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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 .
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 .
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 .
AChE-IN-45 (Compound 14) is an acetylcholinesterase (AChE) inhibitor with IC50 of 11.57±0.45 nM that shows antioxidant and neuroprotective activities .
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 .
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 .
(-)-Cyclopenin ((-)-Cyclopenine) is the enantiomer of Cyclopenin. Cyclopenin is a selective acetylcholinesterase(AChE) inhibitor with the IC50 of 2.04 μM .
Profenofos is an insecticida used on field crops, vegetables, and fruit crops. Profenofos is an acetylcholinesterase(AChE) inhibitor, with neurotoxicity .
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) .
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 .
Fenchlorphos, an organophosphate, is an insecticide. Fenchlorphos is an inhibitor of the enzyme acetylcholinesterase(AChE). Fenchlorphos is able to cause mitochondrial dysfunction .
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) .
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 .
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) .
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 .
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 .
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 .
Linarin (Buddleoside), isolated from the flower extract of Mentha arvensis, shows selective dose dependent inhibitory effect on acetylcholinesterase(AChE) .
Lycoramine hydrobromide, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine hydrobromide is a potent acetylcholinesterase(AChE) inhibitor .
Anatoxin-a (ATX-a) is a neurotoxic alkaloid. Anatoxin-a acts as both a nicotinic acetylcholine receptor (nAChR) agonist and an Acetylcholinesterase(AChE) inhibitor .
Azamethiphos-d6 is deuterated labeled Azamethiphos. Azamethiphos is an organophosphate insecticide and a neurotoxic agent, causing acetylcholinesterase(AChE) inhibition .
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 .
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 .
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 .
Swertianolin, a xanthone isolated from Gentianella Acuta, inhibits acetylcholinesterase(AChE). Swertianolin also exhibits anti-HBV and anti-bacterial activity .
Heliosupine is a pyrrolizidine alkaloid. Heliosupine is an acetylcholinesterase(AChE) inhibitor, with an IC50 0.57 mM. Heliosupine exhibits deterrent effects against generalist herbivores .
Territrem B is an irreversible inhibitor of Acetylcholinesterase(AChE) inhibitor. Territrem B is also a fungal meroterpenoid that can be isolated from Aspergillus terreus .
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 .
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/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 .
Corynoline is a reversible and noncompetitive acetylcholinesterase(AChE) inhibitor with an IC50 of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .
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 .
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 .
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 .
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 .
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 .
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-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 .
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 .
(-)-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 .
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 .
(±)-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 .
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-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 .
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 californicaAChE (TcAChE), hAChE and hBChE enzymes .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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].
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 .
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 .
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.
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].
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 .
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 .
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 .
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) .
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 .
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) .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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.
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 .
(-)-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 .
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 .
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 .
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 .
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 .
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 .
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 .
(-)-Cyclopenin ((-)-Cyclopenine) is the enantiomer of Cyclopenin. Cyclopenin is a selective acetylcholinesterase(AChE) inhibitor with the IC50 of 2.04 μM .
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) .
Linarin (Buddleoside), isolated from the flower extract of Mentha arvensis, shows selective dose dependent inhibitory effect on acetylcholinesterase(AChE) .
Lycoramine hydrobromide, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine hydrobromide is a potent acetylcholinesterase(AChE) inhibitor .
Anatoxin-a (ATX-a) is a neurotoxic alkaloid. Anatoxin-a acts as both a nicotinic acetylcholine receptor (nAChR) agonist and an Acetylcholinesterase(AChE) inhibitor .
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 .
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 .
Heliosupine is a pyrrolizidine alkaloid. Heliosupine is an acetylcholinesterase(AChE) inhibitor, with an IC50 0.57 mM. Heliosupine exhibits deterrent effects against generalist herbivores .
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 .
Bis-(-)-8-demethylmaritidine, a natural alkaloid, is a potent acetylcholinesterase(AChE) inhibitor. Bis-(-)-8-demethylmaritidine can be used for Alzheimer's disease research .
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 .
(-)-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 .
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 .
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 californicaAChE (TcAChE), hAChE and hBChE enzymes .
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 .
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 .
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 .
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 .
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) .
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 .
(-)-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 .
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 .
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.
Galanthamine-d6 (Galantamine-d6) is the deuterium labeled Galanthamine. Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM[1][2].
Azamethiphos-d6 is deuterated labeled Azamethiphos. Azamethiphos is an organophosphate insecticide and a neurotoxic agent, causing acetylcholinesterase(AChE) inhibition .
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].
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].
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.
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