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Acetylcholinesterase, Fly head (ACHE; EC 3.1.1.7) is a cholinergic enzyme mainly found in neuromuscular junctions and cholinergic type chemical synapses used in biochemical research. Acetylcholinesterase, Fly head catalyzes the breakdown or hydrolysis of acetylcholine and some other cholineesters that act as neurotransmitters into acetate and choline. Acetylcholinesterase, Fly head's main role is to terminate neuronal transmission and signaling between synapses to prevent ACh spread and activation of nearby receptors .
Osmanthuside B can be isolated from Pseuderanthemum carruthersii (Seem.) Guill. var. atropurpureum (Bull.) Fosb and has weak acetylcholinesterase inhibitory activity .
Fosthiazate is a broad-spectrum nematicide against various plant parasitic nematodes, including Meloidogyne spp., Globodera spp., and Pratylenchus spp., through inhibiting the synthesis of acetylcholinesterase .
Linarin (Buddleoside), isolated from the flower extract of Mentha arvensis, shows selective dose dependent inhibitory effect on acetylcholinesterase (AChE) .
Heliosupine is a pyrrolizidine alkaloid. Heliosupine is an acetylcholinesterase (AChE) inhibitor, with an IC50 0.57 mM. Heliosupine exhibits deterrent effects against generalist herbivores .
Fenchlorphos, an organophosphate, is an insecticide. Fenchlorphos is an inhibitor of the enzyme acetylcholinesterase (AChE). Fenchlorphos is able to cause mitochondrial dysfunction .
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 .
N-Boc-4-piperidinemethanol (compound 4) is an acetylcholinesterase (AChE) inhibitor. N-Boc-4-piperidinemethanol can used ti study Alzheimer’s Disease .
Lycoramine hydrobromide, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine hydrobromide is a potent acetylcholinesterase (AChE) inhibitor .
K027 is a potent reactivator of Organophosphates (OP)-inhibited acetylcholinesterase (AChE). K027 can be used for the research of Alzheimer's disease .
Obidoxime dichloride is a non-full spectrum oxime agent and can be used as an antidote for organophosphate nerve agent poisoning. Obidoxime dichloride reactivates sarin-inhibited acetylcholinesterase (AChE) and reduces acute toxicity of sarin-evaluated .
Fasciculin-I is isolated from the mambas venom. Fasciculin-I exerts its toxic effects by inhibiting acetylcholinesterase (AChE). Fasciculin-I blocks α-neurotoxins of nicotinic acetylcholine receptors and cardiac toxins that interact with cell membranes .
7β-Hydroxybufalin is a bufadienolide. 7β-Hydroxybufalin can be isolated from the venom of Bufo bufo gargarizans. 7β-Hydroxybufalin inhibits α-glucosidase and acetylcholinesterase .
Talaromycesone A is an oxaphenalenone dimer compound. Talaromycesone A exhibits potent antibacterial activities with an IC50 of 3.70 μM, against human pathogenic Staphylococcus strains. Talaromycesone A displays potent acetylcholinesterase inhibitory activities with an IC50 of 7.49 μM .
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 .
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 .
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively .
AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease .
AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease .
RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue .
Aβ1-42 aggregation inhibitor 1 inhibits AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) with the IC50 value of 2.64 μM and 1.29 μM, respectively. Aβ1-42 aggregation inhibitor 1 inhibits self-mediated Aβ1-42 aggregation by 51.29% at a concentration of 25 μM. Aβ1-42 aggregation inhibitor 1 has the potential for the research of anti-Alzheimer's disease .
AChE-IN-15 (Compound 3d) is a reversible human acetylcholinesterase (huAChE) (IC50=6.8 μM) and human butyrylcholinesterase (huBChE) (IC50=16.1 μM) inhibitor. AChE-IN-15 shows significant antioxidant potency, AChE-IN-15 can be used for the research of Alzheimer’s disease .
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 .
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside), a flavonol, possesses enzyme inhibition property towards α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3,7-di-O-β-glucoside protects differentiating neuronal cells, SH-SY5Y from Amyloid β peptide-induced injury. Kaempferol-3,7-di-O-β-glucoside has the potential for Alzheimer's research .
Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease .
Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease .
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease .
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 12.
(-)-Cyclopenin ((-)-Cyclopenine) is the enantiomer of Cyclopenin. Cyclopenin is a selective acetylcholinesterase (AChE) inhibitor with the IC50 of 2.04 μM .
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease .
