nNOS Inhibitor

L-NMMA (Tilarginine) acetate is a non-selective and competitive inhibitor of nitric oxide synthase. L-NMMA acetate inhibits three subtypes, namely nNOS, eNOS, and iNOS, and reduces NO production. L-NMMA acetate alleviates mechanical allodynia, thermal hyperalgesia, and choroidal fibrosis. L-NMMA acetate is applicable to research related to nociception, bone cancer pain, and myopia.

Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α.

L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with K_is of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively. L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats.

Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC₅₀ values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC₅₀ values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

7-Nitroindazole is a selective and BBB-penetrable inhibitor of nitric oxide synthase (NOS) (IC₅₀ = 0.47 μM in mouse cerebellum). 7-Nitroindazole does not affect blood pressure or endothelium-dependent relaxation while inhibiting nNOS in experimental animals. 7-Nitroindazole has anti-injurious and neuroprotective properties, and can be studied in research for neurological diseases such as Parkinson’s disease.

nNOS-IN-2 trihydrochloride is a blood-brain barrier-permeable nitric oxide synthase (nNOS) inhibitor. nNOS-IN-2 trihydrochloride exhibits Ki values of 1.7 nM and 2.3 nM against human and rat nNOS, respectively, and shows high selectivity for human eNOS and iNOS. nNOS-IN-2 trihydrochloride also effectively reduces PD-L1 expression in human melanoma cells under both basal conditions and IFN-γ exposure. nNOS-IN-2 trihydrochloride can be used for the study of melanoma and related signaling pathways.

HMN-1180 is a selective, competitive neuronal nitric oxide synthase (nNOS) inhibitor with a K_i value of 5.4 μM against rat nNOS. HMN-1180 exerts no significant effect on endothelial nitric oxide synthase (eNOS) or inducible nitric oxide synthase (iNOS). HMN-1180 inhibits nitric oxide production. HMN-1180 can be used for the study of nNOS-related neuronal functional physiology.

NOS-IN-4 (Compound 3) is a neuronal nitric oxide synthase (nNOS) inhibitor with an IC₅₀ of 4.00 μM that inhibits nNOS activity. The combined use of alpha-lipoic acid and NOS-IN-4 has a protective effect against MPTP (HY-W114750)-induced dopamine depletion in the mouse brain. NOS-IN-4 can be used for the research of neurological disease.

2-Thiouracil (Thiouracil) is a selective neuronal nitric oxide synthase (nNOS) inhibitor with a K_i value of 20 μM. 2-Thiouracil antagonizes BH4-induced nNOS dimerization. 2-Thiouracil is also an antithyroid compound and a highly specific melanoma detector. 2-Thiouracil stimulates the growth of pea and corn root segments.

Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC₅₀ of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion.

Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC₅₀ values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC₅₀ values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

3-Bromo-7-nitroindazole is a potent and selective inhibitor of neuronal nitric oxide synthase (nNOS). 3-Bromo-7-nitroindazole affects the intercellular messenger nitric oxide (NO) synthesis throughout the body and brain. 3-Bromo-7-nitroindazole can be used for the researches of metabolic and neurological disease, such as diabetes, stroke and depression.

Aminopicoline (Ascensil) is a potent and non-selective inhibitor of nitric oxide synthase (NOS) isoenzymes (iNOS, nNOS, eNOS). Aminopicoline competes with arginine at the substrate-binding site of nitric oxide synthase, reduces cellular nitric oxide production, inhibits the elevation of plasma nitrate, increases mean arterial pressure at high doses, and also serves as a basis for radiolabeled ligands to localize nitric oxide synthase binding sites. Aminopicoline can be used in the research of diseases associated with septic shock, joint inflammation, intestinal inflammation, and CNS inflammation.

nNOS-IN-1(Compound 14) is an inhibitor for nitric oxide synthases (NOS), that exhibits inhibitory activities against neuroal, inducible and endothelial NOS, with IC₅₀s of 2.5, 5.7 and 13 μM, respectively.

NOS1-IN-1 is a selective and cell-permeable nNOS inhibitor with a K_i of 120 nM. NOS1-IN-1 exhibits 2617-fold and 325-fold selectivity over eNOS (K_i=39 μM) and iNOS (K_i=325 μM) , respectively. NOS1-IN-1 can be used for the research of neurological disease, including cerebral palsy (CP).

TRIM is a potent nitric oxide synthase inhibitor. TRIM inhibits mouse cerebellar nNOS and rat lung iNOS in vitro with IC₅₀ values of 28.2 and 27.0 µM, respectively. Antidepressant- and anxiolytic-like effects.

1,4-PBIT (1,4-PB-ITU) dihydrobromide (compound 46) is a potent nitric oxide synthases (NOS) inhibitor, with K_i values of 7.6 nM, 360 nM, and 16 nM for the inducible (iNOS), endothelial (eNOS), and neuronal (nNOS) isozymes, respectively.

Nitroaspirin (NCX 4016) is an orally active inhibitor of ARG1 and NOS2. Nitroaspirin reduces ARG1 enzymatic activity via the STAT6-mediated signaling pathway, and feedback-inhibits the catalytic activity of NOS2 in a NO-releasing group-dependent manner. Nitroaspirin continuously releases intracellular NO, inducing redox-dependent loss of cell viability. Nitroaspirin also exerts anti-angiogenic effects by causing endothelial barrier dysfunction, and effectively inhibits the proliferation of Cisplatin (HY-17394)-resistant human ovarian cancer cells. Nitroaspirin can be used in research related to colon cancer, breast cancer and Cisplatin-resistant human ovarian cancer.

Camstatin, a functionally active 25-residue fragment of PEP-19's IQ motif, binds calmodulin and inhibits neuronal nitric oxide (NO) synthase.

hnNOS-IN-3 (compound 39) is a selective nNOS inhibitor, with a K_i of 0.32 μM. The nNOS binding of hnNOS-IN-3 is competitive with L-arginine. The selectivity of hnNOS-IN-3 for nNOS versus iNOS (K_i=37 μM) and eNOS (K_i=9.4 μM) is 115-fold and 29-fold, respectively.