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

Cholinesterase (ChE)

Cholinesterase (ChE)

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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.

Cholinesterase (ChE) Isoform Specific Products:

Cholinesterase (ChE) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W272207
    AChE/BChE-IN-31
    		Inhibitor
    AChE/BChE-IN-31 (Compound 3c) is a cholinesterase inhibitor. AChE/BChE-IN-31 exhibits certain inhibitory activity against hAChE and eqBChE. AChE/BChE-IN-31 also possesses antioxidant properties with an IC50 value of 105.04 μM against DPPH. AChE/BChE-IN-31 can be used in the research of diseases such as Alzheimer’s disease.
    AChE/BChE-IN-31
  • HY-156754
    3β-Hydroxy-lup-20(29)-en-16-one
    		Inhibitor
    3β-Hydroxy-lup-20(29)-en-16-one (compound 9) is a dual inhibitor of AChE and BChE, with selectivity for BChE (IC50: 28.9 μM).
    3β-Hydroxy-lup-20(29)-en-16-one
  • HY-159880
    AChE/BChE-IN-24
    		Inhibitor
    AChE/BChE-IN-24 (compound 5k) is a neuroprotective agent through cholinesterase inhibition. AChE/BChE-IN-24 inhibits AChE and BChE with IC50 values of 16.38 μM and 10.44 μM, respectively.
    AChE/BChE-IN-24
  • HY-152114
    AChE/BChE/MAO-B-IN-4
    		Inhibitor
    AChE/BChE/MAO-B-IN-4, an indan-1-one derivative, is a potent MAO-B inhibitor with an IC50 of 0.0393 μM for human MAO-B. AChE/BChE/MAO-B-IN-4 is a potent AChE and BChE enzyme inhibitor, with IC50s of 0.0458 μM and 0.075 μM for human AChE and BChE enzyme, respectively. AChE/BChE/MAO-B-IN-4 shows significant antioxidant activity and prevent β-amyloid plaque aggregation. AChE/BChE/MAO-B-IN-4 has the potential for Alzheimer's disease (AD) research.
    AChE/BChE/MAO-B-IN-4
  • HY-163514
    hAChE-IN-8
    		Inhibitor
    hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research.
    hAChE-IN-8
  • HY-N17425
    Lakoochin C
    		Inhibitor
    Lakoochin C is an inhibitor of acetylcholinesterase (AChE) (IC50 = 61.86 μM) and butyrylcholinesterase (BChE) (IC50 = 47.21 μM). Lakoochin C may be used in research related to Alzheimer's disease.
    Lakoochin C
  • HY-155365
    hAChE-IN-5
    		Inhibitor
    hAChE-IN-5 (compound 49) is a potent hAChE and hBuChE inhibitor with IC50 values of 0.17 μM and 0.17 μM, respectively. hAChE-IN-5 shows potent GSK3β inhibition with an IC50 value of 0.21 μM. hAChE-IN-5 is used as tau protein aggregation and Aβ1-42 self-aggregation inhibitor. hAChE-IN-5 can bind virtually with the PAS affecting Aβ aggregation, thus preventing Aβ-dependent neurotoxicity. hAChE-IN-5 can penetrate BBB and has the potential for multi-targeted anti-Alzheimer's agents research.
    hAChE-IN-5
  • HY-49373
    AChE-IN-64
    		Inhibitor
    AChE-IN-64 (compound C4) is an AChE inhibitor (IC50: 36.9 µM), and can be used for cognitive disorders research.
    AChE-IN-64
  • HY-162681
    eeAChE-IN-3
    		Inhibitor
    eeAChE-IN-3 (compound YS3g) is an orally active, potent EeAChE and IL-6 inhibitor with IC50s of 0.54 μM, 0.49 μM, 8.54 μM and 0.57 μM for EeAChE, RatAChE, RatBuChE and IL-6, respectively. eeAChE-IN-3 improves STZ (HY-13753) (Streptozotocin; HY-13753)-induced learning and memory impairment in mice. eeAChE-IN-3 has the potential for Alzheimer's disease (AD) research.
    eeAChE-IN-3
  • HY-W856819
    Eseroline
    		Inhibitor
    Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease.
    Eseroline
  • HY-180358
    Gallamine
    		Inhibitor
