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 (458)
Related Products (458)
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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.
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Azamethiphos
0 ImagesAzamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders.
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Propoxur-d3
0 ImagesCat. No.: HY-B0916SCAS No.: 1219798-56-7Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). 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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AChE-IN-44
0 ImagesCat. No.: HY-156372CAS No.: 2758685-58-2AChE-IN-44 (Compound Tap4) is an AChE inhibitor. AChE-IN-44 can be converted into the thiazole salt AChE inhibitor Tat2.
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BChE-IN-3
0 ImagesCat. No.: HY-144689CAS No.: 3033413-58-7
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K203
0 ImagesCat. No.: HY-146959CAS No.: 955034-69-2K203 is a potent reactivator of tabun-inhibited AChE. K203 is a crucial antidote used for the organophosphate intoxication.
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Dihydroconiferyl dihydro-p-coumarate
0 ImagesCat. No.: HY-N21789CAS No.: 152543-09-4Dihydroconiferyl dihydro-p-coumarate is a mesophenolic acetylcholinesterase (AChE) inhibitor discovered in orchids such as Vanda roxburghii and Dendrobium nobile, with an IC50 of 118.17 μg/mL against mouse AChE. Dihydroconiferyl dihydro-p-coumarate reduces the hydrolytic activity of AChE, scavenges DPPH and hydroxyl radicals, exhibits potassium ferricyanide reducing power, reduces Mo (VI) to Mo (V), and inhibits lipid peroxidation in mouse brain homogenates. Dihydroconiferyl dihydro-p-coumarate is a key hypoglycemic compound and shows no significant cytotoxicity to human cancer cells. Dihydroconiferyl dihydro-p-coumarate can be used in research related to Alzheimer's disease and type 2 diabetes.
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AChE/BChE-IN-30
0 ImagesCat. No.: HY-175973AChE/BChE-IN-30 (Compound 3g) is a Cholinesterase dual-target competitive inhibitor. AChE/BChE-IN-30 can inhibit AChE and BChE with IC50 values of 0.338 and 2.087 μM and Ki values of 0.045 and 0.789 μM. AChE/BChE-IN-30 can be used for the research of neurological disease, such as Alzheimer's disease.
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ChEs/MAOs-IN-2
0 ImagesCat. No.: HY-158092CAS No.: 693268-77-8ChEs/MAOs-IN-2 (compound a11) is a cholinesterases and monoamine oxidases inhibitor with IC50 values of 0.10, 0.20, 0.30, 0.40 µM for MAO-A, MAO-B, AChE, and BChE, respectively. ChEs/MAOs-IN-2 has the potential for the research of Alzheimer's disease.
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JDS364
0 ImagesCat. No.: HY-184279CAS No.: 2072857-15-7JDS364 is a blood-brain barrier-permeable human acetylcholinesterase (hAChE) reactivator with an IC50 of 8.6 μM. JDS364 achieves rapid systemic exposure in mice and acts as a protective agent when used in combination with Atropine (HY-B1205). JDS364 can be used in studies on organophosphate nerve agent poisoning and organophosphate pesticide poisoning.
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Asoxime dimesylate
0 ImagesCat. No.: HY-106901BCAS No.: 144252-71-1Synonyms: HI-6 dimesylateAsoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system.
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Isogarcinol
0 ImagesCat. No.: HY-127087CAS No.: 71117-97-0Synonyms: Cambogin
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BChE-IN-36
0 ImagesCat. No.: HY-169163hBChE-IN-4 (compound 40) is a potent hCA activator and BChE inhibitor with KA values of 266, 76.9, 918, 893, 98.0 nM for hCA I, hCA II, hCA IV, hCA VB, hCA VII, IC50 values of 72.1, 4.2 nM for eeAChE, eqBChE, respectively. hBChE-IN-4 shows no cytotoxicity. hBChE-IN-4 shows potent procognitive effects. hBChE-IN-4 has the potential for the research of neurodegenerative diseases and other neuropsychiatric disorders.
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Scutellarein 4'-methyl ether 7-O-glucuronide
0 ImagesCat. No.: HY-N17775CAS No.: 64924-06-7Synonyms: ClerodendrosideScutellarein 4'-methyl ether 7-O-glucuronide (Clerodendroside) is a flavonoid inhibitor of acetylcholinesterase (AChE) (IC50=1 mg/mL). Scutellarein 4'-methyl ether 7-O-glucuronide can be isolated from Plectranthus barbatus. It also possesses antioxidant activity and can be used in research on neurological diseases such as Alzheimer's disease.
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Neuroprotective agent 15
0 ImagesCat. No.: HY-178943CAS No.: 2476614-40-9Neuroprotective agent 15 (Compound 3e) is a neuroprotective agent. Neuroprotective agent 15 is a selective butyrylcholinesterase (BChE) inhibitor, with IC50 values of 2.6 and 114.3 μM for BChE and AChE respectively. Neuroprotective agent 15 has cannabinoid CB2 receptor (CB2 receptor) agonistic activity. Neuroprotective agent 15 can reduce cell death, LDH release and Caspase-3/7 activity, and inhibit apoptosis. Neuroprotective agent 15 can reduce the formation of superoxide free radicals, maintain cell morphology, and significantly lower oxidative stress levels. Neuroprotective agent 15 can be used in the research of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.
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MAO-B-IN-56
0 ImagesCat. No.: HY-182786MAO-B-IN-56 is a multi-target-directed ligand with AChE, BChE, MAO-B, and BACE1 inhibitory activity, with IC50 values of 0.35 μM, 3.22 μM, 0.14 μM, and 3.85 μM respectively, and shows selectivity for AChE over BChE and MAO-B over MAO-A.MAO-B-IN-56 reduces amyloid-beta production, reduces paw edema, improves spatial memory, and enhances Alzheimer's disease hallmarks and associated histopathological alterations.MAO-B-IN-56 can be used for the research of alzheimer's disease.
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Stemoninine
0 ImagesCat. No.: HY-134006CAS No.: 69772-72-1Stemoninine is a lycoris alkaloid that can be used as an antitussive. Stemoninine has significant inhibitory activity against human acetylcholinesterase (AChE) (IC50=5.52 μM).
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AChE/BuChE-IN-5
0 ImagesCat. No.: HY-163537AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research.
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Multitarget AD-IN-4
0 ImagesCat. No.: HY-180891Multitarget AD-IN-4 (compound IIIj) is a multitarget-directed ligand (MTDL), with the ability to simultaneously inhibit ChE enzymes (EeAChE IC50 = 0.157 μM, eqBuChE IC50 = 0.147 μM, hAChE IC50 = 1.551 μM, hBuChE IC50 = 2.152 μM), exhibit antioxidant activity, provide neuroprotection, and inhibit calcium channels (Ca2+ channel blockade: IC50 = 30.59 μM). Multitarget AD-IN-4 reverses Scopolamine (HY-N0296)-induced amnesia in a mouse model. Multitarget AD-IN-4 can be used for Alzheimer’s disease (AD) research.
