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Acetylcholinesterase (AChE) inhibitors block the enzyme that breaks down acetylcholine at cholinergic synapses. By ending acetylcholine signaling within milliseconds, AChE controls transmission in the brain and at the neuromuscular junction. The 1991 crystal structure of AChE from Torpedo californica showed the active site at the base of a deep, narrow gorge. AChE also has non-catalytic roles, which broaden its interest beyond synaptic transmission. Inhibitors here include donepezil hydrochloride and galanthamine hydrobromide, which are reversible inhibitors. The carbamates rivastigmine tartrate and neostigmine bromide, used in studies of cholinergic signaling and neurodegeneration, are also listed.
DTNP is a BchE-activated near infrared (NIR) fluorescent probe known for its ability to permeate the blood-brain barrier. Upon activation by butyrylcholinesterase (BchE), DTNP exhibits inhibitory effects on enzyme activity, making it a valuable tool in the study of Alzheimer's disease (AD). Its unique properties facilitate research into the pathological mechanisms and potential therapeutic strategies related to neurodegeneration.
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hAChE-IN-6 is a selective acetylcholinesterase (AChE) inhibitor, demonstrating an IC50 of 0.16 μM. It also inhibits human butyrylcholinesterase (hBuChE) and glycogen synthase kinase 3 beta (GSK3β) with IC50 values of 0.69 μM and 0.26 μM, respectively. Notably, hAChE-IN-6 inhibits the self-aggregation of tau protein and amyloid beta 1-42, making it a valuable reagent for research into Alzheimer's disease pathogenesis and therapeutic strategies.
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AChE/BACE1/GSK3β-IN-1 is a potent triple inhibitor targeting acetylcholinesterase (AChE), beta-secretase 1 (BACE1), and glycogen synthase kinase 3 beta (GSK3β). It demonstrates effective inhibitory activity with IC50 values of 1.0 μM for AChE, 20 μM for BACE1, and 15 μM for GSK3β. With favorable blood-brain barrier penetrability and bioavailability, AChE/BACE1/GSK3β-IN-1 is a valuable tool for research into Alzheimer's disease mechanisms and therapeutics.
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ZLWH-23 is a selective inhibitor of acetylcholinesterase (AChE) with an IC50 of 0.27 μM and also inhibits glycogen synthase kinase-3 beta (GSK-3β) with an IC50 of 6.78 μM. It exhibits greater selectivity for AChE compared to butyrylcholinesterase (BChE) and shows preferential inhibition of GSK-3β over a range of multi-kinases. This compound is relevant for research focused on Alzheimer's disease pathophysiology.
PJ17 is a potent dual inhibitor of acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), exhibiting IC50 values of 8.84 μM and 4.19 μM, respectively. This compound demonstrates a lack of significant neurotoxicity in primary cerebellar granule neuron cultures, making it a promising candidate for neuropharmacological studies. PJ17 serves as a valuable template for the development of multitarget therapeutics and is relevant in research focused on Alzheimer's disease.
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hAChE-IN-5 is a potent inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting IC50 values of 0.17 μM for both enzymes. In addition, hAChE-IN-5 demonstrates significant GSK3β inhibition with an IC50 of 0.21 μM. This compound is utilized in research focused on tau protein aggregation and Aβ1-42 self-aggregation, effectively preventing Aβ-dependent neurotoxicity. Furthermore, hAChE-IN-5 can cross the blood-brain barrier, showcasing its potential as a multi-targeted agent in the study of Alzheimer's disease.
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Resorufin butyrate is a fluorogenic substrate primarily utilized for the detection of triglyceride lipases and cholinesterase. With excitation at 570 nm and emission at 580 nm, this compound facilitates sensitive fluorescence-based assays. It is particularly valuable in biochemical studies focusing on lipid metabolism and enzyme activity.
