mao in 1

MAO-IN-1 is a potent monoamine oxidase B (MAO B) inhibitor (IC50: 20 nM) for the study of neurologically related diseases.

AChE/MAO-IN-1 is a potent inhibitor of human acetylcholinesterase (AChE), monoamine oxidase A (MAO-A), and monoamine oxidase B (MAO-B), demonstrating inhibitory concentrations (IC50) of 0.0248 μM, 0.0409 μM, and 0.1108 μM against AChE, MAO-A, and MAO-B, respectively.

MAO-B-IN-1 is a monoamine oxidase B inhibitor and can be used for the research of neurological diseases.

MAO-A/SERT-IN-1 acts as an inhibitor for both MAO-A and the serotonin transporter (SERT). It decreases the SERT-mediated reuptake of 5-HT and demonstrates neuroprotective properties in cellular inhibition models. Additionally, this compound has shown to alleviate depressive behaviors in both zebrafish and mice.

BChE/MAO-B-IN-1 is a dual inhibitor of BChE and MAO-B, with IC50 values of 375 nM and 20 nM, respectively. It effectively counteracts oxidative damage induced by H2O2 and 6-OHDA in SH-SY5Y cells and can penetrate the central nervous system in cell models simulating the blood-brain barrier. BChE/MAO-B-IN-1 is applicable for research into neurological disorders such as Alzheimer's disease (AD).

AChE/BChE/MAO-A-IN-1 (Compound 5c) is a multi-target inhibitor with IC₅₀ values of 78.7 μM for AChE, 22.63 μM for BChE, and 0.84 μM for MAO-A. This compound is useful in Alzheimer's disease research.

AChE/BChE/MAO-B-IN-1 is a reversible, non-time-dependent inhibitor of AChE, BChE, and MAO-B that crosses the blood-brain barrier, exhibiting inhibitory effects on hAChE, hBChE, and hMAO-B with IC50s of 7.31, 0.56, and 26.1 μM, respectively. [AChE/BChE/MAO-B-IN-1] had a neuroprotective effect and was not significantly cytotoxic.

HDAC1/MAO-B-IN-1 has the potential to be used in the Alzheimer's disease research. HDAC1/MAO-B-IN-1 is a potent and selective inhibitor of HDAC1/MAO-B that can cross the blood-brain barrier. The IC50 values of HDAC1/MAO-B-IN-1 for HDAC1 and MAO-B are 21.4 nM and 99.0 nM, respectively [1].

MAO A/HDAC-IN-1 is an effective dual inhibitor of monoamine oxidase A (MAO A) and HDAC, suitable for glioma research.

Dual AChE-MAO B-IN-1 (compound 15) is a safe, metabolically stable neuroprotective agent. This potent, orally active, CNS-permeable inhibitor demonstrates IC50 values of 550 nM for human AChE and 8.2 nM for MAO-B, indicating low in vitro activity against these enzymes.

MAO A/HSP90-IN-1 (4-b) is a dual inhibitor of MAO A and HSP90, with IC50 values of 1.77 μM in glioblastoma (GBM) GL26 cells and 0.019 μM against HSP90α. This compound impairs MAO A activity, disrupts HSP90 binding, and downregulates HER2 and phospho-Akt expressions, thus inhibiting GBM growth. Additionally, it reduces PD-L1 expression, 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].

5-HT6R/MAO-B modulator 1 is an antagonist of 5-HT6R (at Gs signaling) and an irreversible inhibitor of MAO-B that exhibits glial protective activity and induces scopolamine-induced memory deficits.

MAO-B ligand-1 is a selective MAO-B inhibitor.

MAO-A Inhibitor 1 (compound VIII) acts as a MAO-A inhibitor and exhibits an IC50 value of 100 μM [1].

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].

MAO-B-IN-8 is a highly potent and reversible inhibitor of monoamine oxidase-B (MAO-B), also inhibiting microglial production of neuroinflammatory mediators. This compound is specifically designed for research on neurodegenerative diseases [1].

LSD1-IN-40 (Compound 9e) is a potent LSD1 inhibitor with an IC50 value of 9.85 nM. It exhibits greater selectivity for LSD1 over MAO and hERG. LSD1-IN-40 shows significant inhibitory activity against leukemia cells (MV-4-11, HL-60, and THP-1 cells) and can induce apoptosis in MV-4-11 cells. This compound holds potential for research in acute myeloid leukemia.

ChEs/MAOs-IN-1 (Compound 4i) is a dual inhibitor of cholinesterases (ChEs) and monoamine oxidases (MAOs). The IC50 values for ChEs/MAOs-IN-1 are 0.048 μM for AChE, 0.89 μM for BChE, 3.58 μM for MAO-A, and 0.095 μM for MAO-B. This compound can be utilized in studies related to neurodegenerative diseases.

MAO-B-IN-45 is a dual inhibitor of ferroptosis and MAO-B. It selectively inhibits MAO-B with an IC50 of 87.47 nM, demonstrating a selectivity over MAO-A by more than 229 times. In vitro, MAO-B-IN-45 exhibits significant anti-ferroptosis activity by modulating iron metabolism pathways and the GSH-GPX4 axis. Additionally, it improves cognitive and behavioral deficits in 3×Tg (APP/Tau/Ps1) Alzheimer's disease mice and significantly reduces levels of ferritin heavy chain 1 (FTH1), β-amyloid protein (APP), and Tau protein phosphorylation (p-Tau) in their brains.

MAO-B-IN-49 is a selective, reversible MAO-B inhibitor with an IC50 of 1 nM for human MAO-B. It demonstrates significantly higher selectivity for MAO-B over MAO-A (IC50 = 633.9 nM). MAO-B-IN-49 reduces lipopolysaccharide (LPS)-induced ROS production in HT22 cells. It possesses notable neuroprotective properties and significantly improves motor dysfunction in MPTP-induced Parkinson's disease (PD) mouse models. MAO-B-IN-49 is applicable for Parkinson's disease research.

MAO-B-IN-50 (Compound C20) is a selective MAO-B inhibitor with an IC50 value of 0.06 μM. It effectively inhibits the aggregation of Aβ40/42 and Tau proteins, with an overall IC50 of approximately 1 μM. Additionally, MAO-B-IN-50 exhibits potent and selective AChE inhibitory activity (IC50 = 1.78 μM). This compound is useful in Alzheimer's disease research.

ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation a

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)

Erythromycin 2'-propionate is a macrolide antibiotic and an esterified form of erythromycin .1It is active againstS. aureuswhen used at a concentration of 1 μg/ml. Erythromycin 2'-propionate (1 mM) inhibits protein synthesis in a cell-free assay. 1.Tardrew, P.L., Mao, J.C.H., and Kenney, D.Antibacterial activity of 2'-esters of erythromycinAppl. Microbiol.18(2)159-165(1969)