mao-b-in-1

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

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 and exhibits inhibitory effects on hAChE, hBChE and hMAO-B with IC50s of 7.31, 0.56 and 26.1 μM, respectively. 1 had a neuroprotective effect and was not significantly cytotoxic.

Dual AChE-MAO B-IN-1 (compound 15) is a safe, metabolically stable neuroprotective agent.Dual AChE-MAO B-IN-1 is a potent, orally active CNS-permeable inhibitor of human AChE (IC50=550 nM) and MAO-B (IC50=8.2 nM), and has low in vitro activity against AChE and MAO-B with IC50 values of 550 nM, 8.2 nM respectively.

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-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC 50 of 0.204 μM. MAO-B-IN-5 has the research potential in Parkinson's disease (PD) [1].

Dynorphin B (1-13) acetate acts as an agonist on opioid κ-receptor.

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.

b-Casomorphin (1-3) Acetate is a tri-peptide with an opioid effect.

rel-5-(4-Chloro-2-fluorophenyl)-2,3-dimethyl-7-[(2R,4S)-tetrahydro-2-(1-methyl-1H-pyrazol-4-yl)-2H-pyran-4-yl]pyrido[3,4-b]pyrazine has an EC50 value of ≤ 0.05 μM and an E.max value of > 250 μM for TREM2.

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].

MAO-B-IN-26 (Compound IC9) serves as both a MAO-B and acetylcholinesterase inhibitor. It safeguards SH?SY5Y cells from Aβ-induced toxicity, including morphological alterations, reactive oxygen species (ROS) production, and membrane damage, while also preventing Aβ-triggered autophagy and apoptosis. As such, MAO-B-IN-26 holds potential as a neuroprotective agent in the context of Alzheimer’s disease [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].

CR-1-31-B, a synthetic rocaglate, acts as a highly potent inhibitor of eIF4A. By disrupting the interaction between eIF4A and RNA, it effectively obstructs the initiation phase of protein synthesis. Specifically, CR-1-31-B interferes with the association between Plasmodium falciparum eIF4A (PfeIF4A) and RNA. Additionally, CR-1-31-B induces apoptosis in neuroblastoma and gallbladder cancer cells [4].

Scillascilloside B-1 is a natural product from Scilla scilloides.

Factor B-IN-1 is a Factor B inhibitor.

Cardenolide B-1 is a natural product of Nerium, Apocynaceae. The catalog number is TN3595 and the CAS number is 1318158-89-2. Cardenolide B-1 can be used as a reference standard.

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

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.

Tenacigenin B, a component of the plant Poria cocos, is identified as 3-O-β-Allopyranosyl-(1→4).

Quercetin-3-O-β-D-galactopyranosyl-(1→6)-β-D-glucopyranoside (compound 1), a flavonoid glycoside, is extractable from M. delavayi leaves [1].

'(Des-Bromo)-Neuropeptide B (1-23) (human)' is an agonist for orphan G-protein-coupled receptors, exhibiting a K i of 1.2 nM for GPR7 (NPBW1) and 341 nM for GPR8 (NPBW2) respectively [1].

Orexin B, human (TFA) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2.

Plipastatin B 1 is a lipopeptide.

Dynorphin B (1-13), a 13 amino acid, is an extraordinarily potent opioid peptide.

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].

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 is effective in reducing excessive AChE and BuChE levels associated with Alzheimer's disease (AD) and holds potential for use in anti-Alzheimer's research [1].

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-20 (Compound C14), a potent MAO-B inhibitor boasting an IC50 of 0.037 μM, demonstrates excellent metabolic stability and brain-blood barrier permeability. It holds 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-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].

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].

MAO-B-IN-15 is a selective inhibitor of MAO-B that forms π-π interaction with Tyr 326 residue (IC 50 = 13.5 μM) which can be used in Parkinson’s disease research[1].

AChE/BChE/MAO-B-IN-3, an indan-1-one derivative, serves as a potent inhibitor of human monoamine oxidase B (MAO-B) with an IC50 of 0.0359 μM, demonstrating 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, serves as a potent inhibitor for both monoamine oxidase B (MAO-B) and acetylcholinesterase/butyrylcholinesterase (AChE/BChE) enzymes. It exhibits a strong inhibitory effect on human MAO-B with an IC50 of 0.0393 μM, and demonstrates significant potency against human AChE and BChE enzymes with IC50 values of 0.0458 μM and 0.075 μM, respectively. Additionally, this compound displays notable antioxidant properties and the ability to prevent β-amyloid plaque aggregation, marking its potential utility in Alzheimer's disease (AD) research.

MAO-B-IN-16 is a selective inhibitor of monoamine oxidase B (MAO-B ) (IC 50 = 1.55 μM) that can be used in the central nervous disorders study, for example, parkinson's disease [1].

MAO-B-IN-3 is a reversible, selective inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 96 nM and demonstrates 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) represents a powerful MAO-B inhibitor, boasting an IC50 value of 0.014 μM, and exhibits high antioxidant activity alongside effective metal-chelating properties. It also demonstrates adequate BBB permeability and notable neuroprotective effects [1].

MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor (IC50 = 10 nM). MAO-B-IN-13 shows neuroprotective and antioxidant activity which can be used in 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-10 (compound 4f) is a highly potent and selective inhibitor of MAO-B (monoamine oxidase-B). It effectively penetrates the blood-brain barrier and exhibits an IC50 of 5.3 μM. This compound demonstrates the ability to inhibit self-mediated Aβ (amyloid β) aggregation by 58.2% and disaggregate it by 43.3%. Thus, MAO-B-IN-10 holds promise for Alzheimer's disease research [1].

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

MAO-B-IN-8 is a highly potent and reversible inhibitor of monoamine oxidase-B (MAO-B), which also exhibits inhibitory effects on the microglial production of neuroinflammatory mediators. This compound is specifically designed for use in research related to neurodegenerative diseases [1].

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

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

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

hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor with IC50s of 2.5 μΜ for hMAO-B and 3.84 μΜ for MB-COMT. hMAO-B/MB-COMT-IN-1 protects cells from oxidative damage that can be used in neurodegeneration disease research, for example, Parkinson’s Disease (PD) [1].

MAO-B-IN-12 (Compound 16c) is a highly effective inhibitor of monoamine oxidase B (MAO-B), displaying significant potency with an IC50 value of 1.3 μM. Additionally, MAO-B-IN-12 exhibits notable neuroprotective activity [1].

Nucleoside Derivatives - Xylo-nucleosides; 8-Modified purine nucleosides; Amino nucleosides; N-Methylated alkylated nucleosides

(S)-Rasagiline mesylate is rasagiline S-isomer, and is an agent of anti-Parkinson.

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

(S)-Rasagiline is rasagiline S-isomer, and is an agent of anti-Parkinson.

Racemic rasagiline, also known as AGN-1135, is a Monoamine Oxidase type-B inhibitor (MAOI). However, application of this drug can lead to fatal hypertensive crisis in patients who consume tyramine-rich foods. TVP-1022 is the (S)-isomer os Rasagiline and acts as a cardioprotective agent.

Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline, which is an irreversible monoamine oxidase inhibitor.

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