Trimethylammonium chlorideIt is an endogenous metabolite that inhibits deacetylation. Trimethylammonium chlorideIs a non-competitive inhibitor of acetylcholinesterase .
Profenofos is an insecticida used on field crops, vegetables, and fruit crops. Profenofos is an acetylcholinesterase (AChE) inhibitor, with neurotoxicity .
Edrophonium (chloride) (Standard) is the analytical standard of Edrophonium (chloride). This product is intended for research and analytical applications. Edrophonium chloride is a reversible inhibitor of acetylcholinesterase.
(±)-Marmesin is a good precursor of the linear furanocoumarins. (±)-Marmesin derivatives have high degree of acetylcholinesterase inhibitory property .
Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM.
Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE) .
Anatoxin-a (ATX-a) is a neurotoxic alkaloid. Anatoxin-a acts as both a nicotinic acetylcholine receptor (nAChR) agonist and an Acetylcholinesterase (AChE) inhibitor .
Pitofenone hydrochloride, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with Kis of 36 and 45 μM, respectively.
Nodakenin is a major coumarin glucoside in the root of Angelica decusiva. Nodakenin inhibits acetylcholinesterase(AChE) activity with an IC50 of 84.7 μM .
O-Desmethyl Galanthamine (Sanguinine) is galanthamine-type alkaloid. O-Desmethyl Galanthamine is an acetylcholinesterase (AChE) inhibitor, with an IC50 1.83 μM .
Acetyllycoposerramine M is a lycopodine-type alkaloid, which can be isolated from Lycopodium japonicum. But Acetyllycoposerramine M has no inhibitory effect on acetylcholinesterase .
AChE-IN-45 (Compound 14) is an acetylcholinesterase (AChE) inhibitor with IC50 of 11.57±0.45 nM that shows antioxidant and neuroprotective activities .
Swertianolin, a xanthone isolated from Gentianella Acuta, inhibits acetylcholinesterase (AChE). Swertianolin also exhibits anti-HBV and anti-bacterial activity .
Territrem B is an irreversible inhibitor of Acetylcholinesterase (AChE) inhibitor. Territrem B is also a fungal meroterpenoid that can be isolated from Aspergillus terreus .
Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .
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 .
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity .
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 .
Coumaran (2,3-Dihydrobenzofuran) is an AChE inhibitor with antileishmanial activity. Coumaran may acquire antiparasitic capabilities through activation of macrophages and exert immunomodulatory activity. Coumaran can be used as a biopesticide. .
Protopine (Corydinine), an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity .
Galanthamine-d6 (Galantamine-d6) is the deuterium labeled Galanthamine. Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM[1][2].
1-Naphthyl acetate is an attractive chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity. 1-Naphthyl acetate has the potential to detect organophosphorus pesticide (OP) poisoning .
Bis-(-)-8-demethylmaritidine, a natural alkaloid, is a potent acetylcholinesterase (AChE) inhibitor. Bis-(-)-8-demethylmaritidine can be used for Alzheimer's disease research .
AChE-IN-26 (compound 4a) is an AChE (acetylcholinesterase) inhibitor with an IC50 value of 0.42 μM. AChE-IN-26 can be used for the research of Alzheimer’s disease .
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae .
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
Picfeltarraenin IB, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation .
Picfeltarraenin IV, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IV can be used for the treatment of herpes infections, cancer and inflammation .
Picfeltarraenin IA, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IA can be used for the treatment of herpes infections, cancer and inflammation .
Huperzine B is a Lycopodium alkaloid isolated from Huperzia serrata and a highly selective acetylcholinesterase (AChE) inhibitor. Huperzine B can be uesd to can be used to improve Alzheimer's disease .
AChE-IN-25 is a potent, selective and uncompetitive acetylcholinesterase (AChE) inhibitor (IC50=2.95 µM). AChE-IN-25 can be used in Alzheimer's disease research .
AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research .
S-(-)-N-trans-Feruloyl normetanephrine is a nature product with weak anti-acetylcholinesterase activity. S-(-)-N-trans-Feruloyl normetanephrine can be isolated from the aerial parts of Bassia indica Wight .
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines .
Pseudocoptisine (Isocoptisine) acetate is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine acetate inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects .
Pseudocoptisine (Isocoptisine) chloride is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects .
Carbonic anhydrase/AChE-IN-2 (compound 19) is a selective acetylcholinesterase (AChE) and carbonic anhydrase (CA) inhibitor, with Ei of 5.07 nM, 24.42 nM and 19.95 nM for AChE, hCAI and hCAII, respectively .