Synonyms: Coumarin 478
Coumarin 106 is a dipolar laser dye that serves as an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). It exhibits mixed-type inhibition of AChE with a pIC50 of 4.97 and a Ki value of 2.36 μM, while also inhibiting BChE with a slightly lower potency (pIC50 of 4.56). This compound is valuable in studying cholinergic signaling pathways and may aid in the exploration of therapeutic strategies for disorders linked to cholinergic dysfunction.
PE154 is a highly potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 280 pM and 16 nM, respectively. This compound is effective for visualizing β-amyloid plaques in histochemical analyses, making it a valuable tool in research focused on neurodegenerative diseases and cholinergic system studies. Its high specificity and sensitivity enhance its utility in biochemical assays and pathological examinations.
Jatrorrhizine chloride is a bioactive alkaloid derived from Coptis chinensis, exhibiting diverse pharmacological properties such as neuroprotection, antimicrobial action, antiplasmodial effects, and antioxidant activity. This compound acts as a potent and selective inhibitor of acetylcholinesterase (AChE) with an IC50 of 872 nM, demonstrating over 115-fold selectivity for butyrylcholinesterase (BuChE). Additionally, Jatrorrhizine chloride inhibits the uptake of serotonin (5-HT) and norepinephrine (NE) through blockade of uptake-2 transporters, making it a valuable tool in neurological and pharmacological research.
Jatrorrhizine hydroxide is a bioactive alkaloid derived from Coptis chinensis, primarily known for its neuroprotective, antimicrobial, antiplasmodial, and antioxidant properties. It functions as a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 872 nM, exhibiting over 115-fold selectivity for butyrylcholinesterase (BuChE). Additionally, Jatrorrhizine hydroxide inhibits the uptake of serotonin (5-HT) and norepinephrine (NE) through the modulation of uptake-2 transporters, making it valuable for research in neuropharmacology and neurodegenerative disorders.
Jatrorrhizine is a bioactive alkaloid derived from Coptis chinensis, known for its neuroprotective, antimicrobial, antiplasmodial, and antioxidant properties. This compound serves as a potent, orally active inhibitor of acetylcholinesterase (AChE) with an IC50 value of 872 nM, demonstrating over 115-fold selectivity for butyrylcholinesterase (BuChE). Additionally, Jatrorrhizine inhibits the uptake of serotonin (5-HT) and norepinephrine (NE) through the inhibition of uptake-2 transporters, making it a valuable reagent for neurological and pharmacological research.
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Synonyms: Eugeniin
Tellimagrandin II is an antibacterial agent that disrupts the integrity of the cell wall in Staphylococcus aureus, leading to cell lysis and loss of cytoplasmic contents. Additionally, it demonstrates anti-inflammatory properties and inhibits acetylcholinesterase (AChE), which may contribute to improvements in memory impairment. This compound is of interest in research focusing on antibacterial strategies, inflammatory pathways, and neurodegenerative conditions.
Bacillosporin C is an oxaphenalenone dimer that acts as a potent antibiotic. Isolated from the bacterium T. bacillosporus and derived from the lactone bacillosporin D found in the mangrove endophytic fungus SBE-14, Bacillosporin C demonstrates significant antibacterial properties. Additionally, it has been shown to inhibit acetylcholinesterase, making it a valuable tool for research in microbial resistance and neuropharmacology.
Manumycin B is an antibiotic that also demonstrates notable antitumor activity. It functions as an inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 value of 15 mM. This compound is valuable for research in cancer biology and neuropharmacology, providing insights into therapeutic strategies for cancer treatment and neurodegenerative disorders.
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Synonyms: Castanogenin
Medicagenic acid, a potent bacterial inhibitor derived from the roots of Herniaria glabra, demonstrates significant fungistatic activity against various plant pathogens and human dermatophytes. This compound exhibits low enzyme inhibitory activity, specifically targeting xanthine oxidase, collagenase, elastase, tyrosinase, and cholinesterase. Medicagenic acid is valuable for research applications in studying antifungal resistance mechanisms and exploring potential therapeutic avenues for dermatological conditions.
