NOS

L-NMMA acetate (Tilarginine acetate) is an inhibitor of nitric oxide synthase of all NOS isoforms (i.e. NOS1, NOS2, and NOS3). The Ki values are 0.18, 0.4, and 6 µM for nNOS, eNOS, and iNOS, respectively.

Micheliolide(MCL) is a sesquiterpene lactone which inhibits various inflammatory response.

Cindunistat (free base) is an orally available selective iNOS inhibitor for the study of arthritis.

Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also binds to the CB2 receptor; it can relieve interocular pressure, which may be of benefit in the treatment of glaucoma.

Hydrangenol is a natural product and can be isolated from Hydrangea serrata leaves. Hydrangenol is an antiphotoaging compound with oral activity. Hydrangenol can reduce MMP and inflammatory cytokine expression and increase moisturizing factors and antioxidant genes level, result in preventing wrinkle formation.

Syringin (eleutheroside-b) is a compound with antitumor, antiproliferative, immunomodulatory and platelet aggregation inhibiting effects.

Banoxantrone dihydrochloride (AQ4N dihydrochloride) is a novel hypoxic cytotoxin that selectively kills hypoxic cells through an iNOS-dependent mechanism.

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.

1. Negletein (7-O-Methylbaicalein) has anti-inflammatory and immunomodulatory activities via inhibition of TNF-α, iNOS and IL-1β. 2. Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. 3. Negletein shows a comparable redox-active potential, and it (50 μM, 4 h) can activate Nrf2. 4. Negletein shows significant antimicrobial activity. 5. Negletein has anti-hypoxia activity, it can significantly prolong the survival time of hypoxic mice.6. Negletein has anti- Alzheimer's disease activity, it inhibits the iron-dependent formation of ROS and also blocks the iron-induced oligomerization of amyloid beta 42 in vitro. 7. Negletein (IC50: 3.89 + - 0.39 microM) exhibits potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor.

L-NAME hydrochloride (L-NAME HCl), a cell-permeable NO synthase inhibitor, displays Ki values of 4.4 μM, 15 nM, and 39 nM, for iNOS (mouse) , nNOS (bovine) , and eNOS (human), respectively.

Technical grade is a natural from Magnolia sieboldii

Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either in vitro or in vivo.Demethyleneberberine suppresses CYP2E1, hypoxia inducible factor α, and inducible nitric oxide synthase, which contributes to oxidative stress and restored sirtuin 1 AMP-activated protein kinase peroxisome proliferator-activated receptor-γ coactivator-1α pathway-associated fatty acid oxidation in chronic ethanol-fed mice.

S-(2-aminoethyl) Isothiourea (dihydrobromide) is a non-selective inhibitor of all NOS isoforms. For human nNOS, eNOS, and iNOS, the Ki values are 1.8, 2.1, and 0.59 µM, respectively

α-Humulene (Alpha-caryophyllene) is extracted from S.officinalis essential oil.α-Humulene can inhibit tumor cell growth.α-Humulene also shows anti-inflammatory effects, probably by interfering with TNFalpha production and COX-2 and iNOS expression.

Tubuloside A ( 8.6 microM) can inhibit D-galactosamine-induced death of hepatocytes. Tubuloside A has NO radical-scavenging activity, which possibly contributes to its anti-inflammatory effects.Tubuloside A shows stronger free radical scavenging activitie

23-epi-26-Deoxyactein (27-Deoxyactein) has anti-inflammatory activity, it inhibits nitric oxide production by reducing iNOS expression without affecting activity of the enzyme. It also has anti-cancer activity, it can inhibit growth of the MCF7 human breast cancer cells and induce cell cycle arrest at G1.

1. Ruscogenin has anti-inflammatory activity, suppressed zymosan A-evoked peritoneal total leukocyte migration in mice in a dose-dependent manner, 2. Ruscogenin inhibited adhesion of leukocytes to a human umbilical vein endothelial cell line (ECV34) injured by tumor necrosis factor-alpha (TNF-alpha) in a concentration-dependent manner. 3. Ruscogenin significantly attenuate LPS-induced acute lung injury via inhibiting expressions of TF and iNOS and NF-kappa B p65 activation.

