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Catalog No.
Product Name
Application
Product Information
Citations
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MAO-B/Acetylcholinesterase Inhibitor
MAO-B-IN-26 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase, demonstrating neuroprotective properties against β-amyloid (Aβ) induced cytotoxicity in SH-SY5Y cells. This compound effectively mitigates morphological alterations, reactive oxygen species (ROS) generation, and membrane damage associated with neurodegeneration. Additionally, MAO-B-IN-26 suppresses Aβ-induced autophagy and apoptosis, making it a valuable tool for research focused on therapeutic strategies for Alzheimer's disease. -
BChE Inhibitor
Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor (IC50 = 12.96 μg/mL) with additional multi-target mechanisms including inhibition of NF-κB, MAPK, NLRP3 inflammasome activation, and modulation of the Nrf2/ARE pathways. This compound demonstrates significant anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin is suitable for research applications related to inflammatory diseases, osteoporosis, diabetes, and neurodegenerative disorders such as Alzheimer's disease. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1), exhibiting IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM, respectively. This compound demonstrates significant binding affinity for the peripheral anionic site of AChE, facilitates brain penetration, and shows potential in disrupting amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-1 exhibits neuroprotective properties against Aβ-induced stress and possesses promising antioxidant activity, making it a valuable tool for Alzheimer's disease research and related neurodegenerative studies. -
AChE/BChE Inhibitor
AChE/BChE-IN-9 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 5.74 μM and 14.05 μM, respectively. In addition to its enzymatic inhibition, AChE/BChE-IN-9 demonstrates antioxidant properties with an IC50 of 57.35 μM and has the ability to chelate iron, potentially mitigating oxidative stress. This compound also influences the aggregation of amyloid β1-42, making it relevant for research in neurodegenerative diseases and gerontology. Its capacity to cross the blood-brain barrier further enhances its suitability for studies focused on central nervous system disorders. -
AChE/GSK-3β Inhibitor
AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-2 is a potent oral inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), exhibiting IC50 values of 0.069 μM, 0.127 μM, and 0.097 μM, respectively. This compound demonstrates significant binding affinity to the peripheral anionic site of AChE, high brain permeability, and the ability to disassemble amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-2 provides neuroprotective effects against Aβ-induced stress and possesses noteworthy antioxidant properties, making it suitable for research in neurodegenerative disease models. -
AChE/BChE Inhibitor
AChE-IN-14 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), displaying IC50 values of 0.46 μM for electric eel AChE, 0.48 μM for human recombinant AChE, and 0.44 μM for equine serum BChE. In addition to its cholinesterase inhibition, AChE-IN-14 has a high affinity for the human H3 receptor (H3R) with a Ki value of 159.8 nM. This compound is particularly relevant for research focused on neurodegenerative diseases such as Alzheimer’s disease, where the modulation of cholinergic signaling is critical. -
Multitarget Inhibitor
SSZ is a multitarget inhibitor that engages multiple pathological mechanisms associated with Alzheimer's disease (AD). It inhibits key enzymes including acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. Research demonstrates that SSZ enhances cognitive function and provides neuroprotective effects in murine models of Alzheimer's disease, making it a valuable tool for studying therapeutic strategies in neurodegenerative disorders. -
AChE/IL-6 Inhibitor
Y13g is a potent dual inhibitor of acetylcholinesterase (AChE) and interleukin-6 (IL-6). By targeting these pathways, Y13g demonstrates significant potential in addressing memory deficits associated with Alzheimer’s Disease. In preclinical studies, Y13g effectively reverses memory impairment induced by STZ and exhibits histopathological profiles akin to those of healthy specimens, making it a valuable tool for research in neurodegeneration and inflammatory responses.
