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-W003576R
    ACHE-IN-38 hydrochloride (Standard)
    		Inhibitor
    ACHE-IN-38 (hydrochloride) (Standard) is the analytical standard of ACHE-IN-38 (hydrochloride). This product is intended for research and analytical applications. ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission.
    ACHE-IN-38 hydrochloride (Standard)
  • HY-151389
    BChE-IN-14
    BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease.
    BChE-IN-14
  • HY-169470
    Pridinol hydrochloride
    		Inhibitor
    Pridinol hydrochloride is the hydrochloride salt form of Pridinol (HY-B1343A). Pridinol hydrochloride is an orally active anticholinergic agent, and acts as muscle relaxant.
    Pridinol hydrochloride
  • HY-B1738B
    Pralidoxime methanesulfonate
    		Activator
    Pralidoxime methanesulfonate is a potent reactivator of acetylcholinesterase (AChE). Pralidoxime methanesulfonate reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime methanesulfonate is an antidote for organophosphate poisoning.
    Pralidoxime methanesulfonate
  • HY-180892
    Multi-kinase-IN-10
    		Inhibitor
    Multi-kinase-IN-10 (Compound IIIk) is a multi-kinase inhibitor. Multi-kinase-IN-10 exhibits significant calcium channel blocking activity, with its IC50 being 26.67 μM. Multi-kinase-IN-10 is a potent dual cholinesterase inhibitor, with its IC50 values for hAChE and hBuChE being 0.304 μM and 1.033 μM respectively. Multi-kinase-IN-10 has antioxidant and neuroprotective activities, and shows significant anti-amnesia activity. Multi-kinase-IN-10 can be used for research on Alzheimer's disease.
    Multi-kinase-IN-10
  • HY-147962
    AChE/HDAC-IN-1
    		Inhibitor
    COX-2-IN-23 (compound A10) is a potent both AChE and HDAC inhibitor with IC50 values of 0.12 and 0.23 nM. COX-2-IN-23 exhibits antioxidant activity and metal chelating properties. COX-2-IN-23 can be used in alzheimer's disease research.
    AChE/HDAC-IN-1
  • HY-14795
    Mimopezil
    		Inhibitor
    Mimopezil (ZT-1) is an cholinesterase (ChE) inhibitor that rapidly degrades into the active metabolite Huperzine A (HY-17388) in water or aqueous organic solvents. After oral administration, Mimopezil is rapidly absorbed but has low bioavailability (0.37%) in rats. However, after metabolism, it is converted into Huperzine A, which accumulates in the blood and exhibits strong activity. Following intravenous administration, Mimopezil reaches higher blood concentrations and is also rapidly metabolized into Huperzine A.
    Mimopezil
  • HY-101981S3
    Uridine 5'-monophosphate-13C9,15N2 dilithium
    		Activator
    Uridine 5'-monophosphate-13C9,15N2 (5'- Uridylic acid-13C9,15N2) dilithium is 13C and 15N-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea.
    Uridine 5'-monophosphate-<sup>13</sup>C<sub>9</sub>,<sup>15</sup>N<sub>2</sub> dilithium
  • HY-183949
    Insecticidal agent 33
    		Inhibitor
    Insecticidal agent 33 is an AChE inhibitor with nematicidal activity. Insecticidal agent 33 impairs locomotor activity of Caenorhabditis elegans, and induces oxidative damage in Caenorhabditis elegans, including elevated reactive oxygen species (ROS) levels, lipofuscin accumulation, lipid deposition, and disrupted cellular homeostasis. Insecticidal agent 33 can be used for the research of plant-parasitic nematode infection.
    Insecticidal agent 33
  • HY-N0528R
    Linarin (Standard)
    		Inhibitor
    Linarin (Standard) is the analytical standard of Linarin. This product is intended for research and analytical applications. Linarin (Buddleoside) is an orally active and selective inhibitor of acetylcholinesterase (AChE). Linarin has many activities, such as anti-inflammatory, antioxidant, sleep aid and sedation, bone differentiation, anti-tumor, antibacterial and antiviral. Linarin can be used to study diseases such as the nervous system, osteoporosis and cancer.
