MAO-B-IN-1

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

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-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-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-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-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].

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-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-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].

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-19, a selective MAO-B inhibitor, exhibits neuroprotective and anti-inflammatory properties and demonstrates an IC50 value of 0.67 μM [1].

hMAO-B-IN-10 (compound 7) is an inhibitor of MAO-A/B with IC50 values of 424.1 nM and 177.9 nM, respectively. It has demonstrated neuroprotective effects in the MPTP-induced mouse model of Parkinson's Disease (PD).

hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 value of 0.11 µM. It operates by competitively binding to the active site of hMAO-B, thereby preventing the oxidative deamination of monoamines and reducing hydrogen peroxide production. Additionally, hMAO-B-IN-11 inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia. This compound holds potential for research in neurodegenerative diseases such as Parkinson's and Alzheimer's.

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-17 is a selective and potent monoamine oxidase B (MAO-B) inhibitor (IC50: 5.08 μM) used in the study of central nervous system disorders, including Parkinson's.

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

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].

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.

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

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)