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-151436
    ZLMT-12
    Inhibitor
    ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
    ZLMT-12
  • HY-146679
    HDAC6-IN-6
    Inhibitor
    HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against 1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity.
    HDAC6-IN-6
  • HY-136610S
    Chlorpyrifos-oxon-d10
    Inhibitor
    Chlorpyrifos-oxon-d10 is the deuterium labeled Chlorpyrifos-oxon. Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that potently inhibits AChE. Chlorpyrifos-oxon can induce cross-linking between subunits of tubulin and disrupt microtubule function.
    Chlorpyrifos-oxon-d<sub>10</sub>
  • HY-B2015S
    Carbosulfan-d18
    Inhibitor
    Carbosulfan-d18 is the deuterium labeled Carbosulfan. Carbosulfan is an orally active AChE inhibitor that hydrolyzes to Carbofuran in organisms to exert insecticidal effects. Carbosulfan exhibits broad-spectrum insecticidal activity, and it also induces severe oxidative stress by enhancing lipid peroxidation and impairing the antioxidant defense system. Carbosulfan causes reproductive toxicity in male rats and developmental disorders in their offspring. Carbosulfan shows persistence in paddy field environments and potential hazards to non-target organisms, and it is commonly used in studies related to reproductive toxicity and environmental risk assessment.
    Carbosulfan-d<sub>18</sub>
  • HY-163909
    AChE-IN-72
    Inhibitor
    AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 0.59 μM. AChE-IN-72 inhibits BChE with an IC50 of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC50 of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable.
    AChE-IN-72
  • HY-N2034
    Dehydrodicentrine
    Inhibitor
    Dehydrodicentrine is an aporphine alkaloid can be isolated from the root of S. epigaea and has inhibitory effect on acetylcholinesterase (AChE) with an IC50 value of 2.98 μM.
    Dehydrodicentrine
  • HY-106525
    Aclatonium napadisylate
    Agonist
    Aclatonium napadisylate is a cholinergic agonist. Aclatonium napadisylate can increase amylase release and Ca2+ efflux. Aclatonium napadisylate can stimulate pancreatic exocrine secretion and increase motility and peristalsis of the gastrointestinal tract. Aclatonium napadisylate can be used for the research of gastrointestinal disorders.
    Aclatonium napadisylate
  • HY-155366
    hAChE-IN-6
    Inhibitor
    hAChE-IN-6 (compound 51) is a brain penetrant AChE inhibitor with an IC50 of 0.16 μM. hAChE-IN-6 also inhibits hBuChE and GSK3β with IC50 values of 0.69 μM and 0.26 μM, respectively. hAChE-IN-6 inhibits tau protein and Aβ1-42 self-aggregation, and can be used for Alzheimer's disease (AD) research.
    hAChE-IN-6
  • HY-149300
    SB-1436
    Inhibitor
    SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC50s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with Kis of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research.
    SB-1436
  • HY-148108
    AChE-IN-27
    Inhibitor 98.27%
    AChE-IN-27 (compound 8c) is an AChE inhibitor (IC50=0.19 µM). AChE-IN-27 can be used in studies of neurological diseases such as alzheimer's disease, dementia, ataxia and myasthenia gravis.
    AChE-IN-27
  • HY-149473
    AChE-IN-39
    Inhibitor
    AChE-IN-39 (Compound 7c) is an AChE inhibitor (IC50: 0.058 μM). AChE-IN-39 has DPPH scavenging activity. AChE-IN-39 improves the cognitive impairment in AlCl3-induced amnesia animal model. AChE-IN-39 can be used for research of Alzheimer's disease.
    AChE-IN-39
  • HY-19478
    TAK-802
    Inhibitor
    TAK-802 is an orally active and potent acetylcholinesterase inhibitor. TAK-802’s distribution in red blood cells has a significant concentration dependence, with the distribution ratio decreasing as the concentration increases. TAK-802 exhibits significant nonlinear pharmacokinetic behavior.
    TAK-802
  • HY-131127
    7-Acetoxy-1-methylquinolinium iodide
    7-Acetoxy-1-methylquinolinium iodide (AMQI) is a fluorogenic substrate for cholinesterase (Ex = 320 nm, Em = 410 nm). Hydrolysis of 7-acetoxy-1-methylquinolinium iodide is used at the fluorometric flow system for the detection and identification of inhibitors..
    7-Acetoxy-1-methylquinolinium iodide
  • HY-147658
    AChE/BChE/BACE-1-IN-1
    Inhibitor
    AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 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-1 has remarkable antioxidant potential.
    AChE/BChE/BACE-1-IN-1
  • HY-N12075
    Dehydrodiscretamine chloride
    Inhibitor
    Dehydrodiscretamine chloride is a dual inhibitor of AChE and BChE with IC50s of 17.8 and 118.8 μM, respectively. Dehydrodiscretamine chloride has antioxidant activity. Dehydrodiscretamine chloride can be used in study Alzheimer’s disease.
    Dehydrodiscretamine chloride
  • HY-178017
    BChE/hCA II-IN-1
    Inhibitor
    BChE/hCA II-IN-1 (Compound 20) is a dual-functional inhibitor of Butyrylcholinesterase (BChE) and human carbonic anhydrase II (hCA II) with IC50s of 76.50 and 10.69  μM for BChE and hCA II, respectively. BChE/hCA II-IN-1 can be used for neurodegenerative diseases like Alzheimer's and glaucoma research.
    BChE/hCA II-IN-1
  • HY-168052
    hAChE-IN-9
    Inhibitor
    hAChE-IN-9 (compound 7i) is a selective inhibitor of human acetylcholinesterase (hAChE) with IC50 of 0.05 μM and 2.85 μM for AChE and BChE, respectively. hAChE-IN-9 modulates toxic oligomer forms into non-toxic ones and has antioxidant and neuroprotective effects against -induced toxicity. hAChE-IN-9 can be used for the study of Alzheimer's disease.
    hAChE-IN-9
  • HY-146313
    BChE-IN-7
    Inhibitor
    BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species.
    BChE-IN-7
  • HY-162127
    hAChE/hBACE-1-IN-3
    Inhibitor
    hAChE/hBACE-1-IN-3 (Compound 23a) is a mixed-type inhibitor of hAChE and hBACE-1 with IC50 values of 0.32 μM and 0.39 μM, respectively, Ki values of 0.26 μM and 0.46 μM, respectively. hAChE/hBACE-1-IN-3 can penetrate the blood-brain barrier.
    hAChE/hBACE-1-IN-3
  • HY-146035
    AChE-IN-14
    Inhibitor
    AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease.
    AChE-IN-14
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