Monoamine Oxidase

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

Nrf2-ARE/hMAO-B/QR2 modulator 1, a resveratrol derivative and multi-target-directed ligand (mtdl), activated the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibited hMAO-B and QR2（quinone reductase-2，NQO2) (IC 50 = 8.05 and 0.57 μM), and was able to promote hippocampal neurogenesis and exert neuroprotective and antioxidant effects in an Alzheimer's disease model.

Sembragiline (EVT-302) is a selective MAO-B inhibitor for the study of Alzheimer's disease (AD).

2614W94 is a selective inhibitor of MAO-A with IC50 of 5 nM and Ki of 1.6 nM.

4-Hydroxyderricin, a potent and selective MAO-B inhibitor (IC50: 3.43 μM), is the main active ingredient of Angelica sinensis, which mildly inhibits dopamine β-hydroxylase (DBH) activity and possesses antidepressant activity.

β-Aminopropionitrile (3-Aminopropionitrile) is a selective inhibitor of lysyl oxidase.

Ethaverine hydrochloride is a homologue of papaverine and is used as a vasodilator and antispasmodic.[2]

LOX-IN-3 dihydrochloride, an inhibitor of lysyl oxidase (LOX), inhibits bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM) activities.

Tisolagiline (KDS2010) is a potent, highly selective and reversible MAO-B inhibitor with IC50=8 nM and oral activity for the treatment of Alzheimer's disease and obesity.

PXS-6302 hydrochloride is a potent irreversible lysine oxidase (LOX) inhibitor, inhibiting Bovine LOX, rh LOXL1, rh LOXL2, rh LOXL3, and rh LOXL4 with IC50 of 3.7 μM, 3.4 μM, 0.4 μM, 1.5 μM, and 0.3 μM, respectively. PXS-6302 hydrochloride penetrates easily through the skin and is able to reduce collagen accumulation, significantly improving the appearance of scars.

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.

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.

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.

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

Rosiridin (6'-O-Deacetylrosiridoside C) has cardioprotective activity.

MAO-B-IN-5 is a potent, selective, and orally active MAO-B inhibitor with an IC50 of 0.204 μM, showing potential for research in Parkinson's disease (PD) [1].

CX-157 (KP 157) is a novel monoamine oxidase-A (MAO-A) inhibitor for the study of depression-like neurological disorders and cancer.

Contezolid (MRX-I) is an orally available oxazolidinone antibiotic with bactericidal activity that can be used to study complications of skin tissue infections and tuberculosis caused by drug-resistant Gram-positive bacteria.

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.

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.

Osthenol is a natural product, and is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM).It shows antitumor-promoting activity, it also has antifungal and antibacterial activities.

Tetrindole mesylate is a MAO-A inhibitor.

Aminoacetone hydrochloride (1-Aminoacetone Hydrochloride) is an oxidant for ferritin and isolated mitochondria, inducing the loss of ferritin iron ring enzyme and iron uptake activity.

MAO-IN-M30 dihydrochloride is a highly potent non-selective inhibitor of MAO-A and MAO-B (IC50 < 0.1 μM). MAO-IN-M30 dihydrochloride is orally active and can cross the blood-brain barrier. It is an effective iron chelator and free radical scavenger. MAO-IN-M30 dihydrochloride has neuroprotective activity in in vitro and in vivo models of Parkinson's disease (PD). It increases brain dopamine, serotonin and norepinephrine and can serve as a lead drug for the development of multifunctional drugs to treat various neurodegenerative diseases.