AChE
Acetylcholinesterase (AChE) is the principal cholinergic enzyme that rapidly hydrolyzes acetylcholine at cholinergic synapses and neuromuscular junctions, thereby terminating neurotransmission and maintaining synaptic signaling fidelity[1]. Mechanistically, AChE regulates cholinergic pathway activity through efficient acetylcholine clearance, a process that is essential for normal neuronal communication and neuromuscular function[1]. Beyond its catalytic role, AChE displays multiple molecular forms and has been implicated in cellular interactions, neuronal activity modulation, and pathological states, supporting broader biological functions outside classical neurotransmission[1]. In neurodegenerative disease models, particularly Alzheimer’s disease (AD), altered cholinergic signaling is closely associated with cognitive impairment, and cholinesterase inhibition remains a major symptomatic therapeutic strategy[2][3]. Compared with the related isoform butyrylcholinesterase (BChE), AChE is the predominant cholinesterase in the brain and plays a primary role in synaptic acetylcholine hydrolysis, whereas BChE may compensate when AChE activity is reduced and exhibits distinct pathological changes during AD progression[3][4]. For experimental and translational applications, reversible and dual AChE/BChE inhibitors, including rivastigmine, are widely used to enhance cholinergic neurotransmission and investigate mechanisms underlying neurodegeneration and cognitive dysfunction[2][3].
References:
- [1]. Massoulié J, et al. Structure and functions of acetylcholinesterase and butyrylcholinesterase. Prog Brain Res. 1993;98:139-46. [Content Brief]
- [2]. Walczak-Nowicka ŁJ, et al. Acetylcholinesterase Inhibitors in the Treatment of Neurodegenerative Diseases and the Role of Acetylcholinesterase in their Pathogenesis. Int J Mol Sci. 2021 Aug 27;22(17):9290. [Content Brief]
- [3]. Nordberg A, et al. A review of butyrylcholinesterase as a therapeutic target in the treatment of Alzheimer's disease. Prim Care Companion CNS Disord. 2013;15(2):PCC.12r01412. [Content Brief]
- [4]. Geula C, et al. Butyrylcholinesterase, cholinergic neurotransmission and the pathology of Alzheimer's disease. Drugs of Today (Barcelona, Spain : 1998). 2004 Aug;40(8):711-721. [Content Brief]
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AChE Related Products (482)
Related Products (482)
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Desoxypeganine hydrochloride
0 ImagesCat. No.: HY-108048ACAS No.: 61939-05-7Synonyms: Deoxypeganine hydrochloride; Deoxyvasicine hydrochlorideDesoxypeganine (Deoxypeganine) hydrochloride, an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine hydrochloride can be used for alcohol abuse research.
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AChE/BChE-IN-3 hydrochloride
0 ImagesCat. No.: HY-146663ACAS No.: 2410992-69-5
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MR2938
0 ImagesCat. No.: HY-149087CAS No.: 1044870-65-6
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Icopezil
0 ImagesCat. No.: HY-105157CAS No.: 145508-78-7Synonyms: CP-118954Icopezil (CP-118954) is an orally active, selective AchE inhibitor with an IC50 of 0.33 nM. Icopezil increases acetylcholine levels in the brain and striatum of mammals, induces centrally mediated tremors and peripherally mediated salivation, and improves working memory performance in aged dogs. Icopezil serves as a parent compound for radioiodine-labeled acetylcholinesterase imaging agents. Icopezil is applicable to research related to Alzheimer's disease.
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Pitofenone
0 ImagesCat. No.: HY-105853CAS No.: 54063-52-4Pitofenone, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with Kis of 36 and 45 μM, respectively.
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Multi-target kinase-IN-11
0 ImagesCat. No.: HY-189488Multi-target kinase-IN-11 (compound 2a) is a potent multi-target inhibitor of Cholinesterase and Carbonic Anhydrase. Multi-target kinase-IN-11 inhibits AChE, BChE, hCA I, and hCA II with IC50 values of 2.78, 4.88, 0.94, and 4.15 μM, respectively. Multi-target kinase-IN-11 inhibits these enzymes through hydrogen bonding and electrostatic interactions with active site residues. Multi-target kinase-IN-11 can be used for research on Alzheimer's disease.
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AP2238
0 ImagesCat. No.: HY-119292CAS No.: 553681-56-4AP2238 is a dual-function acetylcholinesterase (AChE) inhibitor with Ki values for human AChE (HuAChE) and butyrylcholinesterase (BuChE) of 21.7 and 48.9 μM respectively. AP2238 blocks the pro-fibrotic interaction between the peripheral site of AChE and Aβ, and can inhibit Aβ aggregation. AP2238 can be used for the research of Alzheimer's disease.
