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NOS inhibitor
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor. -
GPR3 agonist/NOS/ NADPH oxidases inhibitor
Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells. -
GTP cyclohydrolase I inhibitor
2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis), blocks BH4 synthesis and suppresses NO production. -
INOS inhibitor
1400W Dihydrochloride is a slow, tight binding, potent and highly selective inhibitor of inducible nitric oxide synthase (Kd = 7 nM). Selective over nNOS and eNOS (Ki values are 2 and 50 μM respectively). Cell-permeable and active in vivo. -
NOS cofactor
Biopterin is the oxidized form of tetrahydro-L-biopterin (BH4), a nitric oxide synthase (NOS) cofactor. L-Biopterin can be reduced to BH4 via thioredoxin reductase followed by dihydropteridine reductase or reduced glutathione. It is extremely toxic to human melanocytes in culture (IC50 = 0.2 uM after 48 hrs). -
Analog of curcumin
Dimethoxycurcumin, a synthetic curcumin analogue with higher metabolic stability, inhibits NO production, inducible NO synthase expression and NF-kappaB activation in RAW264.7 macrophages activated with LPS. -
Nitric oxide donor
Isosorbide dinitrate is an organic nitrate ester and nitric oxide (NO) donor in the same class as nitroglycerin. Isosorbide dinitrate increases oxygenation of tumor tissue in vivo in a mouse xenograft model. It also inhibits platelet aggregation in vitro and in vivo at concentrations in the micromolar range. Formulations containing isosorbide dinitrate have been used for the treatment of angina pectoris. - Tetrahydrobiopterin is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
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NOS inhibitor
Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a number of pathological states.- Raul Salinas, .et al. , PLoS One, 2023, Mar 2;18(3):e0282155 PMID: 36862634
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nitric oxide synthases inhibitor
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively. -
NO synthase inhibitor
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor. -
nNOS inhibitor
3-Bromo-7-nitroindazole is a more potent and selective inhibitor of neuronal nitric oxide synthase (nNOS) than eNOS or inducible nitric oxide synthase (iNOS). -
nNOS inhibitor
7-Nitroindazole, a heterocyclic compound, acts as a selective inhibitor for neuronal nitric oxide synthase showing a 10-fold selectivity for neuronal NOS. -
NOS inhibitor
L-NMMA acetate (NG-monomethyl-L-arginine acetate) is a non-selective nitric oxide synthase (NOS) inhibitor that targets all three NOS isoforms: neuronal (nNOS/NOS1), endothelial (eNOS/NOS3), and inducible (iNOS/NOS2). It exhibits Ki values of approximately 0.18 µM for rat nNOS, 0.4 µM for human eNOS, and 6 µM for mouse iNOS, making it a valuable tool for studying nitric oxide–mediated physiological and pathological processes. -
PPAR agonist
Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases. -
PPAR agonist
Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions. -
NO Synthase Inhibitor
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM. -
Anticancer Agent
(+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage. -
ROS/iNOS/TNF-α/COX-2 Inhibitor
Callistephin chloride is an anthocyanin that functions as an inhibitor of reactive oxygen species (ROS) and nitric oxide synthase (iNOS), as well as tumor necrosis factor-alpha (TNF-α) and cyclooxygenase-2 (COX-2). This compound regulates the expression of inflammatory and apoptosis-related proteins by inhibiting p38 phosphorylation, thereby enhancing the protective effects against microglial cell damage. Callistephin chloride also significantly reduces ROS levels, mitigates glutamate excitotoxicity, and provides neuroprotection to cerebellar granule neurons. Additionally, it inhibits the proliferation and metastasis of breast cancer cells through the induction of apoptosis. -
nNOS Inhibitor
NXN-188 is a selective nNOS inhibitor that also acts as an agonist for the 5HT-1B/1D receptors. This compound exhibits potential in modulating neurogenic inflammation and is particularly relevant in research focused on migraine pathophysiology and treatment strategies. Its dual action supports investigations into the intricate mechanisms underlying headache disorders. -
iNOS Inhibitor
1400W is a selective inhibitor of inducible nitric-oxide synthase (iNOS) with a Kd value of ≤ 7 nM, demonstrating slow and tight binding characteristics. This compound effectively inhibits iNOS induction in microglial cells, leading to reduced nitric oxide production, which in turn helps alleviate oxidative stress and neuronal apoptosis in the rat cerebral cortex. 1400W's ability to ameliorate spatial memory dysfunction associated with acute hypobaric hypoxia-reoxygenation makes it a valuable tool for research in neuroprotection and neurodegenerative disease studies. -
iNOS Inhibitor
iNOS-IN-5 (Compound BN-4) is a potent inhibitor of inducible nitric oxide synthase (iNOS) with an IC50 of 0.1707 μM, effectively reducing nitric oxide levels in LPS-induced RAW264.7 cells. This compound demonstrates protective properties against hypoxic injury by decreasing reactive oxygen species (ROS) and lactate dehydrogenase expression, exhibiting significant anti-necrosis and anti-apoptosis effects. Additionally, iNOS-IN-5 has shown neuroprotective activity and protective effects against cerebral ischemia in SD rat models, while also being capable of penetrating the blood-brain barrier. -
