1. Signaling Pathways
  2. Neuronal Signaling
  3. Cholinesterase (ChE)

Cholinesterase (ChE)

Cholinesterase (ChE) is a family of enzymes present in the central nervous system, particularly in nervous tissue, muscle and red cells, which catalyze the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation. It is one of many important enzymes needed for the proper functioning of the nervous systems of humans.

There are two types: acetylcholinesterase (AChE, acetylcholine hydrolase) and butyrylcholinesterase (BChE, acylcholine acylhydrolase), also known as nonspecific cholinesterase or pseudocholinesterase. AChE is primarily found in the blood on red blood cell membranes, in neuromuscular junctions, and in neural synapses, while BChE is produced in the liver and found primarily in plasma. The difference between the two types of cholinesterase is their relative preferences for substrates: AChE hydrolyzes acetylcholine faster while BChE hydrolyzes butyrylcholine faster.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-147659
    AChE/BChE/BACE-1-IN-2
    Inhibitor
    AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-2 has remarkable antioxidant potential.
    AChE/BChE/BACE-1-IN-2
  • HY-N10487
    Bleformin A
    Inhibitor
    Bleformin A is a potent BChE inhibitor with an IC50 value of 5.2 μM. Bleformin A is a nature product that could be isolated from Bletilla striata. Bleformin A can be used for research of Alzheimer's disease (AD).
    Bleformin A
  • HY-170561
    AChE/BuChE-IN-6
    Inhibitor
    AChE/BuChE-IN-6 (Compound 11f) is an inhibitor of AChE and BuChE, with IC50 values of 1.24 and 1.85 μg/mL, respectively. AChE/BuChE-IN-6 also exhibits strong DPPH free radical scavenging activity (IC50 = 3.15 μg/mL). In vivo toxicity studies indicate that AChE/BuChE-IN-6 is safe, showing no significant differences in blood and biochemical markers compared to the control group after long-term administration, and no abnormalities were observed in liver and kidney tissues. AChE/BuChE-IN-6 holds promise for research into Alzheimer's disease.
    AChE/BuChE-IN-6
  • HY-159888
    SON38
    Inhibitor
    SON38 is a copper chelator capable of chelating divalent copper. SON38 can inhibit the activity of cholinesterases and has potential applications in Alzheimer's disease research.
    SON38
  • HY-146312
    AChE/BChE/MAO-B-IN-1
    Inhibitor 99.57%
    AChE/BChE/MAO-B-IN-1 is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity.
    AChE/BChE/MAO-B-IN-1
  • HY-162606
    MAO-A/B-IN-3
    Inhibitor
    MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases.
    MAO-A/B-IN-3
  • HY-131252
    Dihydro Donepezil
    Inhibitor
    Dihydro Donepezil (Dihydro E2020) is a metabolite of Donepezil. Donepezil is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively.
    Dihydro Donepezil
  • HY-155822
    TZ3O
    Inhibitor 98.17%
    TZ3O (compound TZ30) is an anticholinergic agent with neuroprotective effects. TZ3O (2 mg/kg, 4 mg/kg) can improve memory impairment and cognitive decline in rats in the Scopolamine (HY-N0296)-induced Alzheimer-type model. TZ3O could be used in Alzheimer’s research.
    TZ3O
  • HY-163126
    AChE-IN-52
    Inhibitor
    AChE-IN-52 (compound A6) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-52 shows antitumor efficacy, especially against breast cancer MCF-7 cells. AChE-IN-52 significantly disrupts the amino acid metabolism and inhibits migration of MCF-7. AChE-IN-52 plays anticancer role by regulating Best1 and HIST1H2BJ.
    AChE-IN-52
  • HY-N0810R
    Timosaponin AIII (Standard)
    Timosaponin AIII (Standard) is the analytical standard of Timosaponin AIII. This product is intended for research and analytical applications. Timosaponin AIII could inhibit acetylcholinesterase (AChE) activity, with an IC50 of 35.4 μM.
    Timosaponin AIII (Standard)
  • HY-12153
    JNJ-1930942
    Modulator
    JNJ-1930942 is a selective and blood-brain barrier (BBB) penetrant α(7) nAChR positive allosteric modulator.JNJ-1930942 enhances the Choline (HY-B0282)-evoked rise in intracellular Ca2+ levels and neurotransmission at hippocampal dentate gyrus synapses. JNJ-1930942 reverses the naturally occurring sensory gating deficit in DBA/2 mice.
    JNJ-1930942
  • HY-N0286S
    Isoimperatorin-d6
    Inhibitor
    Isoimperatorin-d6 is the deuterium-labeled Isoimperatorin (HY-N0286).
    Isoimperatorin-d<sub>6</sub>
  • HY-147870
    COX-2-IN-22
    Inhibitor
    COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB.
    COX-2-IN-22
  • HY-162145
    AChE-IN-54
    Inhibitor
    AChE-IN-54 (compound 3c) is an inhibitor of acetylcholinesterase (AChE) and has anti-lipid oxidation activity.
    AChE-IN-54
  • HY-152232
    BChE-IN-15
    Inhibitor
    BChE-IN-15 (Compound 6) is a pseudo-irreversible and covalent BChE inhibitor with an IC50 of 1.76 nM against hBChE .
    BChE-IN-15
  • HY-W165085
    1,10-Bis(pyridinium)decane
    Inhibitor 99.66%
    1,10-Bis(pyridinium)decane (Decamethylenebispyridinium dibromide), a biscationic compound, is an acetylcholinesterase (AchE) inhibitor with an IC50 of 25.8 nM.
    1,10-Bis(pyridinium)decane
  • HY-121143
    Bis-Q
    Agonist
    Bis-Q is an acetylcholine (ACh) agonist that targets voltage-clamped muscle fibers of the fish Xenomystus nigris. Bis-Q exists in two forms: cis-Bis-Q (non-agonist) and trans-Bis-Q (agonist). Photoisomerization converts cis-Bis-Q to trans-Bis-Q, which induces agonist-induced currents. Channels activated by trans-Bis-Q and ACh have similar conductances and open times. Flashes increase the ratio of trans-Bis-Q to cis-Bis-Q until light equilibrium is reached. Further flashes transiently increase agonist-induced currents, indicating binding of trans-Bis-Q to desensitized receptors. Higher concentrations of cis-Bis-Q produce larger agonist-induced currents that decay exponentially..
    Bis-Q
  • HY-B1277A
    Trihexyphenidyl
    Antagonist
    Trihexyphenidyl is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research.
    Trihexyphenidyl
  • HY-151386
    BChE-IN-13
    Inhibitor
    BChE-IN-13 (Compound 17c) is an orally active, potent and selective Butyrylcholinesterase (BChE) inhibitor with IC50s of 0.22 and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 can improve memory and cognitive impairments, and be used in Alzheimer’s disease (AD) research.
    BChE-IN-13
  • HY-157978
    AChE-IN-59
    Inhibitor
    AChE-IN-59 (compounds 3b) is an AChE inhibitor, with an IC50 value of 0.05 μM. AChE-IN-59 can inhibit the aggregation of Aβ1-42, protect nerve cells and penetrate the blood-brain barrier well. AChE-IN-59 can be used for the research of Alzheimer's disease (AD).
    AChE-IN-59
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