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, 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].

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-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).

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.

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].

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)

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.

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.

LSD1-IN-12 (compound 2) is an effective inhibitor of LSD1, with inhibitory Ki values of 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), and 3.5 μM (MAO-B) [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 and can be utilized in neurodegenerative disease research, such as Parkinson's Disease (PD) [1].