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).

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.

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.

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.

L 012 sodium salt, a luminol analogue, is a widely used chemiluminescent (CL) probe for active oxygen and active nitrogen. L 012 sodium salt is widely used to detect the superoxides (O2•−) derived from NADPH oxidase (Nox) to find Nox inhibitors.

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.

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

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.

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).

VAS2870 is an inhibitor of NADPH oxidase (NOX).

RV01 is a novel quinoline-substituted analogue of resveratrol that inhibits DNA damage, reduces ethanol-induced acetaldehyde dehydrogenase (ALDH2) mRNA expression, and has hydroxyl radical scavenging activity. rV01 reduces iNOS expression and has anti-neuroinflammatory effects. rV01 reduces tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion. RV01 reduced tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion, inhibited lps-induced ROS production and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activation, decreased toll-like receptor 4 (TLR4) protein expression, and inhibited lps-induced activation of mitogen-activated protein kinase (MAPK) and nuclear transcription factor-кB (NF-кB) signaling pathways.

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.

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

GKT136901 (AK120765) is an inhibitor of NOX1 4.It acts as Selective and Direct Scavenger of Peroxynitrite

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

Fulvene-5 is a chemical compound that exhibits antitumor activity. It functions as a potent inhibitor of NADPH oxidase 4 (NOX4) and possesses antioxidant properties. Additionally, Fulvene-5 acts as a reactive oxygen species (ROS) modifying agent and a powerful radioprotector.

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.

Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K Akt signalling pathway. Fluorofenidone is an analogue of AMR69. Which displays equivalent lower toxicity, antifibrotic activity, and longer half-life.

NPD6433 is a triazole indole compound that exhibits broad-spectrum activity against all screened fungal strains. It targets the enoyl reductase domain of fatty acid synthase 1 (Fas1), covalently inhibiting its flavin mononucleotide-dependent NADPH oxidase activity, thereby blocking the biosynthesis of essential fatty acids.

Imipramine Blue chloride is an effective anti-invasive agent capable of inhibiting glioma invasion. It suppresses the production of reactive oxygen species (reactive oxygen species) mediated by NADPH oxidase.

NOX4-IN-1 (Compound 14m) is an inhibitor of NADPH oxidase 4 (NOX4) that reduces the production of reactive oxygen species (ROS). It also inhibits the TGF-β1 Smad signaling pathway, leading to decreased expression of fibrosis-related proteins. Additionally, NOX4-IN-1 impedes the migration of NRK-49F cells.