mao-b-in-2

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 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 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].

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.

hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective, BBB-penetrating, and competitively reversible inhibitor of hMAO-B (IC50 = 4 nM) used in Alzheimer's disease research. hMAO-B-IN-2 exhibits good neuroprotective effects and low toxicity in SH-SY5Y cells [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].

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-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-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-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].

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-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].

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].

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

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)

Selective tryptophan 2, 3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. Reduces growth of TDO-expressing P

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-2 is a dual inhibitor of MAO-B MB-COMT with IC50s of 4.27 μM and 2.69 μM for hMAO-B and MB-COMT, respectively. hMAO-B MB-COMT-IN-2 protects cells from oxidative damage and can be used in neurodegeneration disease research, such as Parkinson's Disease (PD) [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].

Neuroinflammatory-IN-2 (compound 7i) is a potent anti-neuroinflammatory agent, capable of acting on MAO-B (IC50: 10.30 μM). Neuroinflammatory-IN-2 inhibits 96.33% of Aβ1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 exhibits neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 can be used to study Alzheimer's disease.

2-PAT, analogous to Rasagiline and Selegiline, functions as a reversible MAO-A inhibitor, exhibiting an IC50 of 0.721 µM, and acts as an inactivator of MAO-B with an IC50 value of 14.6 µM. This compound shows promise for research in Parkinson's disease and depression.

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].

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.