AVE-9488 is a novel endothelial NO synthase (eNOS) enhancer that upregulates eNOS expression, induces NO production, and may ameliorate portal hypertension.

Aminoguanidine hydrochloride (Hydrazinecarboximidamide) is a diamine oxidase and NO synthase inhibitor, used in the treatment of diabetic nephropathy.

NOS1-IN-1(nNOS Inhibitor I) is a potent, selective and cell permeable nNOS inhibitor (Ki: 120 nM).NOS1-IN-1 has a Ki value of 39 μM for eNOS and 325 μM for iNOS.NOS1-IN-1 can be used for the study of neurological disorders such as cerebral palsy.

Regaloside B, a phenylpropanoid isolated from Lilium longiflorum, exhibits anti-inflammatory activity by inhibiting the expression of iNOS (inducible nitric oxide synthase) and COX-2 (cyclooxygenase-2).

Carboxyebselen (HOOC-Ebs) is an endothelial nitric oxide synthase (eNOS) inhibitor that is potent and selective.

β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)

Soyasaponin Ab may represent a viable candidate for effective vaccine adjuvant, TLR4 receptor dependent pathway may be involved in immune stimulatory effects of soyasaponin Ab.

Eburicoic acid (ZINC4655149) exhibits anti-inflammatory and antioxidant activity thereby protecting the liver from CCl4-induced hepatic damage and can be used in studies about anti-liver cancer.

Isolinderalactone shows anti-inflammatory and anticancer capacity, and it exhibits moderate iNOS inhibitory activity, with the IC50 value of 0.30 uM.

Ac2-26 ammonium is an Annexin-A1 (AnxA1) N-terminal derived peptide with anti-inflammatory activity and alleviates liver ischemia-reperfusion injury in mice by regulating IL-22 IL-22R1 STAT3 signaling and eNOS pathways.

MEG hemisulfate (Mercaptoethylguanidine hemisulfate) acts as a highly potent and selective suppressor of inducible NO synthase (iNOS), demonstrating EC50 values of 11.5 μM for iNOS, 110 μM for ecNOS, and 60 μM for bNOS in tissue homogenates. It is notably effective as a peroxynitrite scavenger and blocks peroxynitrite-triggered oxidative mechanisms. Furthermore, this compound offers protective benefits across various experimental inflammation prototypes, such as ischemia reperfusion injury, hemorrhagic shock, periodontitis, inflammatory bowel disease, and both endotoxic and septic shock.

Pelargonidin chloride shows protective effect against CTN-induced oxidative stress in HepG2 cells and up-regulated the activity of detoxification enzyme levels through Keap1 Nrf2 signaling pathway.

1400W dihydrochloride (N-(3-(Aminomethyl)benzyl)acetamidine) is a highly effective and specific inhibitor of inducible NOS2 (iNOS).

Cnidicin has anti-allergic and anti-inflammatory activity, it inhibits the degranulation of mast cell and the NO generation in RAW 264.7 cells(IC50 value, 7.5 microM). Cnidicin exhibits a significant inhibition on the proliferation of cultured human tumor

Schisandrone (Arisantetralone C) is a 4-aryltetrahydrofuran lignan extracted from the dried fruit of Schisandra chinensis.

Flavone (2-Phenyl-4-chromone) have effects on CYP (P450) activity which are enzymes that metabolize most drugs in the body.

AICAR phosphate (Acadesine phosphate) is an AMPK activator and inhibitor of autophagy, YAP, and mitophagy. It serves as an adenosine analog, regulating glucose and lipid metabolism, and inhibiting the production of pro-inflammatory cytokines and iNOS.

Neoandrographolide (Neoandrographiside) has potent hypolipidemic effect and protects the cardiovascular without significant liver damage.Neoandrographolide has anti-inflammatory effect, might result from inhibition of iNOS and COX-2 expression through inhibiting p38 MAPKs activation.Neoandrographolide as chemosensitizer in S-Jurkat and X chromosome-linked inhibitor of apoptosis protein (XIAP)-overexpressing Jurkat cells, a model for chemoresistance.

