mao-b inhibitor 58

MAO-B inhibitor 58 is an effective, selective, and reversible inhibitor of monoamine oxidase B.

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.

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-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.

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

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.

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

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].

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.

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.

MAO-B-IN-20 (Compound C14), a potent MAO-B inhibitor with an IC50 of 0.037 μM, demonstrates excellent metabolic stability and brain-blood barrier permeability, holding potential for Parkinson's disease research [1].

MAO-B-IN-11, also known as Compound 8c, is a highly potent inhibitor of monoamine oxidase B (MAO-B), with an IC50 value of 1.3 μM. Additionally, MAO-B-IN-11 exhibits neuroprotective properties [1].

MAO-B-IN-13 (compound 12a) is a highly potent, reversible, and blood-brain barrier (BBB) penetrant MAO-B inhibitor (IC50 = 10 nM) that exhibits neuroprotective and antioxidant activity, making it suitable for Parkinson’s disease research [1].

MAO-B-IN-23, also known as Compound 11f, is a reversible and competitive monoamine oxidase B (MAO-B) inhibitor with an IC50 value of 1.44 μM and a Ki of 0.51 μM [1].

MAO-B-IN-30 is a selective and potent MAO-B inhibitor that crosses the blood-brain barrier with antiproliferative activity and inhibits both MAO-A and MAO-B.MAO-B-IN-30 reduces the levels of TNF-alpha, IL-6, and NF-kB in organisms, and can be used to study Parkinson's-type neurological disorders.

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-IN-10 (compound 4f) is a highly potent and selective MAO-B (monoamine oxidase-B) inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 of 5.3 μM. It demonstrates the ability to inhibit self-mediated Aβ (amyloid β) aggregation by 58.2% and disaggregate it by 43.3%, holding promise for Alzheimer's disease research [1].

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.

AChE/MAO-B-IN-3 is a dual inhibitor targeting both acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B), exhibiting inhibitory concentrations (IC50s) of 0.0257 μM and 0.0456 μM against human AChE and MAO-B, respectively. This compound holds potential for Alzheimer’s disease research.

Bcl-B inhibitor 1 is an antitumor compound that binds to and inactivates pro-apoptotic proteins in the BH3 structural domain.

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].

Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active, and selective monoamine oxidase B (MAO-B) inhibitor (IC50 = 0.02 nM) capable of crossing the blood-brain barrier (BBB). It exhibits antioxidant and anti-neuroinflammatory activities and can be used in the study of Parkinson's disease[1].

Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor (Ki <0.010 µM) with potential anticancer activity for cancer research.

MAO-B-IN-3 is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 96 nM and shows affinity for the 5-HT6 receptor with a Ki of 696 nM, making it suitable for Alzheimer's disease research [1].

MAO-B-IN-4 (Compound 26) is a reversible monoamine oxidase B (MAO-B) inhibitor with potent in vitro activity, characterized by an IC50 value of 9 nM. This orally active compound exhibits favorable metabolic stability, a satisfactory safety profile, and effective brain permeability. Demonstrating antidepressant effects in rodent models, MAO-B-IN-4 is suitable for research into Alzheimer's disease [1].

MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor with an IC50 value of 0.014 μM, exhibiting significant antioxidant activity, effective metal-chelating properties, adequate BBB permeability, and notable neuroprotective effects [1].

HIV-1 Inhibitor-58 (Compound 10c) is a non-nucleoside reverse transcriptase inhibitor with broad-spectrum antiviral properties, effective against both wild-type strain IIIB and NNRTI-resistant strains like K103N and E138K in MT-4 cells at an EC50 of less than 50 nM. Additionally, it inhibits CYP2C9 and CYP2C19 with IC50 values of 2.06 μM and 1.91 μM, respectively. This compound is utilized in HIV infection research [1].

MAO-B-IN-14 (Compound 9) is a potent and selective monoamine oxidase-B (MAO-B) inhibitor, exhibiting an IC50 of 0.95 μM and a Ki of 0.55 μM for human MAO-B.

MAO-B-IN-29 (compound 9a) acts as an inhibitor of MAO-B activity [1].

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].

Monoamine OxidaseB inhibitor 5 (Compound 16d) is a reversible and selective inhibitor of monoamine oxidase B (hMAO-B), with an IC50 value of 67.3 nM and a Ki of 82.5 nM. It exhibits favorable pharmacokinetic properties and low toxicity in rat models. Additionally, this compound alleviates motor impairments in a Parkinson’s mouse model induced by MPTP, and it is characterized by its ability to penetrate the blood-brain barrier (BBB).

KRAS G12C inhibitor 58 is utilized in cancer research as an inhibitor of the KRAS G12C mutation [1].

Dual AChE-MAO B-IN-3 (Compound C10) is a potent inhibitor of both AChE and MAO-B, with IC50 values of 0.58 μM and 0.41 μM, respectively. It targets the catalytic anionic site and peripheral anionic site of AChE, making it relevant for Alzheimer’s disease (AD) research [1].

MAO-B-IN-21 is an MAO-B inhibitor characterized by superior antioxidant and anti-Aβ aggregation activities, metal-ion chelating capabilities, and mitigation of neuroinflammation (NO, TNF-α). It demonstrates neuroprotective effects with notable BBB permeability and, in an Aβ1-42 induced Alzheimer's disease mouse model, significantly enhances memory and cognitive functions [1].

MAO-B-IN-6 is a selective, potent, orally active MAO-B inhibitor (IC50: 0.019 μM) and demonstrates superior efficacy to Safinamide both in vitro and in vivo.

MAO-B-IN-12 (Compound 16c) is a potent monoamine oxidase B (MAO-B) inhibitor with an IC50 value of 1.3 μM and significant neuroprotective activity [1].

MAO-B-IN-7 is a potent and blood-brain barrier permeable MAO-B and AChE inhibitor, exhibiting IC50 values of 41 nM for human AChE, 87 nM for electric eel AChE, and 0.3 μM for MAO-B. MAO-B-IN-7 effectively alleviates oxidative stress and neuroinflammatory damage.

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

MAO-A B-IN-3 (Compound 12) demonstrated moderate permeability in in vitro experiments, with rates recorded at 16.49 nm s in Caco2 cells and 103.16 nm s in MDCK cells. The compound exhibited a high plasma protein binding rate of 90.97%, indicative of strong binding, suggesting it has an extended half-life and slow excretion characteristics.

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].

MAO-B-IN-18 is a potent, selective inhibitor of MAO B with 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].

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

MAO-B-IN-15 is a selective MAO-B inhibitor (IC50 = 13.5 μM) that forms π-π interactions with the Tyr 326 residue, and it can be utilized in Parkinson’s disease research[1].

AChE BChE MAO-B-IN-3, an indan-1-one derivative, is a potent inhibitor of human monoamine oxidase B (MAO-B) with an IC50 of 0.0359 μM and also demonstrates significant inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 0.0473 μM and 0.0782 μM, respectively. Exhibiting notable antioxidant activity, AChE BChE MAO-B-IN-3 holds considerable promise for Alzheimer's disease (AD) research.

AChE BChE MAO-B-IN-4, an indan-1-one derivative, is a potent inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase butyrylcholinesterase (AChE BChE). It strongly inhibits human MAO-B with an IC50 of 0.0393 μM and is highly effective against human AChE and BChE with IC50 values of 0.0458 μM and 0.075 μM, respectively. Additionally, this compound exhibits significant antioxidant properties and ability to prevent β-amyloid plaque aggregation, suggesting its potential in Alzheimer's disease (AD) research.

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].