iNOS Inhibitor
Myricadenin A is an inhibitor of inducible nitric oxide synthase (iNOS), demonstrating effective inhibition of nitric oxide production with an EC₅₀ value of 18.1 μM. Additionally, it exhibits moderate ABTS free radical scavenging activity (SC₅₀ = 175.4 μM) and shows weak antibacterial activity against tuberculosis (MIC = 80.0 μg/mL). Myricadenin A is suitable for studies focused on inflammation and oxidative stress. -
iNOS/COX-2 Inhibitor
Ermanin is a flavonoid extracted from Tanacetum microphyllum, known for its potent inhibitory effects on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Its biological activities include anti-inflammatory, anti-tuberculous, and anti-viral/bacterial properties, making it a valuable reagent in research related to inflammation and infectious diseases. Ermanin is useful for exploring the pathways associated with nitric oxide production and prostaglandin synthesis in various biological contexts. -
iNOS/ PKC-θ Dual Inhibitor
(Rac)-Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). It selectively inhibits iNOS while also reducing the stability of the PKC-θ protein, showcasing significant biological activity. Research indicates that (Rac)-Anemonin can alleviate symptoms in dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it valuable for studying inflammation-related diseases. -
iNOS/ PKC-θ Dual Inhibitor
Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). This compound significantly reduces the translation and enhances the protein stability of PKC-θ, demonstrating potent anti-inflammatory effects. Anemonin has been shown to alleviate symptoms of dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it a valuable tool for researching inflammation-related diseases. -
iNOS Inhibitor
S-Methylisothiourea sulfate serves as a potent, selective, and competitive inhibitor of inducible nitric oxide synthase (iNOS). This compound has demonstrated significant biological activity in reducing nitric oxide production and exhibits protective effects in rodent models of septic shock. Its role in modulating iNOS activity makes it a valuable reagent for research focused on inflammation and immune response mechanisms. -
CB1R/iNOS Antagonist
(Rac)-Zevaquenabant is a potent cannabinoid receptor type 1 (CB1R) and iNOS antagonist, exhibiting a Ki value of 5.7 nM for CB1R. This compound is primarily utilized in studies related to liver fibrosis, providing valuable insights into its pathophysiology and potential therapeutic interventions. Its selective inhibition of CB1R and iNOS pathways makes it a significant tool for investigating cannabinoid signaling and its implications in fibrotic diseases. -
NO Production Inhibitor
N-Phthaloyl-L-glutamic acid is a nitric oxide production inhibitor that effectively reduces lipopolysaccharide (LPS)-induced nitric oxide synthesis in murine spleen cells. This compound serves as a potential anti-inflammatory agent, demonstrating low cytotoxicity in vitro against tumor cells and in BALB/c mice spleen cell cultures. N-Phthaloyl-L-glutamic acid is suitable for research investigating mechanisms of inflammation and associated therapeutic approaches. -
Nitric oxide donor
S-Nitroso-N-acetyl-DL-penicillamine is a nitric oxide donor that serves as a stable inhibitor of platelet aggregation. It releases nitric oxide in biological systems, thereby contributing to vasodilation and modulation of inflammatory responses. This compound is widely utilized in research related to cardiovascular studies and low blood flow conditions, as well as in investigations of nitric oxide's role in cellular signaling and pathophysiology. -
NO Donor
DETA NONOate is a highly effective exogenous nitric oxide (NO) donor. It releases NO slowly and in controlled amounts, providing long-lasting effects. This compound is widely used in research applications to study NO-mediated physiological processes, such as vasodilation, neuronal signaling, and immune responses. DETA NONOate's stable release profile makes it particularly suitable for in vitro and in vivo studies investigating the role of nitric oxide in various biological systems. -
Monocarboxylic Acid Amide
Lipoamide is a monocarboxylic acid amide that serves as a crucial coenzyme in cellular metabolism, facilitating the transfer of acetyl groups and hydrogen during pyruvate decarboxylation. This compound exhibits protective effects against oxidative stress-induced neuronal cell damage. Additionally, lipoamide plays a significant role in promoting mitochondrial biogenesis in adipocytes through the endothelial nitric oxide synthase-cGMP-protein kinase G signaling pathway, making it valuable for research in metabolic disorders and neuroprotection. -
Porphyrin Complex
Ferroheme is the ferrous form of heme that functions primarily as an oxygen carrier through reversible oxygen binding. Its free form is known to induce oxidative stress and ferroptosis by releasing iron ions, which facilitate the generation of reactive oxygen species via Fenton reactions. This mechanism plays a significant role in pathological conditions such as intracerebral hemorrhage and neurodegenerative diseases, making Ferroheme a valuable reagent for research into iron-overload disorders and the mechanisms underlying ferroptosis-related pathologies. -
