NADPH Oxidase

Diphenyleneiodonium chloride (DPI)(DPI) is an irreversible inhibitor of iNOS and eNOS (IC50 values of 50 nM and 0.3 μM, respectively),and displays broad-spectrum bactericidal activity.

Apocynin (NSC 2146) is a specific NADPH-oxidase inhibitor (IC50: 10 μM).

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

Setanaxib (GKT137831) is a potent, specific dual NADPH oxidase (NOX1/4) inhibitor.

Quercetin-3-O-glucose-6''-acetate (6 -O-Acetylisoquercitrin) is an inhibitor of NADPH oxidase. Quercetin-3-O-glucose-6''-acetate has antioxidant activities.

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

Aucuparin (2,6-dimethoxy-4-phenylphenol) is a plant antibiotic with anti-inflammatory activity. Aucuparin inhibited pulmonary fibrosis in mouse models induced by bleomycin (BLM). ABTS and FRAP showed clear scavenging activity. Aucuparin inhibited superoxide production of human neutrophils induced by fmlp, and its IC50 was 17.0μM.

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

VAS 3947 is a specific inhibitor of NADPH oxidase (NOX).VAS 3947 has a potent anti-platelet effect, inducing apoptosis through UPR activation, mainly due to protein aggregation and misfolding, independent of anti-NOX activity.

gp91 ds-tat is a NADPH oxidase (NOX2) inhibitor that reduces NOX2 expression.

Protosappanin A (PTA) has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Sappanone A is a high isoflavanone that exhibits anti-inflammatory effects by modulating Nrf2.Sappanone A attenuates allergic airway inflammation in ovalbumin-induced asthma.

2-Amino-3-carboxy-1,4-naphthoquinone is an electron transfer mediator that can alter glucose metabolism in homofermentative lactic acid bacteria. It also serves as a novel growth stimulator for bifidobacteria, influencing their end-product profile through the mediated oxidation of NAD(P)H.

Paeonilactone B ((+)-Paeonilactone B), a monoterpenoid from Paeonilactone, has neuroprotective activity, inhibits oxidative stress, and suppresses H2O2-induced neurotoxicity in rat cortical cells.

5-Heneicosylresorcinol shows inhibitory effects on the release of β-hexosaminidase from RBL-2H3 cells, it also prevents triglyceride accumulation in 3T3-L1 cells. 5-Heneicosylresorcinol has nematicidal activity against nematodes Panagrellus redivivus, Cae

Chalepensin, a furanocoumarin isolated from the rutaceae plant Ruta chalepensis L., is a selective CYP2A6 inhibitor, inhibiting CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.Chalepensin exhibits Chalepensin j has antiprotozoal activity and inhibits methicillin-resistant Staphylococcus aureus (MRSA) with MIC values in the range of 32-128 μg/mL.

Zederone is a natural sesquiterpene that modulates inflammatory response, smooth muscle relaxation and endocrinology to treat dysmenorrhea; down-regulates mRNA levels of mTOR and p70s6K to inhibit the proliferation of ovarian cancer cells, and interacts with hypoglycemic proteins 3L4Y and 5UBA to be anti-diabetic and anti-oxidant.

GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.

ML-090 is NOX1-specific inhibitor(IC50 = 90 nM) which is >100 selectivity for NOX1 over NOX2, NOX3, NOX4 (all IC50s >10 μM).

2-Methoxy-4-ethylphenol inhibits Flavin-containing monooxygenase 5 (NADPH oxidase) in human neutrophils and is widely used in biochemical experiments and drug synthesis research.

VAS2870 is an inhibitor of NADPH oxidase (NOX).

1, 5-Isoquinolinediol is an inhibitor of poly(ADP-ribose) synthetase (PARP1; IC50: 0.39 μM). The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis. 1, 5-Isoquinolinediol has been used to study the role of

iNOS-IN-14 (3-bromo-1H-indazole-7-carbonitrile) is a potent nitric oxide synthase (NOS) inhibitor that inhibits the NADPH oxidase activity of nNOS.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.