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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AJ-4
0 ImagesCat. No.: HY-184742AJ-4 is an orally active, blood-brain barrier-permeable GSK-3β/AChE inhibitor, with an IC50 of 4.7 nM against GSK-3β and 2.97 μM against AChE. AJ-4 increases the level of phosphorylated GSK-3β and reduces the expression of Amyloid-β and phosphorylated Tau. AJ-4 improves scopolamine-induced learning and memory impairment and alleviates hippocampal neuron damage in AD mice. AJ-4 can be used for the research of Alzheimer's disease.
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AChE/BChE-IN-12
0 ImagesCat. No.: HY-149211AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.
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ω-Hydroxydigitoemodin
0 ImagesCat. No.: HY-N17416CAS No.: 159898-12-1ω-Hydroxydigitoemodin is an anthraquinone derivative with anti-acetylcholinesterase activity, found in the marine fungus Trichoderma harzianum XS-20090075.
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AChE-IN-105
0 ImagesCat. No.: HY-180946CAS No.: 2678601-07-3AChE-IN-105 (Compound C5) is a potent, mixed AChE inhibitor with an IC50 of 5.02 μM. AChE-IN-105 scavenges ROS, decreases Hydrogen peroxide-induced Caspase-3 activation, reduces activity of the Nrf2-ARE pathway. AChE-IN-105 prevents memory impairments in the Scopolamine (HY-N0296)-induced cognitive dysfunction zebrafish model. AChE-IN-105 has potent antioxidant activity. AChE-IN-105 can be used in the research of Alzheimer's disease.
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Plasiaticine B
0 ImagesCat. No.: HY-N16645CAS No.: 1528768-32-2Plasiaticine B (Compound 2) is an indole alkaloid found in Plantago asiatica. Plasiaticine B shows no significant cytotoxicity to HL-60, A-549 and MCF-7 cells with IC50 >40 μM. Plasiaticine B shows no significant inhibitory effect on AChE, with an inhibition rate <60%.
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hCA I-IN-4
0 ImagesCat. No.: HY-169962CAS No.: 3054159-56-4hCA I-IN-4 (Compound 14) is the inhibitor for carbonic anhydrase and cholinesterase, that inhibits hCA I, hCA II, AChE, and BChE with Ki of 29.94 nM, 17.72 nM, 21.21 nM, and 7.65 nMrespectively. hCA I-IN-4 exhibits cytotoxicity in BT-549 with IC50 of 16.59 μM.
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hAChE/hBACE-1-IN-4
0 ImagesCat. No.: HY-161512CAS No.: 229476-71-5hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research.
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AChE-IN-19
0 ImagesCat. No.: HY-147938CAS No.: 2742707-36-2AChE-IN-19 (compound A15) is a highly potent AChE inhibitor with an IC50 value of 0.56 μM, also inhibits Aβ aggregation. AChE-IN-19 has potent neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE-IN-19 can be used for researching Alzheimer's disease.
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EQ-04
0 ImagesCat. No.: HY-179621EQ-04 is a highly selective positive allosteric modulator (PAM) of α7 nAChR. EQ-04 has no direct inhibitory activity on AChE and BChE. EQ-04 inhibits Aβ aggregation. EQ-04 has safe cytotoxicity and potent neuroprotective activity. EQ-04 can be used for the study of Alzheimer's disease.
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Keap1/Nrf2/ARE activator 2
0 ImagesCat. No.: HY-180155CAS No.: 3105470-83-2Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease.
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KBR 2822
0 ImagesCat. No.: HY-118222CAS No.: 126988-60-1KBR 2822 is an inhibitor of neurological target esterase (NTE) and has an inhibitory effect on AChE. KBR 2822 can aggravate neurological damage under certain conditions, but does not cause neurological disease when used alone in the absence of direct neurotoxicity or biochemical damage.
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AChE-IN-8
0 ImagesCat. No.: HY-115919CAS No.: 2919335-82-1AChE-IN-8 (Compound 19) is a potent inhibitor of AChE with an IC50 of 1.95 μM. AChE-IN-8 has the potential for the research of Alzheimer's disease.
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CUR-IPA
0 ImagesCat. No.: HY-172219CUR-IPA is a cholinesterase inhibitor, with IC50 of 5.99, 59.30, and 60.66 μM for eAChE (electric eel), hAChE (human), and hBChE (human), respectively. CUR-IPA can scavenge free radicals and has antioxidant activity. CUR-IPA can be used in the research of cognitive dysfunction.
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AChE/BChE-IN-25
0 ImagesCat. No.: HY-168731AChE/BChE-IN-25 (Compound 6e) is the orally active inhibitor for hAChE and eqBChE with IC50 of 7.9 nM and 0.79 nM. AChE/BChE-IN-25 exhibits antioxidant activity, that scavenges free radical with IC50 of 22.91 μM. AChE/BChE-IN-25 exhibits neuroprotective effects by reducing mitochondrial and cellular oxidative stress in the Drosophila Alzheimer's disease model. AChE/BChE-IN-25 ameliorates Scopolamine (HY-N0296)-induced spatial and cognitive memory impairment in mouse model.
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AChE/BChE-IN-27
0 ImagesCat. No.: HY-174399AChE/BChE-IN-27 is a blood-brain barrier-permeable mixed inhibitor (Pe = 4.12) of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively. AChE/BChE-IN-27 has potent antioxidant activity with an IC50 value of 6.32 μM in the DPPH (HY-112053) assay and also exhibits potent in vitro antioxidant activity. AChE/BChE-IN-27 exhibits metal chelating properties. AChE/BChE-IN-27 has neuroprotective potential against oxidative stress. AChE/BChE-IN-27 significantly reduces intracellular reactive oxygen species (ROS). In in vivo experiments, AChE/BChE-IN-27 effectively restored AChE and BChE levels, improved cognition, and can be used for Alzheimer's disease (AD).
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Dual AChE-MAO B-IN-3
0 ImagesCat. No.: HY-151885Dual AChE-MAO B-IN-3 (compound C10) is a potent dual AChE/MAO-B inhibitior, with IC50 values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site of AChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research.
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AChE/BChE-IN-33
0 ImagesCat. No.: HY-180819AChE/BChE-IN-33 (Compound 3N) is a dual-target inhibitor of AChE and BChE, with IC50 values of 12.81 and 44.54 nM respectively. AChE/BChE-IN-33 exhibits selective cytotoxicity against SH-SY5Y cells. AChE/BChE-IN-33 can be used for the study of Alzheimer's disease and neuroblastoma.
