mao-a inhibitor 2

MAO-A inhibitor2 (compound HT4) is a monoamine oxidase A (MAO-A) inhibitor with an IC50 of 14.3 µM. It exhibits minimal impact on MAO-B (IC50 of 106 µM) and is almost ineffective against xanthine oxidase (XO). MAO-A inhibitor2 is applicable in research on neurodegenerative diseases and oxidative stress.

Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl), a Monoamine Oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression.

MAO-B-IN-2 is a selective and competitive inhibitor of MAO-B and BChE with IC50 values of 0.51 μM and 7.00 μM, respectively. It attenuates H2O2-induced cellular damage due to its strong ROS scavenging properties.

Rasagiline (AGN1135) is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinsons disease.

CR4056 (6-(1H-imidazol-1-yl)-2-phenylquinazoline) is a selective inhibitor of MAO-A with IC50 of 202.7 nM and a ligand of I2-imidazoline receptor with IC50 of 596 nM.

(-)-2-Phenylpropylamine ((S)-2-Phenylpropylamine) (compound 3b) functions as an inhibitor for both MAO-A and MAO-B, with Ki values of 584 μM and 156 μM, respectively.

2-Methoxyhydroquinone inhibits MAO-A and MAO-B and reduces TNF-α-induced CCL2 production, often serving as a precursor for synthesising the Hsp90 inhibitor Geldanamycin.

7-Hydroxy-4-phenylcoumarin is a dual inhibitor of ALDH-2 and MAO, with IC50 values of 1.5 µM and 0.5 µM, respectively.

Multitarget AD inhibitor-2 (Compound VN-19) is a versatile inhibitor targeting multiple sites, acting on acetylcholinesterase (AChE, IC50 = 0.14 μM), butyrylcholinesterase (BChE, IC50 = 11.6 μM), and monoamine oxidase B (MAO B, IC50 = 0.45 μM). It inhibits amyloid-beta protein Aβ1-42 self-induced aggregation with an inhibition rate of 47.3% at 20 μM and reduces ROS levels in SH-SY5Y cells with an inhibition rate of 80% at 25 μM. Multitarget AD inhibitor-2 can also improve cognitive decline in a scopolamine-induced Alzheimer's zebrafish model.

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

Rasagiline-13C3is intended for use as an internal standard for the quantification of rasagiline by GC- or LC-MS. Rasagiline is an inhibitor of monoamine oxidase B (MAO-B; IC50= 4.43 nM for the rat brain enzyme).1It is selective for MAO-B over MAO-A (IC50= 412 nM for the rat brain enzyme). It inhibits serum and NGF withdrawal-induced apoptosis of PC12 cells when used at concentrations ranging from 0.01 to 100 μM.2Rasagiline inhibits rat brain MAO-Bin vivo(ED50= 0.1 mg/kg).1It reduces cerebral edema in a mouse model of traumatic brain injury.2Rasagiline (0.1 mg/kg) reduces cortical and hippocampal levels of full-length and soluble amyloid precursor protein (APP) in rats and mice. It also reduces α-synuclein-induced substantia nigral neuron loss and improves motor dysfunction in a mouse model of Parkinson's disease.3Formulations containing rasagiline have been used in the treatment of Parkinson's disease. 1.Youdim, M.B.H., Gross, A., and Finberg, J.P.Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase BBrit. J. Pharmacol.132(2)500-506(2001) 2.Youdim, M.B.H., and Weinstock, M.Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R) aminoindan-5-YL)-ethyl methyl carbamate]Cell. Mol. Neurobiol.21(6)555-573(2001) 3.Kang, S.S., Ahn, E.H., Zhang, Z., et al.α-Synuclein stimulation of monoamine oxidase-B and legumain protease mediates the pathology of Parkinson's diseaseEMBO J.37(12)e98878(2018)

Selective tryptophan 2, 3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. Reduces growth of TDO-expressing P

Lazabemide hydrochloride (N-(2-Aminoethyl)-5-chlor-2-pyridincarbox) is a reversible and selective mao-b inhibitor(Ki:7.9nM).

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

LSD1-IN-12 (compound 2) is an effective inhibitor of LSD1, with inhibitory Ki values of 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), and 3.5 μM (MAO-B) [1].

SSAO inhibitor-2 (Compound 1) is an inhibitor of semicarbazide-sensitive amine oxidase (SSAO) with IC50 values <10 nM for human SSAO and 10-100 μM for MAO-A, respectively [1]. It can be used in the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, and multiple sclerosis.

hMAO-B/MB-COMT-IN-2 is a dual inhibitor of MAO-B/MB-COMT with IC50s of 4.27 μM and 2.69 μM for hMAO-B and MB-COMT, respectively. hMAO-B/MB-COMT-IN-2 protects cells from oxidative damage and can be used in neurodegeneration disease research, such as Parkinson's Disease (PD) [1].

Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active, and selective inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 1.33 nM, capable of crossing the blood-brain barrier (BBB). It exhibits antioxidant and anti-neuroinflammatory activities and is useful in the study of Parkinson's disease [1].

Dual AChE-MAO B-IN-2 is a potent dual inhibitor of AChE (IC50: 0.12 μM) and MAO B (IC50: 0.01 μM) with potential for Alzheimer's disease studies.

AChE/BChE/MAO-B-IN-2 is a potent inhibitor of the enzymes AChE, BChE, and MAO-B, with IC50 values of 48.2 nM, 83.9 nM, and 31.2 nM, respectively. It also exhibits significant antioxidant activity and is applicable in Parkinson's disease research.

2-PAT, analogous to Rasagiline and Selegiline, functions as a reversible MAO-A inhibitor, exhibiting an IC50 of 0.721 µM, and acts as an inactivator of MAO-B with an IC50 value of 14.6 µM. This compound shows promise for research in Parkinson's disease and depression.

Methylene Blue (Basic Blue 9) hydrate functions as an inhibitor of guanylyl cyclase (sGC), monoamine oxidase A (MAO-A), and NO synthase (NOS). This compound, known for its vasopressor activity, is widely utilized as a dye in various medical procedures. It operates via the nitric oxide synthase/guanylate cyclase signaling pathway to diminish prepulse inhibition and possesses the capacity to cross the blood-brain barrier. Methylene Blue hydrate acts as a REDOX cycling compound and inhibits Tau protein aggregation. Moreover, it is effective in reducing cerebral edema, damping microglial activation, and alleviating neuroinflammation, demonstrating its multifaceted therapeutic potential [1] [2] [3].

AChE/BuChE/MAO-B-IN-2 (compound 4b) is a potent inhibitor of AChE, BuChE, and hu MAO-B, with respective IC50 values of 5.3 μM, 12.4 μM, and 1.9±0.08 μM, indicating good in vitro blood-brain barrier (BBB) permeability. It effectively reduces excessive AChE and BuChE levels associated with Alzheimer's disease (AD) and holds potential for anti-Alzheimer's research [1].

MAO A/HSP90-IN-2 (compound 4-C), a dual inhibitor of HSP90 and MAO A, exhibits IC50 values of 0.016 μM for MAO A and 4.58 μM for HSP90. This compound enhances HSP70 expression, diminishes HER2 and phospho-Akt levels, downregulates IFN-γ-induced PD-L1 expression in GL26 cells, and demonstrates efficacy against Temozolomide-sensitive and -resistant GBM cells, colon cancer, leukemia, and non-small cell lung cancer, possibly impeding tumor immune evasion [1].