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor[1][2].
Pralidoxime chloride is a potent reactivator of acetylcholinesterase (AChE). Pralidoxime chloride reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime chloride is an antidote for organophosphate poisoning .
Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor .
Pralidoxime is a potent reactivator of acetylcholinesterase (AChE). Pralidoxime reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime is an antidote for organophosphate poisoning .
Kokusaginine is a furoquinoline alkaloids, which exhibits inhibitory efficacy for acetylcholinesterase (AChE) with an IC50 of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptotic inducing effects in MCF-7/ADR cells .
MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC50 values of 31 μM. Lucidadiol shows antiviral activity against influenza virus type A and HSV type 1 .
(-)-Corynoxidine is an acetylcholinesterase inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa .
(-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains in different degrees .
Pralidoxime iodide is a potent reactivator of acetylcholinesterase (AChE). Pralidoxime iodide reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime iodide is an antidote for organophosphate poisoning .
2'-O-Succinyl-cAMP is a cAMP analog that can be covalently coupled to acetylcholinesterase. 2'-O-Succinyl-cAMP conjugate has been used as tracers in a classical heterogeneous competitive enzyme immunoassay allowing the determination of cAMP .
N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC50 of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC50 of 13.3 µM for T. brucei rhodesiense .
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 .
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively) . PE154 can label β-amyloid plaques in histochemical analysis .
Kuwanon U is a potent cholinesterase inhibitor with IC50s of 19.69, 10.11 µM and Kis of 6.48, 9.59 µM for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively. Kuwanon U has the potential for the research of Alzheimer’s disease (AD) .
sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively .
AChE-IN-60 (compound 6k) is a potant acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor with IC50s of 27 nM and 43 nM, respectively. AChE-IN-60 also inhibits monoamine oxidase (MAO)-A and MAO-B with IC50s of 353 nM and 716 nM, respectively .
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease . Ladostigil (hemitartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
AChE-IN-58 (Compound 3) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-58 can extend the mean lifespan, delay the Aβ1-42-induced paralysis, enhanc the locomotion, and alleviate glutamic acid (Glu)-induced neurotoxicity of CL4176 worms .
sEH/AChE-IN-1 (Compound 12a) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-1 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-1 has the potential for the research of Alzheimer's disease (AD) .
sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively .
Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning .
sEH/AChE-IN-2 (Compound 12b) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-2 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-2 has the potential for the research of Alzheimer's disease (AD) .
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes .
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning .
Y13g is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g reverses the STZ-induced memory deficit, and shows histopathology similarly as in normal animals .
Isograndifoliol is a selective inhibitor of butyrylcholinesterase (BChE) with an IC50 value of 0.9 μM. And Isograndifoliol moderately inhibits acetylcholinesterase (AChE) with an IC50 value of 342.9 μM. Isograndifoliol also has vasorelaxant effect and anti-tumor effect. Isograndifoliol can be used for research against dementia caused by neurodegenerative diseases .
Y13g dihydrochloride is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g dihydrochloride reverses the STZ-induced memory deficit, and shows histopathology similarly as in normal animals .
AChE/Aβ-IN-4 is a dual inhibitor of acetylcholinesterase (AChE) and β-amyloid (Aβ) aggregation, with the IC50 values of 1.72 ± 0.18 μM and 1.42 ± 0.3 μM, respectively. AChE/Aβ-IN-4 plays an impotant role in neurological disorders, such as Alzheimer’s disease .
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains .
AChE-IN-51 (compound 8C) is an orally active, non-competitive inhibitor of AChE and BChE (IC50: 84 nM, 97 nM). It also inhibits MMP-2 and amyloid Aβ1-42 aggregates (IC50: 724 nM, 302 nM). AChE-IN-51 has low cytotoxicity and in silico predicted blood-brain barrier permeability. Can be used for research on diseases such as Alzheimer's disease (AD) .
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
Physostigmine-d3 is the deuterium labeled Physostigmine. 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].
Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
Chlorpyrifos-d10 is the deuterium labeled Chlorpyrifos. Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
Trimyristin--d15 is the deuterium labeled Trimyristin. Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
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 .
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment .
Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex .
AChE-IN-52 (compound A6) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-52 shows antitumor efficacy, especially against breast cancer MCF-7 cells. AChE-IN-52 significantly disrupts the amino acid metabolism and inhibits migration of MCF-7. AChE-IN-52 plays anticancer role by regulating Best1 and HIST1H2BJ .
