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 (444)
Related Products (444)
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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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Chuanbeinone
0 ImagesCat. No.: HY-107272CAS No.: 103530-47-8Synonyms: 22-EpidelavinoneChuanbeinone (22-Epidelavinone) is an orally active alkaloid found in Fritillaria pallidiflora. Chuanbeinone shows cytotoxicity against mutiple cancer cells and can induces apoptosis and S phase arrest. Chuanbeinone downregulates Bcl-2, upregulates Bax, and activates caspase-3. Chuanbeinone exerts anti-inflammatory and antitussive effects by reducing pro-inflammatory cytokine (IL-1β, IL-6 and TNF-α) production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways. Chuanbeinone inhibits AChE and BChE with IC50 values of 7.7 and 0.7 μM. Chuanbeinone can be used for the researches of lung carcinoma, cough, inflammatory diseases.
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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.
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(3β,5α,6α,16β)-8,14-Didehydrocevane-3,6,16,20-tetrol
0 ImagesCat. No.: HY-N10032CAS No.: 126594-75-0
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Monardic acid A
0 ImagesCat. No.: HY-N16715CAS No.: 1607436-76-9Monardic acid A is a selective inhibitor of AChE, with an IC50 of 53.1 μM against AChE from electric eel. Monardic acid A shows weak inhibitory activity against human erythrocyte AChE (IC50 >100 μM) and has no significant inhibitory effect on BChE. Monardic acid A reduces acetylcholine breakdown by inhibiting AChE activity, and also exhibits inhibitory activity against histamine release and hyaluronidase, thus exerting anti-inflammatory and neurotransmitter regulatory effects. Monardic acid A can be isolated from lungwort (Pulmonaria officinalis) and thyme (Thymus gobicus), and is mainly used in the development of anti-inflammatory drugs and drugs related to neurodegenerative diseases.
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AChE-IN-107
0 ImagesCat. No.: HY-181161AChE-IN-107 is a selective acetylcholinesterase (AChE) inhibitor with an IC50 of 0.22 μM and a Ki of 0.207 μM. AChE-IN-107 shows no inhibitory effect on equine serum BChE at 10 μM. AChE-IN-107 exhibits mixed-type inhibition of electric eel acetylcholinesterase, binding to both free enzyme and enzyme-substrate complex. AChE-IN-107 acts as a cytotoxin, reduces cell viability in hepatocellular carcinoma HepG2 cells.AChE-IN-107 can be used for the research of alzheimer's disease.
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AChE/BuChE/MAO-B-IN-2
0 ImagesCat. No.: HY-149090CAS No.: 3044829-88-8AChE/BuChE/MAO-B-IN-2 (compound 4b) is a potent AChE/BuChE inhibitor and showed good blood brain barrier (BBB) permeability in vitro with an IC50 value of 5.3 μM, 12.4 μM, 1.9±0.08 μM, for AChE, BuChE, huMAO-B, respectively. AChE/BuChE/MAO-B-IN-2 (compound 4b) can inhibit excess AChE/BuChE in Alzheimer's disease (AD) brain. AChE/BuChE/MAO-B-IN-2 (compound 4b) can be used in anti-Alzheimer's research.
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MHP 133
0 ImagesCat. No.: HY-101653CAS No.: 147340-43-0MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
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hBChE-IN-3
0 ImagesCat. No.: HY-169162hBChE-IN-3 (compound 30) is a combination of carbonic anhydrase (CA) activator and cholinesterase (ChE) inhibitor with IC50 values of 7.4 and 1.9 nM for AchE and BchE, respectively. hBChE-IN-3 can be used in the study of neurodegeneration and psychiatric disorders.
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MDAR-IN-1
0 ImagesCat. No.: HY-172884MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of NMDAR receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease.
