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

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.

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

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 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].

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

Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1), exhibiting a reversible mode of action and oral bioavailability. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses LSD1 enzymatic activity while demonstrating minimal inhibition of LSD2, MOA-A, and MAO-B enzymes. Additionally, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.

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-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].

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].

Tisolagiline (KDS2010), a reversible MAO-B inhibitor, is utilized in Parkinson's disease research [1].

1-Methyl-2-undecyl-4(1H)-quinolone, along with dihydroevocarpine and evodiamine, should serve as chemical markers for the quality control of Evodia rutaecarpa (Juss.) Benth. This compound selectively inhibits type B MAO (MAO-B) activity with an IC(50) value of 15.3 microM using the substrate kynuramine, while not inhibiting type A MAO (MAO-A) activity. It can mitigate high phosphate-induced calcification in human aortic valve interstitial cells (HAVICs) by inhibiting phosphate cotransporter (PiT-1) gene expression and exhibits moderate antiangiogenic activity against human tumor cells.

MAO-IN-3 (Compound 5), a reversible and competitive monoamine oxidase (MAO) inhibitor with inhibition constants (K i) of 0.6 μM for MAO A and 0.2 μM for MAO B, effectively suppresses LN-229 glioblastoma cell proliferation, as denoted by an inhibitory concentration (IC50) of 0.8 μM. This compound holds potential application in cancer research [1].

ETAP, a dual inhibitor of both monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B), exhibits antidepressant-like effects and is utilized in the research of major depressive disorder [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].

Pivalylbenzhydrazine (Pivhydrazine) is a potent monoamine oxidase (MAO) inhibitor that decreases cartilage growth in normal rats and can be used in depression 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].

Monoamine oxidase Aromatase-IN-1 (compound 2q) is a potent dual inhibitor of monoamine oxidase (MAO) and aromatase, with IC50 values of 39 nM for MAO-B and 31 nM for aromatase. It holds significant potential for research in neurological disorders and breast cancer [1].

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

MAO-IN-4 (Compound 2l), a monoamine oxidase (MAO) inhibitor, demonstrates IC50 values of 0.07 μM for MAO-A and 0.75 μM for MAO-B. This compound is utilized in studying depression and Parkinson’s disease (PD) [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].

Tranylcypromine (SKF 385), a potent monoamine oxidase (MAO) inhibitor [1], is used in medicinal applications.

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].

CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 μM) and MAO-A (IC50 ≥ 10 μM). At 1-20 μM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson's disease. An additional strategy in the treatment of Parkinson's disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.

LSD1-IN-26 (compound 12u), a potent LSD1 inhibitor, exhibits an IC50 of 25.3 nM. It also demonstrates inhibition of MAO-A (IC50 = 1234.57 nM) and MAO-B (IC50 = 3819.27 nM), significantly inducing apoptosis in MGC-803 cells. This compound is applicable in gastric cancer research [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].

MAO-B-IN-26 (Compound IC9) is a dual MAO-B and acetylcholinesterase inhibitor that protects SH-SY5Y cells from Aβ-induced toxicity, including morphological alterations, reactive oxygen species (ROS) production, and membrane damage, while preventing Aβ-triggered autophagy and apoptosis, thus showing potential as a neuroprotective agent in Alzheimer's disease [1].

HIF-1α-IN-5 is an inhibitor of HIF-1α with an IC 50 value of 24 nM in HEK293T cells that also inhibits the activity of MAO-A. HIF-1α-IN-5 downregulates the mRNA expressions of VEGF and PDK1 under hypoxia. HIF-1α-IN-5 has the potential to be used in the cancer research[1].

Safrazine is an irreversible, non-specific, and orally active monoamine oxidase (MAO) inhibitor that can be used in depression research[1].

AChE-IN-11 (compound 5C) is a multifunctional agent used in Alzheimer's disease research, exhibiting neuroprotective and antioxidant activity (ORAC = 2.5 eq). It has IC50 values of 7.9 μM, 9.9 μM, and 8.3 μM against AChE, MAO-B, and BACE1, respectively. AChE-IN-11 demonstrates mixed-type AChE inhibition by binding to both the CAS and PAS of AChE and acts as a selective metal ions chelator [1].

LSD1-IN-16 (compound 4b) is a potent inhibitor of LSD1 that inhibits LSD1-CoREST, MAO-A, and MAO-B with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 also induces cell growth arrest in prostate cancer LNCaP cells with an IC50 value of 15.2 μM [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].

MAO-B-IN-16 is a selective inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 1.55 μM, suitable for research in central nervous system disorders such as Parkinson's disease [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.

ChEs MAOs-IN-2 (compound a11) serves as an inhibitor for both cholinesterases and monoamine oxidases, exhibiting IC 50 values of 0.10 µM for MAO-A, 0.20 µM for MAO-B, 0.30 µM for AChE, and 0.40 µM for BChE. This compound shows promise for Alzheimer's disease research [1].

C175-0062, a monoamine oxidase B (MAO-B) inhibitor, is applicable in research focused on neurodegenerative disorders such as Parkinson's disease (PD), Alzheimer's disease (AD), and amyotrophic lateral sclerosis (ALS) [1].

1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK NFκB and Jak2 STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydromethysticin and Desmethoxy yangonin involves transcription activation, probably through a PXR-independent or PXR-involved indirect mechanism.

IHC3 is a competitive and reversible monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.672 μM, targeting Cys172 within the enzyme's active site, used in the study of neurological diseases [1].

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].

(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.

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

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.

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

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

Peptide5 acetate reduces animal swelling, astrogliosis, and neuronal cell death after spinal cord injury. Peptide5 acetate significantly reduces the degree of spinal cord injury (SCI) in a rodent ex vivo model.