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MAO-A-IN-4
0 ImagesCat. No.: HY-181110MAO-A-IN-4 is a highly selective and reversible inhibitor of monoamine oxidase A (MAO-A), with an IC50 of 0.06 μM against hMAO-A. MAO-A-IN-4 exhibits anti-inflammatory, antioxidant, neuroprotective, and antidepressant activities. MAO-A-IN-4 possesses favorable ADME properties and is suitable for research related to depression.
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AD-35
0 ImagesCat. No.: HY-117710BCAS No.: 1531586-64-7AD-35 is an orally active, blood-brain barrier-permeable acetylcholinesterase inhibitor with an IC50 of 793 nM. AD-35 inhibits metal-induced amyloid-β aggregation and disassembles preformed amyloid-β aggregates. In rat models of cognitive impairment, AD-35 attenuates Aβ25-35-induced astrocyte activation, TNF-α and IL-1β release, inhibits ERK phosphorylation, and alleviates learning and memory deficits. AD-35 can be used for research on Alzheimer's disease.
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AChE-IN-122
0 ImagesCat. No.: HY-189417AChE-IN-122 is an acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) inhibitor with IC50 values of 0.084 μM and 0.65 μM, respectively, and an IC50 of 0.667 μM against butyrylcholinesterase (BuChE). AChE-IN-122 can be used for research on Alzheimer's disease.
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AChE/MAO-B-IN-8
0 ImagesCat. No.: HY-181141AChE/MAO-B-IN-8 is an acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) inhibitor with IC50 values of 0.72 and 0.19 μM. AChE/MAO-B-IN-8 interactions with AChE and MAO-B active-site amino acid residues. AChE/MAO-B-IN-8 can be used for the research of Alzheimer’s disease.
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CAI/II-IN-8
0 ImagesCat. No.: HY-161507CAS No.: 3036136-18-9CAI/II-IN-8 (Compound 8) is a hydrazide derivative based on 4-hydroxybenzaldehyde. CAI/II-IN-8 primarily targets human carbonic anhydrase isomerase I (hCA I) and II (hCA II) for inhibition (IC50 = 21.35 ± 0.39 nM (CA I); 7.12 ± 0.12 nM (CA II)). CAI/II-IN-8 inhibits AChE and BChE as well(IC50 = 46.27 ±0.75 nM (AChE); 43.38 ± 0.83 nM (BChE)). ..
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AChE-IN-117
0 ImagesCat. No.: HY-184140AChE-IN-117 is an AChE/nAChR inhibitor with larvicidal activity against Culex pipiens third-instar larvae. AChE-IN-117 forms stable catalytic site interactions to disrupt cholinergic signaling. AChE-IN-117 binds to its receptor via hydrogen bonding and π-cation interactions to interfere with cholinergic synaptic transmission. AChE-IN-117 induces neurotoxic symptoms including hyperactivity, erratic movement, tremors, paralysis, and larval mortality. AChE-IN-117 can be used for the research of mosquito-borne infectious diseases.
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Itopride
0 ImagesCat. No.: HY-B0732ACAS No.: 122898-67-3Synonyms: HSR803 free baseItopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).
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Multi-kinase-IN-10
0 ImagesCat. No.: HY-180892Multi-kinase-IN-10 (Compound IIIk) is a multi-kinase inhibitor. Multi-kinase-IN-10 exhibits significant calcium channel blocking activity, with its IC50 being 26.67 μM. Multi-kinase-IN-10 is a potent dual cholinesterase inhibitor, with its IC50 values for hAChE and hBuChE being 0.304 μM and 1.033 μM respectively. Multi-kinase-IN-10 has antioxidant and neuroprotective activities, and shows significant anti-amnesia activity. Multi-kinase-IN-10 can be used for research on Alzheimer's disease.
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Insecticidal agent 33
0 ImagesCat. No.: HY-183949Insecticidal agent 33 is an AChE inhibitor with nematicidal activity. Insecticidal agent 33 impairs locomotor activity of Caenorhabditis elegans, and induces oxidative damage in Caenorhabditis elegans, including elevated reactive oxygen species (ROS) levels, lipofuscin accumulation, lipid deposition, and disrupted cellular homeostasis. Insecticidal agent 33 can be used for the research of plant-parasitic nematode infection.
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AChE/BChE-IN-37
0 ImagesCat. No.: HY-183760AChE/BChE-IN-37 is a blood-brain barrier-permeable AChE/BChE inhibitor, with an IC50 of 73.65 μM against electric eel-derived AChE and an IC50 of 82.93 μM against horse-derived BChE. AChE/BChE-IN-37 exhibits chelating activity towards Cu2+, Ca2+, Mg2+, Fe2+ and Zn2+. AChE/BChE-IN-37 interacts with HSP90AA1 and GSK-3β. AChE/BChE-IN-37 inhibits the self-induced aggregation of Aβ1-42. AChE/BChE-IN-37 suppresses LPS-induced NO production in cells. AChE/BChE-IN-37 can be used in research related to Alzheimer's disease and inflammatory diseases.
