Monoamine Oxidase

Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.

Paeonol (Peonol) is an active extraction from Paeonia suffruticosa. Paeonol inhibits MAO-A and MAO-B with IC50 of 54.6 μM and 42.5 μM, respectively.

MAO-B-IN-9 is a monoamine oxidase B MAO-B inhibitor (IC50: 0.18 μM) that crosses the blood-brain barrier with potency, selectivity and time-dependence. MAO-B-IN-9 has neuroprotective effects against Aβ1-42-induced neuronal cell death, which may be related to the anti-aggregation effect of Aβ1-42.

hMAO-B-IN-5 is a potent reversible and selective human monoamine oxidase hMAO-B inhibitor (IC50:0.12μM). hMAO-B-IN-5 can cross the blood-brain barrier and can be used in the study of Parkinson's disease. It is a promising compound in the treatment and diagnosis of central nervous system diseases.

PXS-5153A is an effective, selective, and fast-acting inhibitor of lysyl oxidase like 2/3 enzymes with enzymatic activity almost entirely blocked within 15 minutes. PXS-5153A could reduce crosslinks and ameliorates fibrosis.

CCT365623 is an orally bioavailable Lysyl Oxidase inhibitor with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy.

Lenumlostat is an orally available, selective and potent lysyl oxidase-like protein 2 (LOXL2) inhibitor with inhibitory effects on hLOXL2, hLOXL3 and LOXL2 for the study of fibrotic diseases.

PAT-1251 is an inhibitor of LOXL2 with IC50s of 10, 0.12, and 0.16 μM for the mouse, rat, and dog and can be used in studies about fibrotic diseases.

Medifoxamine (LG 152) is a selective non-monoamine oxidase inhibitor that exhibits antidepressant activity through inhibition of 5 HT reuptake.Medifoxamine preferentially inhibits dopamine reuptake.

Rosmarinic acid (Labiatenic acid) is widely found in plants and has antioxidant, anti-inflammatory, and antibacterial activities. It inhibits MAO-A, MAO-B, and COMT with IC50 of 50.1, 184.6, and 26.7 μM respectively.

Methylene Blue (Tetramethylthionine chloride) (IC50 of 1.9 μM) inhibits tau filament formation. And it inhibits soluble guanylyl cyclase. It is also used as a dye in chromoendoscopy.

J-147 is an experimental drug with reported effects against both Alzheimer's disease and ageing in mouse models of accelerated aging. It is a curcumin derivative and a potent neurogenic and neuroprotective drug candidate initially developed for the treatment of neurodegenerative conditions associated with aging that impacts many pathways implicated in the pathogenesis of diabetic neuropathy.

Nialamide (Nialamid) is an MAO inhibitor that is used as an antidepressive agent.

Pargyline (Pargylamine) is a monoamine oxidase inhibitor with antihypertensive properties.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

MAO-B-IN-19, a selective MAO-B inhibitor, exhibits neuroprotective and anti-inflammatory properties and demonstrates an IC50 value of 0.67 μM [1].

Eprobemide (LIS 630) is a non-competitive reversible inhibitor of monoamine oxidase A (MAO-A).

7-Hydroxy-3,4-dihydro-2(1H)-quinolinone is a weak MAO-A inhibitor(with an IC50 of 183 μM) .

Tranylcypromine (SKF 385), a potent monoamine oxidase (MAO) inhibitor [1], is used in medicinal applications.

Azure B (Azure B chloride) is a cationic dye and the major metabolite of Methylene blue. Azure B is a selective, and reversible inhibitor of MAO-A (IC50s: 11 and 968 nM for recombinant human MAO-A and MAO-B).

Bifemelane hydrochloride is a MAO inhibitor

MAO-B-IN-27 (Compound 12c), a monoamine oxidase B (MAO-B) inhibitor, exhibits a potent and selective inhibitory effect on hMAO-B, with an IC50 value of 8.9 nM, and is utilized in Parkinson's disease (PD) research [1].

(±)-Amiflamine (2-dimethylphenethylamine) is an inhibitor of reversible MAO-A.

Simtuzumab is a monoclonal antibody against lysyl oxidase-like protein 2 (LOXL2). Simtuzumab can be used to treat primary sclerosing cholangitis (PSC) and is not effective in patients with bridging fibrosis or compensatory cirrhosis caused by non-alcoholic steatohepatitis.

Iproniazid Phosphate is a non-selective, irreversible monoamine oxidase inhibitor (MAOI).

Tisolagiline (KDS2010), a reversible MAO-B inhibitor, is utilized in Parkinson's disease research [1].

MAO-IN-3 (Compound 5), a reversible and competitive monoamine oxidase (MAO) inhibitor with inhibition constants (K i) of 0.6 μM for MAO A and 0.2 μM for MAO B, effectively suppresses LN-229 glioblastoma cell proliferation, as denoted by an inhibitory concentration (IC50) of 0.8 μM. This compound holds potential application in cancer research [1].

