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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AChE-IN-95
0 ImagesCat. No.: HY-175856AChE-IN-95 (Compound 7) is a highly selective competitive acetylcholinesterase (AChE) inhibitor (IC50=17.87 μM, Ki=19.48 μM). AChE-IN-95 exhibits strong cytotoxicity against SH-SY5Y neuroblastoma cells. AChE-IN-95 is promising for research of Alzheimer’s disease and neurodegenerative disorders.
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Isograndifoliol
0 ImagesCat. No.: HY-N10781CAS No.: 1445475-53-5Isograndifoliol is a selective inhibitor of butyrylcholinesterase (BChE) with an IC50 value of 0.9 μM. And Isograndifoliol moderately inhibits acetylcholinesterase (AChE) with an IC50 value of 342.9 μM. Isograndifoliol also has vasorelaxant effect and anti-tumor effect. Isograndifoliol can be used for research against dementia caused by neurodegenerative diseases.
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Circumdatin C
0 ImagesCat. No.: HY-N16739CAS No.: 223130-61-8Circumdatin C is an alkaloid. Circumdatin C shows inhibitory effects against LPS-stimulated NO production. Circumdatin C inhibits AChE activity with an IC50 value of 13.9 μM. Circumdatin C can be used in the research of Alzheimer's disease.
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hBChE-IN-1
0 ImagesCat. No.: HY-149273CAS No.: 1776948-12-9hBChE-IN-1 (compound 4), a quinolizidinyl derivative, is a potent hBChE inhibitor (IC50=7 nM) and highly selective over hAChE. hBChE-IN-1 shows inhibitory activity against tau and Aβ40 protein aggregation, with IC50 values of 20 and 4.3 μM, respectively. hBChE-IN-1 can be used for Alzheimer's disease research.
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AChE-IN-47
0 ImagesCat. No.: HY-157296CAS No.: 3033056-55-9AChE-IN-47 (compound g17) is a AChE inhibitor with the IC50 of 0.24 μM. AChE-IN-47 inhibits amyloid β peptides self-aggregation. AChE-IN-47 displays neuroprotective effects and effectively suppresses the intracellular accumulation of reactive oxygen species.
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AChE-IN-11
0 ImagesCat. No.: HY-115973AChE-IN-11 (compound 5C) is a triple inhibitor targeting AChE/MAO-B/BACE1 (IC50=7.9 μM, 9.9 μM, 8.3 μM, respectively) and a selective metal ion chelators. AChE-IN-11 exhibits mixed AChE inhibitory effects, binding to both CAS and PAS of AChE. AChE-IN-11 also exhibits good antioxidant activity (ORAC=2.5 eq) and potential neuroprotective effects in Alzheimer's disease.
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AChE-IN-90
0 ImagesCat. No.: HY-174462AChE-IN-90 (Compound 5b) is an orally active, brain-penetrant and potent acetylcholinesterase (AChE) inhibitor with an IC50 value of 0.023 μM against human AChE and lower selectivity for butyrylcholinesterase (BuChE) (IC50 1.8 μM). AChE-IN-90 increases acetylcholine levels in the synaptic cleft. AChE-IN-90 is promising for research of neurodegenerative diseases such as Alzheimer's disease.
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(±)Phenserine
0 ImagesCat. No.: HY-103374BCAS No.: 159652-53-6Synonyms: (±)-Eseroline phenylcarbamate(±)Phenserine ((±)-Eseroline phenylcarbamate) is the racemic form of Phenserine (HY-103374). Phenserine is a derivative of Physostigmine (HY-N6608) and is an effective, non-competitive, long-acting and selective AChE inhibitor. Phenserine can reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ). Phenserine can improve cognitive ability and slow down the progression of Alzheimer's disease.
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AChE-IN-10
0 ImagesCat. No.: HY-144775CAS No.: 2770832-90-9AChE-IN-10 (Compound 24r) is a potent inhibitor of AChE (IC50 = 2.4 nM). AChE-IN-10 potently inhibits AChE, reduces tau phosphorylation at S396 residue, provides neuroprotection by rescuing neuronal morphology and increasing cell viability. AChE-IN-10 is also found to reduce amyloid aggregation in the presence of AChE.
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AChE/BChE-IN-34
0 ImagesCat. No.: HY-181167AChE/BChE-IN-34 is an acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor with IC50s of 5.97 μM and 4.57 μM, respectively. AChE/BChE-IN-34 functions as an antioxidant, oxidative stress inhibitor, reduces MDA levels, and elevates SOD and catalase in hippocampal tissue. AChE/BChE-IN-34 acts as a cognitive function enhancer, improves learning and memory in a Scopolamine (HY-N0296)-induced animal model. AChE/BChE-IN-34 is non-toxic in neuroblastoma cells across a specified concentration range. AChE/BChE-IN-34 can be used for the research of Alzheimer's disease.
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MAO-B-IN-48
0 ImagesCat. No.: HY-175523MAO-B-IN-48 is a selective MAO-B inhibitor (IC50 = 0.09 μM, Ki = 0.02 μM). MAO-B-IN-48 exhibits inhibitory activity against hBChE (IC50 = 1.10 μM, Ki = 0.43 μM) and AChE (IC50 = 0.56 μM, Ki = 0.14 μM). MAO-B-IN-48 suppresses self-induced aggregation of toxic β-amyloid peptides and exerts antioxidant activity, including DPPH radical scavenging, CUPRAC copper ion reduction, and superoxide anion scavenging. MAO-B-IN-48 can be used for the study of Alzheimer's disease (AD).
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hAChE/hBACE-1-IN-2
0 ImagesCat. No.: HY-149288hAChE/hBACE-1-IN-2 is a potent, orally active, blood-brain barrier transboundary triple inhibitor of hAChE, hBChE, and HACE-1 with IC50s of 0.113 μM, 1.48 μM and 0.38 μM, respectively. hAChE/hBACE-1-IN-2 has antioxidant activity. hAChE/hBACE-1-IN-2 also inhibits Aβ11-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease.
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AChE/BChE-IN-36
0 ImagesCat. No.: HY-182290AChE/BChE-IN-36 is a dual acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor with blood-brain barrier permeability. AChE/BChE-IN-36 mediates blood-brain barrier transport through specific interactions with choline transporters. AChE/BChE-IN-36 can be used for the research of Alzheimer's disease.
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Dyclonine hydrochloride (Standard)
0 ImagesSynonyms: Dyclocaine hydrochloride (Standard)Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.
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Trimedoxime dichloride
0 ImagesTrimedoxime dichloride (TMB-4 dichloride) is a blood-brain barrier-permeable cholinesterase reactivator. Trimedoxime dichloride reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime dichloride reduces mortality and prolongs survival time. Trimedoxime dichloride exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime dichloride can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning.
