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/MAO-IN-2
0 ImagesCat. No.: HY-152110Dual AChE-MAO B-IN-5, indanone derivative, is a potent dual AChE/MAO-B inhibitior with IC50 values of 0.0224, 0.0412, and 0.1116 μM for AChE, MAO-B and MAO-A, respectively. Dual AChE-MAO B-IN-5 has antioxidant activity and prevents β-amyloid plaque aggregation. Dual AChE-MAO B-IN-5 can be used for Alzheimer’s disease (AD) research.
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Brassicasteryl linoleate
0 ImagesCat. No.: HY-186298CAS No.: 73691-63-1Brassicasteryl linoleate is a cholinesterase inhibitor. Brassicasteryl linoleate inhibits acetylcholinesterase, butyrylcholinesterase and urease. Brassicasteryl linoleate inhibits lipid peroxidation. Brassicasteryl linoleate is applicable to research related to breast cancer, lung cancer and colon adenocarcinoma.
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Merulinic acid
0 ImagesCat. No.: HY-N19855CAS No.: 69506-63-4Synonyms: Geranicardic acid
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hAChE-IN-3
0 ImagesCat. No.: HY-155085CAS No.: 2983723-56-2hAChE-IN-3 (compounds 5c) is a potent and blood-brain barrier permeable AChE, BuChE， MAO-B-IN-1 and BACE-1 inhibitor, with IC50 values of 0.44, 0.08, 5.15 and 0.38 μM, respectively. hAChE-IN-3 has antioxidant activity and metal chelating ability. In addition, hAChE-IN-3 can bind to peripheral anion sites, and affect β amyloid and reduce Alzheimer's-associated neurodegeneration. hAChE-IN-3 has the potential for the research of Alzheimer's disease.
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AChE/PDE4-IN-1
0 ImagesCat. No.: HY-147846CAS No.: 3033234-46-4AChE/PDE4-IN-1 (compound 12c) is a potent and selective dual PDE4/AChE inhibitor, with IC50s of 0.28 μM and 1.88 μM for AChE and PDE4D, respectively. AChE/PDE4-IN-1 exhibits anti-neuroinflammatory effect for the research of Alzheimer's disease.
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Cubebin
0 ImagesCat. No.: HY-N10423CAS No.: 18423-69-3Synonyms: (-)-CubebinCubebin ((-)-Cubebin), a dibenzyl butyrolactone lignan, is an orally active AChE inhibitor. Cubebin binds to active sites of NF-κB, TNF-α, and TGF-β1 via hydrogen and hydrophobic interactions, obstructing critical residues to inhibit pro-inflammatory or renal fibrosis-related activity. Cubebin enhances p38 MAPK phosphorylation to increase tyrosinase gene expression, stimulating melanogenesis via elevated tyrosinase activity, expression, and mRNA levels. Cubebin reduces oxidative stress via enhanced endogenous antioxidant enzyme activity and inhibited lipid peroxidation, regulates lipid metabolism, improves glycemic control, and exerts renoprotective effects via reduced renal dysfunction markers and improved renal architecture. Cubebin shows antimicrobial activity. Cubebin exerts larvicidal activity against Angiostrongylus cantonensis larvae, with no cytotoxicity toward monkey or human cell lines or Caenorhabditis elegans. Cubebin can be used for the research of diabetic nephropathy, melanoma, colon adenocarcinoma, neuroangiostrongyliasis, Alzheimer’s disease (AD) and depression.
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α-Amylase/α-Glucosidase-IN-7
0 ImagesCat. No.: HY-162036CAS No.: 1038094-94-8α-Amylase/α-Glucosidase-IN-7 (Compound 3f) is a competitive α-glucosidase and α-amylase enzyme inhibitor with IC50 values of 18.52 and 20.25 µM, respectively. α-Amylase/α-Glucosidase-IN-7 can also effectively inhibit AChE and BChE, with IC50 values of 9.25 and 10.06 µM respectively. α-Amylase/α-Glucosidase-IN-7 can be used in diabetes and Alzheimer’s research.
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AChE-IN-63
0 ImagesCat. No.: HY-158261CAS No.: 876685-78-8AChE-IN-63 (Compound 5AD) is a selective inhibitor of hAChE (IC50=0.103 μM). AChE-IN-63 also inhibits hBChE and hBACE-1 (IC50= 10 μM (hBChE); 1.342 μM (hBACE-1)). AChE-IN-63 inhibits Aβ aggregation, preventing the formation and deposition of Aβ1-42. AChE-IN-63 can effectively penetrate the blood-brain barrier and is orally effective. It is primarily used in Alzheimer's disease research.