MAO-B-IN-24 (compound 11h) is a selective, reversible, competitive inhibitor of MAO-B with an IC50 value of 1.60 μM. It also exhibits inhibitory effects on MAO-A with an IC50 of 22.42 μM. At a concentration of 10 μM, MAO-B-IN-24 reduces the activities of AChE and BChE to 54.58% and 88.43%, respectively [1].

ETAP, a dual inhibitor of both monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B), exhibits antidepressant-like effects and is utilized in the research of major depressive disorder [1].

Pargyline hydrochloride (Pargylamine hydrochloride) is an irreversible monoamine oxidase(MAO) inhibitor with antihypertensive properties.

BI-1467335 HCl(BI 1467335) is a selective, orally active inhibitor of semicarbazide-sensitive amine oxidase (SSAO) that helps improve chronic obstructive pulmonary disease in mice[2].

Norharmane (β-Carboline) is a natural β-carboline first isolated from plants of the Zygophyllaceae family.

Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.

Toloxatone (MD 69276) is a reversible monoamine oxidase A (MAOA) inhibitor.

Isatin (2,3-Indolinedione) is an endogenous MAO inhibitor.

MAO-B-IN-25 (compound 92) is a selective inhibitor of monoamine oxidase B (MAO-B), exhibiting inhibitory half-maximal inhibitory concentrations (IC50) of 240 nM for MAO-B and 0.5 nM for MAO-A [1].

Lysyl Hydroxylase 2-IN-1 (compound 12) is a selective inhibitor of lysyl hydroxylase 2 (LH2) with an IC50 of approximately 300 nM and demonstrates specificity for LH2 over LH1 and LH3 [1].

MAOA-IN-1 (compound 15) is an orally-active inhibitor of monoamine oxidase A (MAOA) that exhibits cytotoxic effects on prostate cancer cells. This compound demonstrates Caco-2 permeability while maintaining reduced central nervous system (CNS) permeability, indicating its potential utility in anti-cancer and anti-inflammatory research [1].

MAO-B-IN-18 is a potent, selective inhibitor of MAO B, demonstrating IC50 values of 52 nM for hMAO B and 14 μM for hMAO A. It exhibits cytoprotective effects against hydrogen peroxide-induced damage in neuroblastoma and astrocyte cultures [1].

TB5 is a potent, selective and reversible inhibitor of hMAO-B.

1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS/D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK/NFκB and Jak2/STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydromethysticin and Desmethoxy yangonin involves transcription activation, probably through a PXR-independent or PXR-involved indirect mechanism.

PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.

Isocarboxazid has the formula 1-benzyl-2-(5-methyl-3-isoxazolylcarbonyl)hydrazine-isocarboxazid. It is a monoamine oxidase inhibitor.[2] It is used in the treatment of major depression, dysthymic disorder, atypical disorder, panic disorder and the phobic

Clorgyline hydrochloride (Clorgiline hydrochloride), a white powder, is served as monoamine oxidase inhibitor.

Phenelzine sulfate is a non-selective and irreversible inhibitor of monoamine oxidase (MAOI), and with antidepressant and anxiolytic.

Rasagiline Mesylate (AGN1135) is a novel MAO-B inhibitor, which can treat idiopathic Parkinson's disease.

Lysyl Hydroxylase 2-IN-2 (compound 13) is a potent inhibitor of Lysyl Hydroxylase 2 (LH2), exhibiting an IC50 of approximately 500 nM. It effectively inhibits cell migration in 344SQ WT cells without affecting the migration of LH2 knockout cells [1].

MAO A/HSP90-IN-1 (4-b) is a dual inhibitor of MAO A and HSP90, exhibiting IC50 values of 1.77 μM in glioblastoma (GBM) GL26 cells and 0.019 μM against HSP90α. This compound impairs the activities of MAO A, disrupts HSP90 binding, and downregulates both HER2 and phospho-Akt expressions, thereby inhibiting GBM growth. Additionally, it diminishes PD-L1 expression, thereby thwarting T cell activation and potential tumor immune evasion. MAO A/HSP90-IN-1 (4-b) is valuable for research into brain tumor-related diseases [1].

Minaprine is a reversible inhibitor of MAO-A, used in the treatment of various depressive states.

MAO-IN-M30 dihydrochloride (M 30 dihydrochloride) is a potent and brain selective monoamine oxidase (MAO) inhibitor (EC50 values are 37 and 57 nM for MAO-A and MAO-B, respectively). Also an iron chelator with antioxidant properties. Protects cells against 6-OHDA induced apoptosis. Attenuates MPTP depletion of DA and increases striatal monoamine levels in a mouse Parkinson's disease model.