    Linarin (Standard)
  • HY-183760
    AChE/BChE-IN-37
    		Inhibitor
    AChE/BChE-IN-37 is a blood-brain barrier-permeable AChE/BChE inhibitor, with an IC50 of 73.65 μM against electric eel-derived AChE and an IC50 of 82.93 μM against horse-derived BChE. AChE/BChE-IN-37 exhibits chelating activity towards Cu2+, Ca2+, Mg2+, Fe2+ and Zn2+. AChE/BChE-IN-37 interacts with HSP90AA1 and GSK-3β. AChE/BChE-IN-37 inhibits the self-induced aggregation of Aβ1-42. AChE/BChE-IN-37 suppresses LPS-induced NO production in cells. AChE/BChE-IN-37 can be used in research related to Alzheimer's disease and inflammatory diseases.
    AChE/BChE-IN-37
  • HY-N10032
    (3β,5α,6α,16β)-8,14-Didehydrocevane-3,6,16,20-tetrol
    		Inhibitor
    (3β,5α,6α,16β)-8,14-Didehydrocevane-3,6,16,20-tetrol (compound 3) is an inhibitor targeting acetylcholinesterase (AChE). At a concentration of 100 μg/mL, (3β,5α,6α,16β)-8,14-Didehydrocevane-3,6,16,20-tetrol exhibits an in vitro inhibition rate of 12% against AChE.
    (3β,5α,6α,16β)-8,14-Didehydrocevane-3,6,16,20-tetrol
  • HY-159943
    ROS151
    		Inhibitor
    ROS151 is an AChE inhibitor, with IC50s of 14 nM (hAChE), 1.68 μM (eqBChE), 8.17 μM (hFAAH) respectively. ROS151 is also a chelator of Fe3+ and Cu2+. ROS151 can be used for research of Alzheimer's disease.
    ROS151
  • HY-178750
    AChE-IN-96
    		Inhibitor
    AChE-IN-96 (Compound 8a) is an AChE inhibitor, with an IC50 of 0.697 μM. AChE-IN-96 can be used for the study of neurodegenerative diseases such as Alzheimer's disease (AD).
    AChE-IN-96
  • HY-146142
    AChE/BuChE-IN-2
    		Inhibitor
    AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB.
    AChE/BuChE-IN-2
  • HY-N16715
    Monardic acid A
    		Inhibitor
    Monardic acid A is a selective inhibitor of AChE, with an IC50 of 53.1 μM against AChE from electric eel. Monardic acid A shows weak inhibitory activity against human erythrocyte AChE (IC50 >100 μM) and has no significant inhibitory effect on BChE. Monardic acid A reduces acetylcholine breakdown by inhibiting AChE activity, and also exhibits inhibitory activity against histamine release and hyaluronidase, thus exerting anti-inflammatory and neurotransmitter regulatory effects. Monardic acid A can be isolated from lungwort (Pulmonaria officinalis) and thyme (Thymus gobicus), and is mainly used in the development of anti-inflammatory drugs and drugs related to neurodegenerative diseases.
    Monardic acid A
  • HY-146383
    H3R antagonist 2
    		Inhibitor
    H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB.
    H3R antagonist 2
  • HY-136813
    Multitarget AD inhibitor-1
    		Inhibitor
    Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research.
    Multitarget AD inhibitor-1
  • HY-181161
    AChE-IN-107
    		Inhibitor
    AChE-IN-107 is a selective acetylcholinesterase (AChE) inhibitor with an IC50 of 0.22 μM and a Ki of 0.207 μM. AChE-IN-107 shows no inhibitory effect on equine serum BChE at 10 μM. AChE-IN-107 exhibits mixed-type inhibition of electric eel acetylcholinesterase, binding to both free enzyme and enzyme-substrate complex. AChE-IN-107 acts as a cytotoxin, reduces cell viability in hepatocellular carcinoma HepG2 cells.AChE-IN-107 can be used for the research of alzheimer's disease.
    AChE-IN-107
  • HY-B1239A
    Drofenine
    		Inhibitor
    Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.
    Drofenine
Cat. No. Product Name / Synonyms Application Reactivity
Cholinesterase (ChE) Isoform Comparison

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