Xanthohumol I, a chalkone, is a derivative of Xanthohumol (HY-N1067). Xanthohumol is a Cholinesterase (ChE) inhibitor, which inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) wih IC50s of 71.34 μM and 32.67 μM, respectively. The hydroxy compound of Xanthohumol (3-hydroxy-xanthohumol), also shoes inhibitory effect on AChE and BChE with IC50s of 51.25 μM and 63.07 μM .
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
AChE/BChE-IN-16 (compound C7) is a potent cholinesterase (ChE) inhibitor with IC50s of 30 nM and 48 nM for human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE), respectively. AChE/BChE-IN-16 exhibits a remarkable capacity to safeguard PC12 cells against H2O2-induced apoptosis and effectively suppresses the production of reactive oxygen species (ROS) .
Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
AChE/BChE-IN-3 (BMC-1) is a dual AChE and BChE inhibitor with IC50 values of 6.08 μM and 0.383 μM against electric eel AChE (elAChE) and equine serum BChE (eqBChE), respectively .
AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity .
AChE/BChE-IN-3 (BMC-1) hydrochloride is a dual AChE and BChE inhibitor with IC50 values of 6.08 μM and 0.383 μM against electric eel AChE (elAChE) and equine serum BChE (eqBChE), respectively .
AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB .
AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 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-2 has remarkable antioxidant potential .
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/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
β-Amyrone (β-Amyron) is a triterpene compound which has anti-inflammatory activity through inhibiting the expression of COX-2. β-Amyrone has antifungal activity , as well as antiviral activity against Chikungunya virus. β-Amyrone also inhibits α-glucosidase and acetylcholinesterase (AChE) activity. β-Amyrone can be used in the research of disease like inflammation, infection, and obesity .
MAO-B-IN-26 (Compound IC9) is a MAO-B and acetylcholinesterase inhibitor. MAO-B-IN-26 protects SH?SY5Y cells against Aβ induced cytotoxicity, morphological changes, ROS generation and membrane damage. MAO-B-IN-26 also inhibits Aβ induced autophagy and apoptosis. MAO-B-IN-26 can be used as a neuroprotective agent against Alzheimer’s disease .
Isoeugenol acetate (Acetyl isoeugenol), an essential oil constituent of nutmeg, clove, and cinnamon, shows excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes (IC50=77 nM; Ki=16 nM), α-glycosidase (IC50=19.25 nM; Ki=21 nM), and α-amylase (IC50=411.5 nM). Isoeugenol acetate is used medical and cosmetics industries for its antioxidant, anticancer, antimicrobial and anti-inflammatory properties .
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 .
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 .
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 .
AChE/BChE-IN-4 (BMC-3) is a dual AChE and BChE inhibitor with IC50 values of 792 nM and 2.2 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-4 can cross the BBB .
AChE/BChE-IN-5 (BMC-16) is a dual AChE and BChE inhibitor with IC50 values of 266 nM and 10.6 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-5 can cross the BBB .
AChE/hCA I/II-IN-1 (Compound 6) is a potent inhibitor of AChE/Hca with IC50 values of 22.21, 60.79 and 66.64 nM for AChE, Hca Ⅰ and Hca Ⅱ. AChE/hCA I/II-IN-1 can be used for the rsearch for glaucoma, Alzheimer's disease, diabetes .
Desoxypeganine (Deoxypeganine), an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine can be used for alcohol abuse research .
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research .
AChE/Aβ-IN-1 (compound 32) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 86 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 3.876 μM. AChE/Aβ-IN-1 also inhibits Aβ aggregation and shows good blood-brain barrier permeability and neuroprotection. AChE/Aβ-IN-1 improves cognitive and spatial memory impairment in rats model .
AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model .
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 .
TZ4M is a 2,4-thiazolidinedione (TZD)-based anti-ADV agent with neuroprotective effects. TZ4M exhibits AChE inhibition in human plasma. TZ4M improves memory and cognitive impairment in adult rats in a scopolamine (HY-N0296)-induced Alzheimer-type model .
TZ3O (compound TZ30) is an anticholinergic agent with neuroprotective effects. TZ3O (2 mg/kg, 4 mg/kg) can improve memory impairment and cognitive decline in rats in the Scopolamine (HY-N0296)-induced Alzheimer-type model. TZ3O could be used in Alzheimer’s research .
