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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Isatin-O
0 ImagesIsatin-O (Isatin β-oxime; Isatin 3-oxime) is an acetylcholinesterase (AChE) reactivator capable of crossing the blood-brain barrier. Isatin-O reactivates paraoxon-inhibited acetylcholinesterase in the central and peripheral nervous systems. As a glycosylation substrate, Isatin-O undergoes complete glycosylation in a Rauvolfia serpentina cell suspension culture system to form isatin-3-oxime-glucoside. Isatin-O can be used in studies related to organophosphate poisoning.
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AChE-IN-20
0 ImagesCat. No.: HY-147952CAS No.: 2428389-65-3AChE-IN-20 (compound M26) is a potent AChE inhibitor with IC50 value of 397.32 nM and with Ki value of 335.76 nM. AChE-IN-20 shows inhibition potency against hCA I , hCA II and α-GLY with IC50 values of 84.14, 69.24 and 52.08 nM and with Ki values of 97.86, 76.23 and 57.93 nM, respectively.
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Propoxur (Standard)
0 ImagesPropoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.
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sEH/AChE-IN-5
0 ImagesCat. No.: HY-183341sEH/AChE-IN-5 is a selective, orally active and brain-penetrant acetylcholinesterase (AChE) and soluble epoxide hydrolase (sEH) dual inhibitor with IC50 values of 1.7 nM and 0.7 nM. sEH/AChE-IN-5 mediates neuroprotection and anti-inflammation via reduced TNF-α, IL-1β, IL-6, iNOS. sEH/AChE-IN-5 improves Scopolamine (HY-N0296)-induced learning and memory deficits mice. sEH/AChE-IN-5 can be used for the research of Alzheimer's disease.
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2,3,9,10-Tetrahydroxyberberine bromide
0 ImagesCat. No.: HY-N11962ACAS No.: 2847856-62-42,3,9,10-Tetrahydroxyberberine bromide is an acetylcholinesterase AChE inhibitor (IC50=7.8 μM). 2,3,9,10-Tetrahydroxyberberine bromide exhibits DPPH free radical scavenging activity (IC50=43 μM) and is applicable to research related to Alzheimer's disease.
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NSC 620023 TFA
0 ImagesCat. No.: HY-181445NSC 620023 TFA is a highly selective butyrylcholinesterase (BChE) inhibitor with an IC50 of 32 nM. NSC 620023 TFA acts via π-stacking interactions with dual benzimidazole moieties and hydrophobic interactions within the BChE binding site. NSC 620023 TFA can be used for the research of alzheimer’s disease.
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Dual AChE-MAO B-IN-4
0 ImagesCat. No.: HY-158695Dual AChE-MAO B-IN-4 (compound 7) is a dual AChE/MAO-B inhibitor, with IC50 values of 261 nM and 15 nM, respectively. Dual AChE-MAO B-IN-4 protects against oxidative damage induced by H2O2 and 6-OHDA in SH-SY5Y cells. Dual AChE-MAO B-IN-4 can penetrate the central nervous system in a cell model that mimics the blood-brain barrier. Dual AChE-MAO B-IN-4 can be used in the study of neurological diseases such as Alzheimer's disease (AD).
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AChE/BChE-IN-32
0 ImagesCat. No.: HY-179711AChE/BChE-IN-32 (Compound 4a) is an AChE and BChE inhibitor, with Ki values of 2.48 and 0.696 μM respectively. AChE/BChE-IN-32 inhibits Aβ aggregation and exhibits a strong ABTS•+ scavenging ability (TEAC = 2.40). AChE/BChE-IN-32 shows significant neuroprotective activity in glutamate and hydrogen peroxide-induced oxidative stress models. AChE/BChE-IN-32 can be used for the study of Alzheimer's disease.
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Manumycin B
0 ImagesCat. No.: HY-123887CAS No.: 139023-58-8Manumycin B is an antibiobic, and exhibits antitumor activity. Manumycin B is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 15 mM.
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(Rac)-Sclerone
0 ImagesCat. No.: HY-N8547ACAS No.: 19638-58-5Synonyms: 4,5-Dihydroxytetralone; 4-Hydroxy-α-tetralone(Rac)-Sclerone is a natural product, that can be isolated from the green husk of Carya illinoinensis. (Rac)-Sclerone shows appreciable inhibition of AChE, with an IC50 of 192.65 ± 10.12 μg/mL.
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AChE/BChE-IN-35
0 ImagesCat. No.: HY-182254AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC50 of 123.66 nM, human AChE IC50 of 122.34 nM, and equine BChE IC50 of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease.
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AChE-IN-82
0 ImagesCat. No.: HY-170938AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-82 inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50s of 0.072, 9.81, 14.52, 0.024, 2.42 μM, respectively. AChE-IN-82 inhibits COX-1, COX-2 and 5-LOX with IC50s of 60.41, 0.187, 0.18 μM, respectively. AChE-IN-82 shows an excellent neuroprotective effect by significantly reducing oxidative stress induced by H2 O2.
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eeAChE-IN-1
0 ImagesCat. No.: HY-132903CAS No.: 2763366-27-2eeAChE-IN-1 is a potent eeAChE inhibitor with an IC50 value of 23 nM.
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AChE/BChE-IN-19
0 ImagesCat. No.: HY-161508CAS No.: 3036136-22-5AChE/BChE-IN-19 (Compound 12) is a nicotinic hydrazide derivative. AChE/BChE-IN-19 is a inhibitor of AChE (IC50 = 21.45 nM) and BChE (IC50 =18.42 nM). AChE/BChE-IN-19 can be used in Alzheimer's disease research.