2-Hydroxydocosanoic acid is a versatile compound known for its antioxidant properties, inhibition of cholinesterase, and antimicrobial activity. It has shown potential in mitigating oxidative stress, making it relevant for studies focused on neuroprotection and aging. Additionally, its antimicrobial effects support research applications in combating microbial resistance. This compound serves as a valuable tool for exploring mechanisms related to oxidative damage and microbial inhibition.
(-)-Corynoxidine is an acetylcholinesterase (ChE) inhibitor with an IC50 of 89.0 μM, derived from the aerial parts of Corydalis speciosa. This compound demonstrates antibacterial activity against Staphylococcus aureus, including methicillin-resistant strains, making it a valuable tool for research in neurology and antimicrobial studies.
Ilicicolin C is an antibacterial agent with demonstrated efficacy against Pseudomonas syringae, exhibiting an IC50 of 28.5 µg/mL. Additionally, it has shown weak inhibitory effects on acetylcholinesterase and β-glucuronidase, with IC50 values ranging from 30 to 43 µg/mL. The compound also displays weak cytotoxicity in human lung fibroblasts, with IC50 values of 64 to 120 µg/mL. Furthermore, Ilicicolin C influences seed germination and root tip growth in lettuce, indicating potential implications in plant research.
Talaromycesone A is an oxaphenalenone dimer with significant antibacterial properties, exhibiting an IC50 of 3.70 μM against Staphylococcus strains pathogenic to humans. Additionally, it demonstrates strong inhibition of acetylcholinesterase with an IC50 of 7.49 μM. This compound is valuable for research applications focusing on antimicrobial susceptibility and neuropharmacology.
Quinuronium disulfate is a potent babesicidal agent with demonstrated anticholinesterase activity. It is primarily utilized in the study of protozoan infections, particularly those caused by Babesia species. This compound serves as a valuable tool in researching therapeutic interventions for babesiosis and related parasitic diseases.
Synonyms: HSR803 free base
Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies.
SMase-IN-1 is a specific inhibitor of bacterial sphingomyelinase (SMase), exhibiting an IC50 value of 6.43 µM against B. cereus SMase. In addition to its primary activity, SMase-IN-1 also demonstrates a significant inhibition rate of 59.50% for equine butyrylcholinesterase (eqBuChE) at a concentration of 50 µM. This compound forms a complex with Cu2+ in biometal interactions and effectively reduces hemolysis induced by B. cereus in sheep erythrocytes. SMase-IN-1 is valuable for research in microbial pathogenesis and enzyme inhibition studies.
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Synonyms: HSR803-d6 free base
Itopride-d6 is a deuterated form of Itopride, a potent dopamine D2 receptor antagonist and acetylcholinesterase (AChE) inhibitor. Its unique stable isotope labeling allows for advanced metabolic and pharmacokinetic studies. Itopride enhances gastric motility through its combined antidopaminergic and anti-AChE actions, making it valuable in research applications focused on gastrointestinal prokinetics and conditions such as gastro-esophageal reflux disease (GERD).
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Synonyms: Temefos
Temephos is an organophosphate insecticide that functions as an irreversible inhibitor of acetylcholinesterase (AChE). This inhibition leads to cholinergic overactivation, effectively disrupting the larval development of Aedes aegypti and Aedes albopictus, making it a valuable tool in research concerning Dengue Virus, Zika Virus, and other mosquito-borne pathogens. While exhibiting important biological activity, Temephos has been shown to cause genotoxicity, neurodevelopmental toxicity, and potential liver and reproductive system effects in mammals. Additionally, it can accumulate in adipose tissues and aquatic organisms, with its metabolism primarily occurring through oxidation and hydrolysis. Temephos serves as a critical reagent in studies of vector control and viral transmission dynamics.
