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.

Cholinesterase (ChE) Related Products (460):

Cat. No. Product Name Effect Purity
  • HY-14566
    Donepezil Inhibitor
    Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
  • HY-B0034
    Donepezil Hydrochloride Inhibitor 99.94%
    Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
  • HY-Y0320
    Dimethyl sulfoxide Inhibitor
    Dimethyl sulfoxide (DMSO) is an aprotic solvent that dissolves polar and non-polar compounds, including water-insoluble therapeutic and toxic agents. Dimethyl sulfoxide (DMSO) has a strong affinity for water and can rapidly penetrate or enhance the penetration of other substances into biological membranes. Dimethyl sulfoxide also has potential free radical scavenging and anticholinesterase effects and may affect coagulation activity. Dimethyl sulfoxide also induces histamine release from mast cells but is thought to have low systemic toxicity. Dimethyl sulfoxide also exhibits antifreeze and antibacterial properties[1][2][3].
    MCE provides Dimethyl sulfoxide that complies with the inspection standards (Ch.P) of Part 4 of the Chinese Pharmacopoeia (2020 Edition).
  • HY-138097
    α-NETA Inhibitor
    α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity[1][2].
  • HY-108477
    TMPyP4 tosylate Inhibitor
    TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2[1][2][3][6].
  • HY-157959
    Orphenadrine Antagonist
    Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and cytochrome P450 (CYP) 2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation[1][2][3].
  • HY-161466
    AChE-IN-62 Inhibitor
    AChE-IN-62 (Compound 1) is an effective mixed and selective acetylcholinesterase (AChE) inhibitor with an IC50 value of 0.421 μM. AChE-IN-62 exhibits excellent blood-brain barrier permeability and neuroprotective effects. Additionally, AChE-IN-62 can inhibit the aggregation of Aβ1?42 with an IC50 value of 44.64 μM. AChE-IN-62 is also an effective multi-target-directed ligand (MTDL) that can be utilized in the research of Alzheimer's disease[1].
  • HY-162340
    Z32439948 Inhibitor
    Z32439948 is a butyrylcholinesterase (BChE) inhibitor (IC50: 1.4 μM, hBChE) and is a derivative of m-sulfamoylbenzamide. Z32439948 also exhibited neuroprotective effects against glutamate in SH-SY5Y cells[1].
  • HY-161058
    AChE-IN-49 Inhibitor
    AChE-IN-49 (Compd (S)-7g) is an acetylcholinesterase (AChE) inhibitor, with an IC50 of 0.0003 μM[1].
  • 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[1].
  • 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[1].
  • 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[1].
  • 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[1].
  • HY-N6608
    Physostigmine Inhibitor
    Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
  • HY-121467S
    Acotiamide-d6 Inhibitor
    Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia[1][2].
  • HY-N6895
    Violanthin Inhibitor
    Violanthin is isolated from the stems of Dendrobium officinale, has potent antioxidant and antibacterial activities. Violanthin inhibits acetylcholinesterase (AChE) with an IC50 value of 79.80 μM[1].
  • 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.[1].
  • HY-N8376
    Fustin Inhibitor
    Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research[1].
  • 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[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[1].