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 (456)
Related Products (456)
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Territrem B
0 ImagesCat. No.: HY-126765CAS No.: 70407-20-4
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HDAC6-IN-5
0 ImagesCat. No.: HY-146678CAS No.: 2413603-15-1HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity.
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ZLMT-12
0 ImagesCat. No.: HY-151436CAS No.: 2841473-39-8ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
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Icopezil maleate
0 ImagesCat. No.: HY-105157ACAS No.: 145815-98-1Synonyms: CP-118954 maleateIcopezil maleate (CP-118954 maleate) is an orally active, selective AchE inhibitor with an IC50 of 0.33 nM. Icopezil maleate 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 maleate serves as a parent compound for radioiodine-labeled acetylcholinesterase imaging agents. Icopezil maleate is applicable to research related to Alzheimer's disease.
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AChE-IN-72
0 ImagesCat. No.: HY-163909AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 0.59 μM. AChE-IN-72 inhibits BChE with an IC50 of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC50 of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable.
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hAChE-IN-6
0 ImagesCat. No.: HY-155366CAS No.: 3007667-17-3hAChE-IN-6 (compound 51) is a brain penetrant AChE inhibitor with an IC50 of 0.16 μM. hAChE-IN-6 also inhibits hBuChE and GSK3β with IC50 values of 0.69 μM and 0.26 μM, respectively. hAChE-IN-6 inhibits tau protein and Aβ1-42 self-aggregation, and can be used for Alzheimer's disease (AD) research.
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SB-1436
0 ImagesCat. No.: HY-149300CAS No.: 2925298-08-2SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC50s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with Kis of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research.
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BChE/hCA II-IN-1
0 ImagesCat. No.: HY-178017BChE/hCA II-IN-1 (Compound 20) is a dual-functional inhibitor of Butyrylcholinesterase (BChE) and human carbonic anhydrase II (hCA II) with IC50s of 76.50 and 10.69 μM for BChE and hCA II, respectively. BChE/hCA II-IN-1 can be used for neurodegenerative diseases like Alzheimer's and glaucoma research.
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hAChE-IN-9
0 ImagesCat. No.: HY-168052hAChE-IN-9 (compound 7i) is a selective inhibitor of human acetylcholinesterase (hAChE) with IC50 of 0.05 μM and 2.85 μM for AChE and BChE, respectively. hAChE-IN-9 modulates toxic Aβ oligomer forms into non-toxic ones and has antioxidant and neuroprotective effects against Aβ-induced toxicity. hAChE-IN-9 can be used for the study of Alzheimer's disease.
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AChE-IN-14
0 ImagesCat. No.: HY-146035CAS No.: 2390042-05-2AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease.
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AChE-IN-100
0 ImagesCat. No.: HY-180113AChE-IN-100 (Compound 5n) is an AChE inhibitor with an IC50 of 2.38 nM. AChE-IN-100 shows superior ROS-scavenging capabilities. AChE-IN-100 has antioxidant capacity. AChE-IN-100 shows a significant neuroprotective effect against hydrogen peroxide-induced damage. AChE-IN-100 can be used in the research of Alzheimer’s diseases.
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ChE/GSK-3β-IN-1
0 ImagesCat. No.: HY-179496ChE/GSK-3β-IN-1 (compound 18o) is a potent dual ChE/GSK-3β inhibitor. ChE/GSK-3β-IN-1 exhibits dual inhibition of AChE (IC50 = 1.7 μM), butyrylcholinesterase (BChE) (IC50 = 5.3 μM), and GSK-3β (IC50 = 5.7 μM). ChE/GSK-3β-IN-1 inhibits Aβ1-42 self-aggregation. ChE/GSK-3β-IN-1 can be used for Alzheimer’s disease (AD) research.
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AChE-IN-120
0 ImagesCat. No.: HY-184791AChE-IN-120 is a blood-brain barrier-permeable AChE inhibitor, with an IC50 of 0.91 μM and a Ki of 1.027 μM against human AChE. AChE-IN-120 exerts neuroprotective effects against oxidative damage. AChE-IN-120 can be used for the research of Alzheimer's disease.
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GFAP/NF-κB/APOE/NLRP3-IN-1
0 ImagesCat. No.: HY-183796GFAP/NF-κB/APOE/NLRP3-IN-1 is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC50 of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC50 of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ1-42 aggregation with an IC50 of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma.
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AChE-IN-81
0 ImagesCat. No.: HY-170925AChE-IN-81 (compound 22) is a potent, irreversible and selective AChE inhibitor. AChE-IN-81 inhibits activity on AChE with inhibitory rates of 80.0%, with an IC50 of 3.7 μM. AChE-IN-81 binds to AChE with a binding affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces in zebrafish brain cells. AChE-IN-81 exhibits potential neuroprotective activities on H2O2-induced SH-SY5Y cell injury model.
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Luteolin 5,3'-dimethyl ether
0 ImagesCat. No.: HY-N9846CAS No.: 62346-14-9Luteolin 5,3'-dimethyl ether is a flavonoid compound that exhibits strong binding to enzymes such as acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-Glycosidase. Luteolin 5,3'-dimethyl ether can be naturally extracted from the dried roots of Alhagi maurorum (camel thorn). The methanol extract of this plant has significant free radical scavenging ability and enzyme inhibitory potential. Luteolin 5,3'-dimethyl ether can be used in research related to neurodegenerative diseases, diabetes, and skin pigmentation-related diseases.
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BuChE-IN-22
0 ImagesCat. No.: HY-181865BuChE-IN-22 is a pseudo-irreversible butyrylcholinesterase (BuChE) inhibitor, with IC50 values of 4 nM and 157 nM against hBuChE and hAChE, respectively. It also acts as a prodrug of 7-hydroxysertraline. BuChE-IN-22 releases 7-hydroxysertraline during BuChE inhibition. BuChE-IN-22 completely reverses Aβ25-35-induced short-term and long-term memory impairments in a mouse model of Alzheimer's disease. BuChE-IN-22 can be used in research related to Alzheimer's disease.
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BChE/p38-α MAPK-IN-2
0 ImagesCat. No.: HY-178433BChE/p38-α MAPK-IN-2 is a BChE and p38-α MAPK dual inhibitor. BChE/p38-α MAPK-IN-2 inhibits hBChE with an IC50 of 5.1 nM, showing 1000-fold selectivity over hAChE. BChE/p38-α MAPK-IN-2 inhibits p38α MAPK with an IC50 of 8.12 μM. BChE/p38-α MAPK-IN-2 exhibits neuroprotective effect and can be used for the research of neurological disease, such as Alzheimer’s disease.
