hMAO-A

Compound 8 (hMAO-A-IN-1) is a potent inhibitor of hMAO-A, exhibiting an IC50 value of 90 nM. It may be utilized in studies targeting anxiety and depression [1].

Salvigenin is a potent hMAO-A inhibitor, has neuroprotective, antitumor and immunomodulatory effects.

Osthenol is a natural product, and is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM).It shows antitumor-promoting activity, it also has antifungal and antibacterial activities.

Obtusin is a natural product.

hMAO-B-IN-32 is a potent hMAO-B selective inhibitor with an IC50 of 45.52 μM.

hMAO-B-IN-4 is a selective, reversible and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B, IC50=0.067 μM, Ki= 0.03 μM, hMAO-A, IC50= 33.82 μM).

Moclobemide (Ro111163) is a reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.

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).

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. It inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50 values of 0.072, 9.81, 14.52, 0.024, and 2.42 μM, respectively. Additionally, AChE-IN-82 inhibits COX-1, COX-2, and 5-LOX with IC50 values of 60.41, 0.187, and 0.18 μM, respectively. The compound also demonstrates strong neuroprotective effects by significantly reducing H2O2-induced oxidative stress.

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-43 (4) is a potent inhibitor of hMAO-B and a mild inhibitor of GSK3β kinase, with Ki values for hMAO-A and hMAO-B of 0.044 μM and 0.004 μM, respectively. This compound is applicable in the study of neurodegenerative diseases.

MAO-B-IN-28 (compound 10e) is a potent hMAO-B inhibitor with an IC50 value of 1.9±0.5 nM, potentially serving as a candidate molecule for neurodegenerative disease research.

MAO-B-IN-46 (Compound 16) is a selective human MAO-B inhibitor with an IC50 of 26.8 nM, while showing weaker activity against hMAO-A (IC50: 7.2054 μM). This compound, also referred to as MAO-B-IN-46 (Compound 8), acts as an α-amylase inhibitor with an IC50 of 19.46 μM. It demonstrates certain neuroprotective properties and exhibits no significant toxicity to human gingival fibroblasts and SH-SY5Y cells. Additionally, MAO-B-IN-46 can scavenge DPPH and ABTS radicals, with IC50 values of 17.86 and 17.71 μM, respectively. MAO-B-IN-46 is applicable in research on neurodegenerative diseases like Parkinson's, diabetes, and conditions related to oxidative stress.

8-CSC is a dual agent endowed with good hMAO-B inhibitory activity (Ki: 235 nM in baboon liver mitochondria) and A2A affinity (Ki: 36 nM in rat brain striatal membranes receptor).

TB5 is a potent, selective, and reversible inhibitor of hMAO-B.

Rubrofusarin triglucoside, a glycoside isolated from Cassia obtusifolia Linn seeds, demonstrates inhibitory activity against human monoamine oxidase A (hMAO-A), exhibiting an IC50 value of 85.5 μM[1].

Chrysophanol-1-O-β-gentiobioside, an anthraquinone glycoside derived from the seeds of Cassia obtusifolia, specifically inhibits hMAO-A isozyme activity with an IC50 value of 96.15 μM.

Nrf2-ARE/hMAO-B/QR2 modulator 1, a resveratrol derivative and multi-target-directed ligand (mtdl), activated the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibited hMAO-B and QR2（quinone reductase-2，NQO2) (IC 50 = 8.05 and 0.57 μM), and was able to promote hippocampal neurogenesis and exert neuroprotective and antioxidant effects in an Alzheimer's disease model.

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].

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].

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.

hMAO-B-IN-3 (Compound 15) is a potent hMAO-B inhibitor (IC50 = 47.4 nM) with favorable drug-like properties and a broad safety window, making it a suitable candidate for lead optimization and multitarget-directed ligand development [1].

H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist with inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, it demonstrates favorable anti-neuropathic pain and memory-enhancing effects and can cross the blood-brain barrier (BBB) [1].

hMAO-B-IN-5 is a potent reversible and selective human monoamine oxidase hMAO-B inhibitor (IC50:0.12μM). hMAO-B-IN-5 can cross the blood-brain barrier and can be used in the study of Parkinson's disease. It is a promising compound in the treatment and diagnosis of central nervous system diseases.