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NOS Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S5577 6-Biopterin 6-Biopterin ( L-Biopterin, L-Erythro-Biopterin) is a natural product that has been considered as a growth factor for some insects.
E5776 Asymmetric dimethylarginine Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS). It also functions as a marker of endothelial dysfunction in several pathological states.
S9029 Prim-o-glucosylcimifugin Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. It shows potential anticancer activity. Prim-O-glucosylcimifugin downregulates the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner.
E4037 L-Canavanine sulfate L-Canavanine sulfate is a selective inhibitor of inducible NO synthase. This compound exhibits IC50 values ranging from 5 to 10 mM in arginine-rich media and causes a limited degree of cytotoxicity in HeLa, Hep G2, and SK-HEP-1 cells.
S3589 Bendazol Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. This compound inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.
S3899 Hederagenin Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. This compound inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB.
S3304 Stylopine Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. This compound is a major component of the leaf of Chelidonium majus L.
S5542 7-Nitroindazole 7-Nitroindazole, a heterocyclic compound, acts as a selective inhibitor for neuronal nitric oxide synthase showing a 10-fold selectivity for neuronal NOS.
S5229 Isosorbide dinitrate Isosorbide Dinitrate (ISDN, Sorbide nitrate, Sorbidnitrate, Isordil, Nitrosorbide) is the dinitrate salt form of isosorbide, an organic nitrate with vasodilator activity. Isosorbide Dinitrate is a medication used for heart failure, esophageal spasms, and to treat and prevent chest pain from not enough blood flow to the heart. Isosorbide Dinitrate can converte to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase (atrial natriuretic peptide receptor A).
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. This compound inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. It inhibits expression of COX-2 and iNOS mRNA. This chemical also inhibits Ca2+ influx. It inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Drug Des Devel Ther, 2022, 16:2767-2782
J Ginseng Res, 2022, 46(5):700-709
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3924 Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. This compound, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. It also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. This chemical reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
J Biol Chem, 2024, 300(8):107542
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
J Biol Chem, 2021, S0021-9258(21)00790-0
S2979 CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. This compound activates both the innate and the adaptive immune systems. It signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
Nat Commun, 2025, 16(1):2743
Biomedicine & Pharmacotherapy, 2023, 114638
Biomed Pharmacother, 2023, 162:114638
S9208 Ginsenoside Rb3 Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. This compound (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. It shows the significant activity with an IC50 of 8.2 μM. This chemical also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL).
Chin Med, 2024, 19(1):70
S5640 Ethyl caffeate Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro.
Int J Mol Sci, 2023, 24(12)9997
S6850 NE 52-QQ57 NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. This compound effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with this chemical significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
Exp Hematol Oncol, 2024, 13(1):13
S9502 Madecassic acid Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition.
Drug Des Devel Ther, 2022, 16:3793-3804
S3261 Myrislignan Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. This compound inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). It significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. It also inhibits the NF-κB signalling pathway activation.
Oxid Med Cell Longev, 2023, 2023:7098313
S0924 Pteryxin Pteryxin ((+)-Pteryxin), a dihydropyranocoumarin derivative found in Apiaceae family, is a potent inhibitor of butyrylcholinesterase (BChE) with IC50 of 12.96 μg/ml. This compound inhibits LPS-induced nitric oxide production in mouse peritoneal macrophages with IC50 of 20 µM. It is potential for Alzheimer's disease (AD) treatment.
E4805 Methylene Blue trihydrate Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) acts as an inhibitor of soluble guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS). Methylene blue trihydrate exhibits antimalarial, antidepressant, and anxiolytic activity effects. Methylene Blue trihydrate has potential applications in treating methemoglobinemia, neurodegenerative disorders, and ifosfamide-induced encephalopathy.