NO Inhibitor
Carboxy-PTIO potassium is a potent nitric oxide (NO) inhibitor that facilitates the rapid reaction with NO to yield nitrogen dioxide (NO2). This compound exhibits significant biological activity by preventing hypotension and alleviating endotoxic shock, particularly in lipopolysaccharide-stimulated rat models. It serves as a valuable reagent for researchers investigating the role of nitric oxide in various physiological and pathophysiological processes. -
Glycosaminoglycan
Chondroitin sulfate sodium (from shark cartilage) is a glycosaminoglycan that plays a critical role in cartilage structure and function. It exhibits significant anti-inflammatory properties by reducing the production of inflammatory cytokines, inducible nitric oxide synthase (iNOS), and matrix metalloproteinases (MMPs). This compound is commonly investigated in therapeutic research focused on osteoarthritis and other joint disorders, where it supports cartilage health and alleviates symptoms associated with inflammation. -
NO Scavenger
PTIO is a selective nitric oxide (NO) scavenger and redox mediator. It reacts with nitric oxide to produce imino nitroxides and nitrogen dioxide, effectively mitigating the effects of NO in biological systems. PTIO also enhances the oxidation of organic contaminants by permanganate, making it valuable in studies involving redox chemistry and environmental research. Its applications include investigating NO-related signaling pathways and assessing oxidative stress in various biological contexts. -
NOS Uncoupling Inducer
7,8-Dihydro-L-biopterin serves as a nitric oxide synthase (NOS) uncoupling inducer and is capable of crossing the blood-brain barrier. As a reduced, non-conjugated pteridine and the primary metabolite of 4-amino-tetrahydro-L-biopterin, it promotes the conversion of NOS to a superoxide-producing form, elevating oxidative stress levels, particularly in the renal outer medulla, and triggering apoptosis. This compound's sensitivity to superoxide dismutase (SOD) inhibition makes it valuable for research into salt-sensitive hypertension, traumatic brain injury, and neurodegenerative diseases. -
NO Donor
Spermine NONOate is a nitric oxide (NO) donor characterized by its ability to release NO in aqueous solutions. This compound facilitates various biological processes, including vasodilation and signaling pathways associated with cardiovascular health. Spermine NONOate is commonly utilized in research applications focusing on nitric oxide's role in cellular communication and its implications in various physiological and pathological conditions. -
NO Synthase Inhibitor
L-Canavanine sulfate is a selective inhibitor of inducible nitric oxide synthase (iNOS). It demonstrates significant inhibition of nitric oxide production, making it a valuable tool for studying inflammatory pathways and the role of iNOS in various disease models. This compound is utilized in research applications focused on neurodegeneration, cancer, and cardiovascular disease, providing insights into the mechanisms of nitric oxide-mediated signaling. -
iNOS Inhibitor
Asperuloside is an iridoid compound derived from Hedyotis diffusa, primarily known for its role as an inducible nitric oxide synthase (iNOS) inhibitor. This compound exhibits notable anti-inflammatory properties by suppressing the NF-κB and MAPK signaling pathways. Asperuloside is valuable in studying inflammatory processes and developing therapeutic strategies for related diseases. -
Nitrogen Donor
L-Arginine L-glutamate serves as a critical nitrogen donor for the synthesis of nitric oxide, a key signaling molecule in various biological processes. This compound is valuable in studying gastrointestinal hypofunction or dysfunction, including conditions such as functional dyspepsia. Its role in modulating nitric oxide levels makes it significant for research into cardiovascular health and metabolic regulation. -
NO Donor
MAHMA NONOate is a nitric oxide (NO) donor that facilitates the release of NO in biological systems. It demonstrates significant inhibitory effects on platelet aggregation induced by collagen or ADP, making it valuable for research related to cardiovascular physiology and thrombosis. This compound is useful for studying the mechanisms of NO signaling in various biological contexts. -
CaV1.2 Channel Inhibitor
Demethylsuberosin, a coumarin derivative isolated from Angelica gigas Nakai, primarily targets the L-type CaV1.2 channel as an inhibitor. This compound demonstrates significant antihypertensive effects, in addition to possessing antioxidant and anti-inflammatory properties. Notably, Demethylsuberosin offers neuroprotective effects against glutamate-induced cytotoxicity in primary cultured rat cortical cells, making it a valuable reagent for research in cardiovascular and neurological studies. -
Cyanide Antidote
Hydroxocobalamin acetate is a derivative of vitamin B12 that acts as an effective cyanide antidote. It works by binding to nitric oxide and facilitating the detoxification of cyanide and sodium sulfide. Additionally, hydroxocobalamin acetate has been shown to mitigate hypotension. This compound is utilized in research pertaining to vitamin B12 deficiency disorders, including pernicious anemia.