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AChE-IN-112
0 ImagesCat. No.: HY-182333AChE-IN-112 is an acetylcholinesterase (AChE) inhibitor with an IC50 of 0.41 μM. AChE-IN-112 scavenges various reactive oxygen and reactive nitrogen species, including DPPH, ABTS, NO, hydroxyl and hydrogen peroxide free radicals. AChE-IN-112 can be used for the research of Alzheimer's disease.
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Methyl isoplatydesmine
0 ImagesCat. No.: HY-N21823CAS No.: 220961-34-2Methyl isoplatydesmine is a cholinesterase inhibitor with spasmolytic activity, with a Ki value of 30.0 μM against electric eel acetylcholinesterase and a Ki value of 19.0 μM against horse serum butyrylcholinesterase. Methyl isoplatydesmine mediates spasmolytic activity by blocking voltage-dependent calcium channels. Methyl isoplatydesmine can be used in the research of Alzheimer's disease and related dementias.
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AF03
0 ImagesCat. No.: HY-180141AF03 is a larvicide against Aedes aegypti Vector Larvae with a LC50 of 41.6 μg/mL. AF03 binds stably to the sterol carrier protein-2 (AeSCP-2) of Aedes aegypti, interfering with lipid metabolism in larvae. AF03 can increase acetylcholinesterase (AChE) activity in the zebrafish brain, slightly elevate catalase (CAT) activity in the liver and heart, and increased superoxide dismutase (SOD) activity in the brain. AF03 can be used for the research of arboviruses infection, such as Dengue.
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2-Acetoxyacorenone
0 ImagesCat. No.: HY-W750970CAS No.: 185154-95-42-Acetoxyacorenone (compound 8) is a sesquiterpenoid, which can be isolated from the rhizome of Acorus tatarinowii. 2-Acetoxyacorenone has potent AChE and β-BACE1 inhibitory activity and can be used in the study of Alzheimer's disease.
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Stacofylline hydrochloride
0 ImagesCat. No.: HY-106412ACAS No.: 138472-18-1Synonyms: S 9977Stacofylline hydrochloride (S 9977), 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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AChE-IN-108
0 ImagesCat. No.: HY-181744AChE-IN-108 is a potent mixed-type acetylcholinesterase (AChE) inhibitor with an in vitro IC50 of 0.17 nM. AChE-IN-108 acts on both free AChE and the enzyme-substrate complex to exert mixed-type inhibition. AChE-IN-108 can be used for the study of acetylcholinesterase inhibition in Alzheimer’s disease (AD).
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AChE-IN-119
0 ImagesCat. No.: HY-184796AChE-IN-119 is a selective acetylcholinesterase (AChE) inhibitor with an IC50 of 0.0641 μM and a Ki of 0.01648 μM. AChE-IN-119 exerts antioxidant effects by scavenging DPPH free radicals. AChE-IN-119 exhibits mixed-type inhibition and interacts with both the catalytic active site and the peripheral anionic site of acetylcholinesterase. AChE-IN-119 can be used for the research of Alzheimer's disease.
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AChE/BChE/MAO-A-IN-2
0 ImagesCat. No.: HY-184159AChE/BChE/MAO-A-IN-2 is an AChE, BChE, and MAO-A inhibitor with IC50 values of 104.28 nM, 23.04 nM, and 215.50 nM, respectively. AChE/BChE/MAO-A-IN-2 exhibits selective antiproliferative activity against cancer cells and low toxicity toward normal cells. AChE/BChE/MAO-A-IN-2 can be used for the research of alzheimer's disease, neuroblastoma.
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AChE/MAO-B-IN-9
0 ImagesCat. No.: HY-181861CAS No.: 2341935-88-2AChE/MAO-B-IN-9 (Compound E12) is an orally active, selective, reversible, non-competitive AChE and MAO-B inhibitor, with an IC50 of 0.156 μM against electric eel AChE. AChE/MAO-B-IN-9 inhibits Aβ40/42 fibril formation, promotes Aβ fibril depolymerization, and inhibits Tau protein fibril formation. AChE/MAO-B-IN-9 exerts antioxidant and neuroprotective effects, and improves scopolamine (HY-N0296)-induced memory impairment in mice. AChE/MAO-B-IN-9 can be used for the research of Alzheimer's disease.
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AChE-IN-88
0 ImagesCat. No.: HY-176439CAS No.: 2758789-03-4AChE-IN-88 (Compound 26) is a novel pyridazine derivative. AChE-IN-88 is an orally active multi-target ligand for Alzheimer's disease (AD) that inhibits both acetylcholinesterase (AChE) and amyloid β protein (Aβ) aggregation (pIC50: 7.16).