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BChE/p38-α MAPK Inhibitor
BChE/p38-α MAPK-IN-1 is a selective dual inhibitor targeting human butyrylcholinesterase (BChE) with an IC50 of 772 nM and p38 α MAPK with an IC50 of 191 nM. This compound significantly reduces the production of pro-inflammatory cytokines such as IL-1β, IL-6, IL-8, and TNF-α in cellular models. BChE/p38-α MAPK-IN-1 demonstrates the potential to ameliorate cognitive impairments induced by scopolamine and alleviate spatial learning deficits in LPS-treated mice, making it a valuable tool for studying Alzheimer's disease by addressing cholinergic deficits and neuroinflammation. -
AChE/ACP/ALP Inhibitor
Trimyristin is a potent inhibitor of acetylcholinesterase (AChE) as well as acid and alkaline phosphatase (ACP/ALP). It has demonstrated significant inhibitory effects on AChE, ACP, and ALP activities in the nervous tissue of Lymnaea acuminata, with IC50 values of 0.11 mM, 0.16 mM, and 0.18 mM, respectively. This compound is valuable for research applications focused on neurological pathways and enzyme activity modulation. -
AChE Inhibitor
Propoxur is a reversible competitive inhibitor of acetylcholinesterase (AChE) that effectively penetrates the blood-brain barrier. This compound induces neurotoxicity by inhibiting AChE activity, resulting in the accumulation of acetylcholine, thereby causing neurological dysfunction. In addition, Propoxur promotes MMP-2 expression and enhances tumor cell migration and invasion through the generation of reactive oxygen species (ROS) and the activation of the ERK/Nrf2 signaling pathway. It is also utilized as a carbamate insecticide for managing pests in turf, forestry, and household environments. -
AChE/BChE Inhibitor
Epiberberine chloride is an alkaloid derived from Coptis chinensis, functioning primarily as a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 1.07 μM and 6.03 μM, respectively. This compound also serves as a non-competitive inhibitor of BACE1, with an IC50 of 8.55 μM. In addition to its cholinesterase inhibition, Epiberberine chloride exhibits antioxidant properties, demonstrated by its ability to scavenge peroxynitrite (IC50 of 16.83 μM), suggesting a potential protective role in Alzheimer’s disease research. Furthermore, it inhibits the early differentiation of 3T3-L1 preadipocytes and downregulates key signaling pathways, indicating its relevance in studies on diabetes. -
Aβ/tau Aggregation Inhibitor
Aβ/tau aggregation-IN-4 is a potent inhibitor of amyloid-beta (Aβ) and tau aggregation. It effectively promotes the degradation of Aβ40 and Aβ42 with IC50 values of 2.151 μM and 3.622 μM, respectively. Additionally, Aβ/tau aggregation-IN-4 exhibits selective inhibition of acetylcholinesterase (AChE) with an IC50 of 5.56 μM, and inhibits monoamine oxidase A (MAO-A) and B (MAO-B) with IC50 values of 0.59 μM and 0.09 μM, respectively. This compound also reduces intracellular reactive oxygen species (ROS) levels, making it a valuable tool in Alzheimer's disease research. -
MAO-B Inhibitor
MAO-B-IN-7 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE), demonstrating IC50 values of 41 nM for human AChE, 87 nM for electric eel AChE, and 0.3 μM for MAO-B. This compound is notable for its ability to penetrate the blood-brain barrier, making it suitable for central nervous system research. MAO-B-IN-7 has been shown to mitigate oxidative stress and neuroinflammation, supporting its potential applications in neurodegenerative disease studies. -
Pancreatic Lipase/Acetylcholinesterase/Glutamic-oxaloacetic Transaminase 1/Alpha-glucosidase Inhibitor
Aspulvinone H is a potent inhibitor targeting pancreatic lipase, acetylcholinesterase, glutamic-oxaloacetic transaminase 1 (GOT1), and α-glucosidase, with IC50 values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It demonstrates key biological activities including inhibition of cancer cell proliferation, disruption of glutamine metabolism, and induction of apoptosis in cancer cells. Additionally, Aspulvinone H lowers postprandial blood glucose levels in mice and exhibits antibacterial properties against Staphylococcus aureus. This compound is suitable for research into pancreatic ductal adenocarcinoma, diabetes management, and infectious diseases caused by Staphylococcus aureus. -
Cholinesterase (ChE) Inhibitor
