Nitric Oxide Signaling (NOS)

GW274150 is a potent and highly selective inhibitor of iNOS, reduces experimental renal ischemia/reperfusion injury.

L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor.

Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells.

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.

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.

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).

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.

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.

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.

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.

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.

SDMA (Symmetric dimethylarginine) is an endogenous inhibitor of nitric oxide (NO) synthase activity.

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).

AVE-3085 is a potent endothelial nitric oxide synthase enhancer, used for cardiovascular disease treatment.

L-NIL is a potent and selective inhibitor of inducible NO synthase with IC50s of 3.3 and 92 μM for mouse inducible NO synthase and rat brain constitutive NO synthase, respectively.

7-Nitroindazole, a heterocyclic compound, acts as a selective inhibitor for neuronal nitric oxide synthase showing a 10-fold selectivity for neuronal NOS.