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 (446)
Related Products (446)
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AChE/BChE-IN-20
0 ImagesCat. No.: HY-159081CAS No.: 3052008-10-0AChE/BChE-IN-20 (compound 3m) is an acetylcholinesterase (AChE, IC50=34.81 μM) and butylcholinesterase (BChE, IC50=20.66 μM) inhibitor, which has been demonstrated to have affinity for key enzyme pockets and favorable interaction profiles by molecular docking and kinetic simulations, and can be used in the study of Alzheimer's disease.
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NDs-IN-1
0 ImagesCat. No.: HY-158334CAS No.: 3033806-97-9(Neurodegenerative diseases) NDs-IN-1 (Compound 3g) inhibits the activities of key enzymes such as hBACE-1, hAChE and hMAO-B. NDs-IN-1 is a novel non-covalent multi-target inhibitor. NDs-IN-1 is mainly used in the study of neurodegenerative diseases.
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AChE/BChE/MAO-B-IN-5
0 ImagesCat. No.: HY-172460CAS No.: 1432738-00-5AChE/BChE/MAO-B-IN-5 is a multitarget inhibitor of cholinesterases (AChE and BChE) and monoamine oxidase MAO-B with blood–brain barrier permeability. It exhibits IC50 values of 0.24 µM, 6.29 µM, and 0.11 µM against AChE, BChE, and MAO-B, respectively. AChE/BChE/MAO-B-IN-5 shows promise for research in the field of neurodegenerative diseases such as Alzheimer's disease.
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AChE/BChE-IN-1
0 ImagesCat. No.: HY-131971CAS No.: 2720624-42-8AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease.
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BChE-IN-5
0 ImagesCat. No.: HY-143465CAS No.: 2983586-25-8
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Flucopride
0 ImagesCat. No.: HY-168241CAS No.: 1639925-34-0Flucopride (Compound 4a) is an AChE inhibitor (IC50: 24 nM), and a partial 5-HT4R agonist (Ki: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT4R (EC50: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay).
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hAChE-IN-10
0 ImagesCat. No.: HY-170583CAS No.: 3058182-98-9hAChE-IN-10 (Compound ET11) is the inhibitor for human acetylcholinesterase (AChE) with an IC50 of 6.34 nM. hAChE-IN-10 scavenges free radicals, and exhibits antioxidant activity. hAChE-IN-10 exhibits metal chelating activity, inhibits Cu2+-induced Aβ1-42 aggregation, reduces the formation of amyloid plaques, and exhibits neuroprotective activity. hAChE-IN-10 ameliorates the Scopolamine (HY-N0296)-induced cognitive impairment in mouse models.
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AChE-IN-85
0 ImagesCat. No.: HY-173144AChE-IN-85 (Compound 7k) is an AChE inhibitor with an IC50 of 0.083 μM. AChE-IN-85 can inhibit the release of NO, the production of TNF-α and IL-1β, the levels of LDH and ROS, as well as the aggregation of Aβ42. AChE-IN-85 has anti-inflammatory and neuroprotective effects and can be used in the research of diseases such as Alzheimer's disease.
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Stacofylline
0 ImagesSynonyms: S 9977 free base; S 9977-2 free baseStacofylline (S 9977 free base; S 9977-2 free base), a Xanthine (HY-W017389) derivative, is a potent AChE inhibitor with an IC50 of 5-50 nM. Stacofylline shows anti-amnesic and promnesic activities.
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8-Hydroxydihydrochelerythrine
0 Images8-Hydroxydihydrochelerythrine is a benzophenanthridine alkaloid-derived, selective and competitive AChE inhibitor (IC50=0.61 μM) isolated from the roots of Zanthoxylum nitidum (Roxb.) DC. 8-Hydroxydihydrochelerythrine increases the content of acetylcholine in the synapses of cholinergic neurons and enhances cholinergic neurotransmission. 8-Hydroxydihydrochelerythrine is applicable to the research of neurodegenerative diseases with dementia such as Alzheimer's disease.
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tau/Aβ40 aggregation-IN-1
0 ImagesCat. No.: HY-149272CAS No.: 2973377-10-3tau/Aβ40 aggregation-IN-1 (Compound 20) is a tau and Aβ40 aggregation inhibitor with IC50s of 1.8 μM and 1.3 μM, respectively.
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AChE/BChE-IN-6
0 ImagesCat. No.: HY-146315CAS No.: 2416910-94-4AChE/BChE-IN-6 (compound 22) is a potent dual AChE/BChE inhibitor with IC50 values of 0.809 µM, 2.248 µM and > 100 µM for hBChE, hAChE and hMAO-B, respectively. AChE/BChE-IN-6 penetrates the blood-brain barrier (BBB). AChE/BChE-IN-6 can be used for Alzheimer’s disease (AD) research.
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AChE-IN-24
0 ImagesCat. No.: HY-151152CAS No.: 3033542-32-1AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD).
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AChE-IN-51
0 ImagesCat. No.: HY-157382AChE-IN-51 (compound 8C) is an orally active, non-competitive inhibitor of AChE and BChE (IC50: 84 nM, 97 nM). It also inhibits MMP-2 and amyloid Aβ1-42 aggregates (IC50: 724 nM, 302 nM). AChE-IN-51 has low cytotoxicity and in silico predicted blood-brain barrier permeability. Can be used for research on diseases such as Alzheimer's disease (AD).
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Artanin
0 ImagesCat. No.: HY-N2898CAS No.: 96917-26-9Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChE inhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitory activities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively.
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ACS03
0 ImagesCat. No.: HY-177958CAS No.: 2227022-64-0ACS03 is a hybrid thiophene-acridine compound. ACS03 induces an increase in lactate dehydrogenase, glutathione S-transferase, and AChE activities. ACS03 has antileishmanial activity. ACS03 exhibits selective anti-cancer effects against colon carcinoma.
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MAO-B-IN-50
0 ImagesCat. No.: HY-180842CAS No.: 3105860-84-9MAO-B-IN-50 (Compound C20) is a selective MAO-B inhibitor with an IC50 value of 0.06 μM. MAO-B-IN-50 shows good inhibitory effects on the aggregation of Aβ40/42 and Tau proteins, with overall IC50 values around 1 μM. MAO-B-IN-50 exhibits potent and selective AChE inhibition (IC50 = 1.78 μM). MAO-B-IN-50 can be used in the research of Alzheimer's disease.
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BChE-IN-49
0 ImagesCat. No.: HY-181248BChE-IN-49 is an orally active BChE inhibitor with IC50 values of 0.73 μM and 6.43 μM against BChE and AChE, respectively. BChE-IN-49 reduces AChE levels to inhibit the degradation of acetylcholine. By inhibiting GSK-3β, BChE-IN-49 potently activates the Wnt/β-catenin signaling pathway, exerting potent anti-Aβ, antioxidant, anti-neuroinflammatory and anti-apoptotic effects. BChE-IN-49 can be used in research related to Alzheimer's disease.
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AChE/BuChE/MAO-B-IN-1
0 ImagesCat. No.: HY-151562CAS No.: 2834758-29-9AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC50s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ1 and σ2 receptors with Ki values of 42.8 nM (human σ1 receptor) and 191 nM (rat σ2 receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research.
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Skimmianine (Standard)
0 ImagesSkimmianine (Standard) is the analytical standard of Skimmianine. This product is intended for research and analytical applications. Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca2+ signaling and protein kinase C signaling.
