective, and antioxidant activities, making it valuable for research into oxidative stress, neurodegenerative diseases, and inflammation-related conditions. Its oral bioavailability enhances its utility in various experimental settings aimed at understanding the role of reactive oxygen species in cellular processes.

NOX2-IN-1 is a selective inhibitor of nicotinamide adenine dinucleotide phosphate oxidase isoform 2 (NOX2). It effectively disrupts the protein-protein interaction between p47phox and p22phox, demonstrating favorable binding affinities and significant cellular activity. This compound is valuable for research applications focusing on oxidative stress-related diseases and inflammation pathways.

ML171 analog 1 is a selective inhibitor of NOX1, a member of the NADPH oxidase family implicated in various cellular processes. This compound exhibits significant biological activity in the modulation of reactive oxygen species, making it a valuable tool in cancer research. Its role in inhibiting NOX1 provides insights into oxidative stress related pathways in tumor biology.