6-Formylpterin (Pterin-6-aldehyde) is an inhibitor of Xanthine Oxidase (Ki ~0.6 nM) with potent neuroprotective effects against transient IRI in gerbils.6-Formylpterin induces intracellular ROS generation in HL-60 cells as well as apoptosis ( 6-Formylpterin inhibits the expression of iNOS, produces hydrogen peroxide intracellularly and restores the impaired bactericidal activity of human neutrophils.

3,4-O-Isopropylidene-shikimic acid (3,4-O-Isopropylidene shikimic acid) exhibits significant anti-inflammatory, anti-thrombosis, antioxidant, and analgesic effects, and provides protective benefits against trinitrobenzenesulfonic acid-induced experimental colitis in rats, likely because of its antioxidant properties.

Ermanin, a flavonoid isolated from Tanacetum microphyllum, inhibits platelet aggregation and exhibits anti-tuberculosis, anti-viral bacterial, and potential anti-HIV-1 activities. It has anti-inflammatory properties through the inhibition of iNOS and COX-2 expression and is effective at lower concentrations in inhibiting Dione juno larvae.

Cyclo(L-Pro-L-Val), a 2,5-diketopiperazine extracted from the fruits of Mycobacterium chiliolyticum AZ2 and Mycobacterium leprae, possesses anti-inflammatory activity and virulence activity against phytopathogenic microorganisms (e.g., R. fascians LMG 3605) and inhibits Gram-positive plant pathogens.Cyclo(L-Pro-L-Val) significantly inhibited IKKα phosphorylation and IκBα and NF-κB activation as well as iNOS and COX-2 activation in a concentration Cyclo(L-Pro-L-Val) significantly inhibited the phosphorylation of IKKα, IKKβ, IκBα, and NF-κB, as well as the activation of iNOS and COX-2 in a concentration-dependent manner, and is a potential therapeutic agent for the treatment of inflammation-related diseases.

GW274150 is an orally active, selective and potent dual inhibitor of NADPH-dependent human nitric oxide synthase (iNOS) (Kd=40 nM) and rat inducible nitric oxide synthase (iNOS).GW274150 has a low activity against endothelial nitric oxide synthase (eNOS) and neuronal nitric oxide synthase (nNOS) in humans and rats. GW274150 showed protective effects in an inflammatory model of acute lung injury.

Myricetin 3-O-galactoside (Myricetin 3-O-beta-D-galactopyranoside) can inhibit xanthine oxidase (xanthine oxidase; XO) activity, lipid peroxidation and scavenging free radicals. Myricetin 3-O-galactoside has many effects, including cytotoxicity, anti-oxidation, anti-genotoxicity, anti-infectivity, anti-inflammatory and antioxidant activities, and its main effect is to inhibit the synthesis of inducible nitric oxide synthase (iNOS). The IC50 of Myricetin 3-O-galactoside inhibited lipid peroxidation was 160 μg mL.

Stylopine is a protoberberine-type alkaloid that has potential biological activities, including anti-inflammatory activity.

Diallyl disulfide has antitumor effect, the effect can be enhanced by miR-200b and miR-22.

EX-A5758 is a novel putative small molecule nNOS-NOS1AP inhibitor, suppressing inflammatory nociception and chemotherapy-induced neuropathic pain and synergizes with paclitaxel to reduce tumor cell viability.

3-Bromo-7-nitroindazole is a specific neuronal nitric oxide synthase (nNOS) inhibitor that affects the synthesis of the intercellular messenger NO throughout the brain and body.

Miconazole (R18134) is an imidazole antifungal agent used both topically and via intravenous infusion.

Catalposide is a potent inducer of (HO)-1 isolated from Catalpa ovate G. Don (Bignoniaceae). Catalposide possesses antioxidant, anti-apoptotic, anti-microbial, anti-tumoral, and anti-inflammatory properties.

S-Methylisothiourea sulfate ((S)-Methylisothiourea sulfate) is a potent and selective inhibitor of iNOS and exerts beneficial effects in rodent models of septic shock[1].