AChE/BuChE-IN-4(compound 4a) is aorally activeandbrain-penetrantmultitarget-directedAChE/BuChEinhibitor againstAChEandBuChE, with theIC50of 2.08 and 7.41 μM .
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu 2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease .
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively) . PE154 can label β-amyloid plaques in histochemical analysis .
N-Boc-4-piperidinemethanol (compound 4) is an acetylcholinesterase (AChE) inhibitor. N-Boc-4-piperidinemethanol can used ti study Alzheimer’s Disease .
Fasciculin-I is isolated from the mambas venom. Fasciculin-I exerts its toxic effects by inhibiting acetylcholinesterase (AChE). Fasciculin-I blocks α-neurotoxins of nicotinic acetylcholine receptors and cardiac toxins that interact with cell membranes .
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 12.
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Osmanthuside B can be isolated from Pseuderanthemum carruthersii (Seem.) Guill. var. atropurpureum (Bull.) Fosb and has weak acetylcholinesterase inhibitory activity .
Linarin (Buddleoside), isolated from the flower extract of Mentha arvensis, shows selective dose dependent inhibitory effect on acetylcholinesterase (AChE) .
Heliosupine is a pyrrolizidine alkaloid. Heliosupine is an acetylcholinesterase (AChE) inhibitor, with an IC50 0.57 mM. Heliosupine exhibits deterrent effects against generalist herbivores .
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 .
Lycoramine hydrobromide, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine hydrobromide is a potent acetylcholinesterase (AChE) 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 .
Talaromycesone A is an oxaphenalenone dimer compound. Talaromycesone A exhibits potent antibacterial activities with an IC50 of 3.70 μM, against human pathogenic Staphylococcus strains. Talaromycesone A displays potent acetylcholinesterase inhibitory activities with an IC50 of 7.49 μM .
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 .
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively .
Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside), a flavonol, possesses enzyme inhibition property towards α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3,7-di-O-β-glucoside protects differentiating neuronal cells, SH-SY5Y from Amyloid β peptide-induced injury. Kaempferol-3,7-di-O-β-glucoside has the potential for Alzheimer's research .
Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease .
Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease .
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease .
(-)-Cyclopenin ((-)-Cyclopenine) is the enantiomer of Cyclopenin. Cyclopenin is a selective acetylcholinesterase (AChE) inhibitor with the IC50 of 2.04 μM .
(±)-Marmesin is a good precursor of the linear furanocoumarins. (±)-Marmesin derivatives have high degree of acetylcholinesterase inhibitory property .
Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM.
Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE) .
Anatoxin-a (ATX-a) is a neurotoxic alkaloid. Anatoxin-a acts as both a nicotinic acetylcholine receptor (nAChR) agonist and an Acetylcholinesterase (AChE) inhibitor .
Nodakenin is a major coumarin glucoside in the root of Angelica decusiva. Nodakenin inhibits acetylcholinesterase(AChE) activity with an IC50 of 84.7 μM .
O-Desmethyl Galanthamine (Sanguinine) is galanthamine-type alkaloid. O-Desmethyl Galanthamine is an acetylcholinesterase (AChE) inhibitor, with an IC50 1.83 μM .
Acetyllycoposerramine M is a lycopodine-type alkaloid, which can be isolated from Lycopodium japonicum. But Acetyllycoposerramine M has no inhibitory effect on acetylcholinesterase .
Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .
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 .
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity .
Coumaran (2,3-Dihydrobenzofuran) is an AChE inhibitor with antileishmanial activity. Coumaran may acquire antiparasitic capabilities through activation of macrophages and exert immunomodulatory activity. Coumaran can be used as a biopesticide. .
Protopine (Corydinine), an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity .
Bis-(-)-8-demethylmaritidine, a natural alkaloid, is a potent acetylcholinesterase (AChE) inhibitor. Bis-(-)-8-demethylmaritidine can be used for Alzheimer's disease research .
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae .
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
Picfeltarraenin IV, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IV can be used for the treatment of herpes infections, cancer and inflammation .
Huperzine B is a Lycopodium alkaloid isolated from Huperzia serrata and a highly selective acetylcholinesterase (AChE) inhibitor. Huperzine B can be uesd to can be used to improve Alzheimer's disease .
S-(-)-N-trans-Feruloyl normetanephrine is a nature product with weak anti-acetylcholinesterase activity. S-(-)-N-trans-Feruloyl normetanephrine can be isolated from the aerial parts of Bassia indica Wight .
