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-144660
    AChE-IN-7
    		Inhibitor
    AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability.
    AChE-IN-7
  • HY-180843
    Aβ/tau aggregation-IN-4
    		Inhibitor
    Aβ/tau aggregation-IN-4 (Compound D21) is an Aβ/tau aggregation inhibitor. Aβ/tau aggregation-IN-4 promotes the degradation of Aβ40/42 (Aβ40, IC50 = 2.151 μM; Aβ42, IC50 = 3.622 μM). Aβ/tau aggregation-IN-4 shows selective AChE inhibition (IC50: 5.56 μM). Aβ/tau aggregation-IN-4 inhibits MAO-A and MAO-B with IC50s of 0.59 μM and 0.09 μM, respectively. Aβ/tau aggregation-IN-4 suppresses intracellular ROS levels. Aβ/tau aggregation-IN-4 can be used in the research of Alzheimer's disease.
    Aβ/tau aggregation-IN-4
  • HY-114899
    Azamethiphos
    		Inhibitor 98.10%
    Azamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders.
    Azamethiphos
  • HY-B0916S
    Propoxur-d3
    		Inhibitor
    Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.
    Propoxur-d<sub>3</sub>
  • HY-156372
    AChE-IN-44
    		Inhibitor
    AChE-IN-44 (Compound Tap4) is an AChE inhibitor. AChE-IN-44 can be converted into the thiazole salt AChE inhibitor Tat2.
    AChE-IN-44
  • HY-W753485
    Profenofos-d3
    Profenofos-d3 is the deuterium labeled Profenofos (HY-B0832). Profenofos is an insecticida used on field crops, vegetables, and fruit crops. Profenofos is an acetylcholinesterase (AChE) inhibitor, with neurotoxicity.
    Profenofos-d<sub>3</sub>
  • HY-114899R
    Azamethiphos (Standard)
    		Inhibitor
    Azamethiphos (Standard) is the analytical standard of Azamethiphos (HY-114899). This product is intended for research and analytical applications. Azamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders.
    Azamethiphos (Standard)
  • HY-N6575
    7β-Hydroxybufalin
    		Inhibitor
    7β-Hydroxybufalin is a bufadienolide. 7β-Hydroxybufalin can be isolated from the venom of Bufo bufo gargarizans. 7β-Hydroxybufalin inhibits α-glucosidase and acetylcholinesterase.
    7β-Hydroxybufalin
  • HY-146686
    BuChE-IN-3
    		Inhibitor
    BuChE-IN-3 (Compound C4) is a potent inhibitor of BuChE with an IC50 of 8.3 nM. BuChE-IN-3 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity.
    BuChE-IN-3
  • HY-144689
    BChE-IN-3
    		Inhibitor
    BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC50 of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE.
    BChE-IN-3
  • HY-146959
    K203
    		Activator
    K203 is a potent reactivator of tabun-inhibited AChE. K203 is a crucial antidote used for the organophosphate intoxication.
    K203
  • HY-W011246S
    Velnacrine-d3 maleate
    Velnacrine-d3-1 maleate (HP 029-d3-1) is the deuterium labeled Velnacrine maleate (HY-W011246). Velnacrine maleate (HP 029) is an orally active cholinesterase inhibitor that can be used for the research of Alzheimer's disease.
    Velnacrine-d<sub>3</sub> maleate
  • HY-151927
    AChE-IN-28
    		Inhibitor
    AChE-IN-28 (Compound 2h) is a selective slow-binding inhibitor of acetylcholinesterase with an IC50 of 0.2 nM.
    AChE-IN-28
  • HY-N9513
    Echimidine N-oxide
    		Inhibitor
    Echimidine N-oxide, a pyrrolizidine alkaloid, has acetylcholinesterase (AChE) inhibitory activity (IC50=0.347 mM).
    Echimidine N-oxide
  • HY-175973
    AChE/BChE-IN-30
    		Inhibitor
    AChE/BChE-IN-30 (Compound 3g) is a Cholinesterase dual-target competitive inhibitor. AChE/BChE-IN-30 can inhibit AChE and BChE with IC50 values of 0.338 and 2.087 μM and Ki values of 0.045 and 0.789 μM. AChE/BChE-IN-30 can be used for the research of neurological disease, such as Alzheimer's disease.
    AChE/BChE-IN-30
  • HY-158092
    ChEs/MAOs-IN-2
    		Inhibitor
    ChEs/MAOs-IN-2 (compound a11) is a cholinesterases and monoamine oxidases inhibitor with IC50 values of 0.10, 0.20, 0.30, 0.40 µM for MAO-A, MAO-B, AChE, and BChE, respectively. ChEs/MAOs-IN-2 has the potential for the research of Alzheimer's disease.
    ChEs/MAOs-IN-2
  • HY-122957
    Huperzine C
    		Inhibitor
    Huperzine C is an alkaloid isolated from Huperzia serrate. Huperzine C is an acetylcholinesterase (AChE) inhibotor, with an IC50 of 0.6 μM. Huperzine C can be used for the research of Alzheimer’s disease.
    Huperzine C
  • HY-106901B
    Asoxime dimesylate
    		Inhibitor
    Asoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system.
    Asoxime dimesylate
  • HY-155708
    AChE/BChE-IN-13
    		Inhibitor
    AChE/BChE-IN-13 (compound 5j) is a potent dual inhibitor of AChE and BChE with IC50s of 20.89 and 17.37 μM, respectively. AChE/BChE-IN-13 can be used in Alzheimer’s disease (AD) research.
    AChE/BChE-IN-13
  • HY-127087
    Isogarcinol
    		Inhibitor
    Isogarcinol (Cambogin) is a potent AChE and BChE inhibitor, with IC50 values of 1.13 and 8.30 μM, respectively. Isogarcinol also shows leishmanicidal activity, with an IC50 of 0.33 μM against L. donovani.
    Isogarcinol
Cat. No. Product Name / Synonyms Application Reactivity
Cholinesterase (ChE) Isoform Comparison

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