    Gallamine is an allosteric, selective muscarinic M2 acetylcholine receptor antagonist (EC50: 130 nM for [3H]NMS dissociation from porcine muscarinic M2 receptors). Gallamine is also an acetylcholinesterase inhibitor (IC50s : 1070 μM, 1480 μM, 235  μM for EeAChE, hAChE, hBChE, respectively (in the absence of MeCN)). Gallamine increases free norepinephrine levels. Gallamine can be used as a muscle relaxant.
    Gallamine
  • HY-161156
    BChE-IN-26
    		Inhibitor
    BChE-IN-26 (Compound 7b) is a selective AChE and BChE inhibitor with Ki value of 35 μM and 1.6 μM. BChE-IN-26 has cytotoxicity to human neuroblastoma (SH-SY5Y) cell line. BChE-IN-26 can be used for the research of Alzheimer’s disease.
    BChE-IN-26
  • HY-N7480A
    Quinolactacin A1
    		Inhibitor
    Quinolactacin A1 is a potent acetylcholinesterase (AChE) inhibitor from solid state fermentation of Penicillium citrinum 90648. Quinolactacin A1 can be used for the research of Alzheimer disease.
    Quinolactacin A1
  • HY-147954
    α-Glycosidase-IN-1
    		Inhibitor
    α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.
    α-Glycosidase-IN-1
  • HY-120131
    Cyanofenphos
    		Inhibitor
    Cyanofenphos is an orally active organophosphate insecticide and brain AChE inhibitor with neurotoxicity. Cyanofenphos induces delayed neurotoxicity such as ataxia and paralysis. Cyanofenphos also causes symptoms including somnolence, reduced feed intake and weight loss in hens. Cyanofenphos has a unique self-antagonistic effect: repeated low-dose pre-treatment not only reduces subsequent acute toxicity, but also exacerbates delayed neurotoxicity and attenuates enzyme inhibition, with the protective effect peaking at 24 h after the last pre-treatment. Cyanofenphos is commonly used in studies related to delayed neurotoxicity.
    Cyanofenphos
  • HY-162639
    α-Glucosidase-IN-68
    		Inhibitor
    α-Glucosidase-IN-68 (Compound 2) is an inhibitor for α-Glucosidase, AChE, and BChE, with IC50 of 0.251, 0.774 and 0.793 μM, respectively. α-Glucosidase-IN-68 exhibits antioxidant efficacy, with IC50 of 0.69 μM and 0.02 μM, in DPPH and ABTS experiments. α-Glucosidase-IN-68 exhibits antidiabetic effect in Streptozotocin (HY-13753)-induced diabetic rat models.
    α-Glucosidase-IN-68
  • HY-153432
    TRV-7019
    		99.64%
    TRV-7019 is a BBB-penetrable radioligand for brain imaging that target butyrylcholinesterase. TRV-7019 can be used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity.
    TRV-7019
  • HY-W746884
    2-Methyl-2-butenyl (E)-Caffeate
    		Inhibitor
    2-Methyl-2-butenyl (E)-Caffeate is a type of caffeic acid ester compound. The petroleum ether and chloroform extracts containing 2-Methyl-2-butenyl (E)-Caffeate have inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The ether extract containing 2-Methyl-2-butenyl (E)-Caffeate exhibits strong antioxidant properties. 2-Methyl-2-butenyl (E)-Caffeate can be used in the research of Alzheimer's disease.
    2-Methyl-2-butenyl (E)-Caffeate
  • HY-147880
    BChE-IN-9
    		Inhibitor
    BChE-IN-9 (Azepano-11-deoxo-glycyrrhetol) is a mixed type BChE inhibitor with a Ki of 0.21 µM.
    BChE-IN-9
  • HY-19689
    Ipidacrine hydrochloride
    		Inhibitor
    Ipidacrine (NIK-247; Amiridine) hydrochloride is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine hydrochloride has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine hydrochloride is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine hydrochloride is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine hydrochloride is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases.
    Ipidacrine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Cholinesterase (ChE) Isoform Comparison

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