Pseudocoptisine (Isocoptisine) acetate is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine acetate inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects .
Pseudocoptisine (Isocoptisine) chloride is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects .
Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor .
Kokusaginine is a furoquinoline alkaloids, which exhibits inhibitory efficacy for acetylcholinesterase (AChE) with an IC50 of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptotic inducing effects in MCF-7/ADR cells .
Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC50 values of 31 μM. Lucidadiol shows antiviral activity against influenza virus type A and HSV type 1 .
(-)-Corynoxidine is an acetylcholinesterase inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa .
(-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains in different degrees .
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 .
Kuwanon U is a potent cholinesterase inhibitor with IC50s of 19.69, 10.11 µM and Kis of 6.48, 9.59 µM for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively. Kuwanon U has the potential for the research of Alzheimer’s disease (AD) .
AChE-IN-58 (Compound 3) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-58 can extend the mean lifespan, delay the Aβ1-42-induced paralysis, enhanc the locomotion, and alleviate glutamic acid (Glu)-induced neurotoxicity of CL4176 worms .
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes .
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment .
Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex .
Xanthohumol I, a chalkone, is a derivative of Xanthohumol (HY-N1067). Xanthohumol is a Cholinesterase (ChE) inhibitor, which inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) wih IC50s of 71.34 μM and 32.67 μM, respectively. The hydroxy compound of Xanthohumol (3-hydroxy-xanthohumol), also shoes inhibitory effect on AChE and BChE with IC50s of 51.25 μM and 63.07 μM .
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
β-Amyrone (β-Amyron) is a triterpene compound which has anti-inflammatory activity through inhibiting the expression of COX-2. β-Amyrone has antifungal activity , as well as antiviral activity against Chikungunya virus. β-Amyrone also inhibits α-glucosidase and acetylcholinesterase (AChE) activity. β-Amyrone can be used in the research of disease like inflammation, infection, and obesity .
Isoeugenol acetate (Acetyl isoeugenol), an essential oil constituent of nutmeg, clove, and cinnamon, shows excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes (IC50=77 nM; Ki=16 nM), α-glycosidase (IC50=19.25 nM; Ki=21 nM), and α-amylase (IC50=411.5 nM). Isoeugenol acetate is used medical and cosmetics industries for its antioxidant, anticancer, antimicrobial and anti-inflammatory properties .
Desoxypeganine (Deoxypeganine), an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine can be used for alcohol abuse research .
Acetylcholinesterase (ACHE) proteins exhibit multiple functions, including acetylcholinesterase activity and protein self-association. It regulates acetylcholine processing, receptor signaling and recycling. Acetylcholinesterase/ACHE Protein, Mouse (HEK293, His) is the recombinant mouse-derived Acetylcholinesterase/ACHE protein, expressed by HEK293 , with C-10*His labeled tag. The total length of Acetylcholinesterase/ACHE Protein, Mouse (HEK293, His) is 583 a.a., with molecular weight of ~80 kDa.
Acetylcholinesterase (ACHE) protein is pivotal in neurotransmission, rapidly hydrolyzing acetylcholine in the synaptic cleft to terminate signal transduction at the neuromuscular junction. Beyond neurotransmitter regulation, ACHE is implicated in neuronal apoptosis, indicating a broader role in cellular processes associated with programmed cell death. Acetylcholinesterase/ACHE Protein, Human (CHO, His) is the recombinant human-derived Acetylcholinesterase/ACHE protein, expressed by CHO , with C-6*His labeled tag. The total length of Acetylcholinesterase/ACHE Protein, Human (CHO, His) is 583 a.a., with molecular weight of ~66 kDa.
CUTA protein is a trimeric membrane anchor protein of AChE and a homolog of the bacterial divalent cation chelator CutA1 protein. CUTA protein also interacts with BACE1 and inhibits APP beta processing and Aβ production. CutA Protein, Human (His) is the recombinant human-derived CutA protein, expressed by E. coli , with C-6*His labeled tag. The total length of CutA Protein, Human (His) is 156 a.a., with molecular weight of ~17.0 kDa.
Galanthamine-d6 (Galantamine-d6) is the deuterium labeled Galanthamine. Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM[1][2].
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor[1][2].
Physostigmine-d3 is the deuterium labeled Physostigmine. 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].
Chlorpyrifos-d10 is the deuterium labeled Chlorpyrifos. Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
Trimyristin--d15 is the deuterium labeled Trimyristin. Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease . Ladostigil (hemitartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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