Sophoflavescenol is a prenylated flavonol that acts as a cholinesterase (ChE) inhibitor, demonstrating potent inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 10.98 μM and 8.21 μM, respectively. Additionally, it shows significant inhibition of other enzymes, including RLAR, HRAR, and BACE1. This compound is primarily utilized in research related to neurodegenerative diseases and cognitive function enhancement, making it a valuable reagent for studying cholinergic pathways. -
p38α MAPK/BChE Inhibitor
ARRY-371797 is a potent and orally bioavailable inhibitor of p38α MAPK and butyrylcholinesterase (BChE), demonstrating IC50 values of 12.0 µM for p38α MAPK and 0.13 µM for BChE, with minimal activity against human acetylcholinesterase (hAChE). This compound shows promise for research applications in Alzheimer’s disease, particularly in the context of neuroinflammation and cholinergic system modulation. -
AChE/hCA Inhibitor
AChE/hCA I-IN-1 is a selective inhibitor of acetylcholinesterase (AChE) and human carbonic anhydrases (hCA I and hCA II). It demonstrates potent inhibition with IC50 values of 302 nM for AChE, 265 nM for hCA I, and 283 nM for hCA II. This compound is valuable for research applications exploring neurodegenerative disorders and the regulation of physiological pH balance. -
AChE/hCA Inhibitor
AChE/hCA I/II-IN-1 is a potent inhibitor of acetylcholinesterase (AChE) and human carbonic anhydrases I and II (hCA I/II), demonstrating IC50 values of 22.21 nM for AChE, and 60.79 nM and 66.64 nM for hCA I and II, respectively. This compound is valuable for research applications related to glaucoma, Alzheimer’s disease, and diabetes, providing insights into the modulation of these critical enzymatic targets. -
hCA I/II Inhibitor
hCAI/II-IN-5 is a potent inhibitor of human carbonic anhydrase isoenzymes I and II, exhibiting IC50 values of 37.88 nM and 45.23 nM, respectively. Additionally, it demonstrates inhibitory activity against α-Glycosidase and acetylcholinesterase (AChE) with IC50 values of 48.98 nM and 420.14 nM. This compound is valuable for research applications in various diseases, including diabetes, Alzheimer's disease, heart failure, ulcers, and epilepsy. -
CA/ChE Inhibitor
hCA I-IN-4 is an inhibitor of carbonic anhydrase (CA) and cholinesterase (ChE), demonstrating potent inhibitory activity against hCA I, hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) with Ki values of 29.94 nM, 17.72 nM, 21.21 nM, and 7.65 nM, respectively. This compound also exhibits cytotoxic effects in BT-549 cancer cells, with an IC50 value of 16.59 μM. hCA I-IN-4 is valuable for research involving enzyme regulation and cancer therapeutics. -
α-GLY Inhibitor
α-Glycosidase-IN-1 is a selective inhibitor of α-glycosidase (α-GLY), exhibiting a potent IC50 of 44.72 nM and a KI of 41.74 nM. Additionally, it demonstrates inhibitory activity against human carbonic anhydrase isoenzymes I and II, as well as acetylcholinesterase, with IC50 values of 104.87 nM, 100.04 nM, and 654.87 nM, respectively. This compound is valuable for research into various conditions, including diabetes, Alzheimer’s disease, heart failure, ulcers, and epilepsy. -
hCAI/II Inhibitor
hCAI/II-IN-8 is a hydrazide derivative that serves as a selective inhibitor of human carbonic anhydrase isomerases I and II, with IC50 values of 21.35 ± 0.39 nM and 7.12 ± 0.12 nM, respectively. In addition to its primary target, hCAI/II-IN-8 also demonstrates inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 46.27 ± 0.75 nM and 43.38 ± 0.83 nM, respectively. This compound is relevant for studies involving enzyme inhibition and has potential applications in understanding neurodegenerative diseases and carbonic anhydrase-related pathologies. -
AChE/BChE Inhibitor
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. -
AChE/BChE Inhibitor
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. -
AChE Inhibitor
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. -
AChE/BACE1/GSK3β Inhibitor
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. -
AChE/GSK-3β Inhibitor
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. -
AChE/GSK-3β Inhibitor
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. -
hAChE/hBuChE Inhibitor
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. -
ACE Inhibitor
Ovotransferrin (328-332) is an Angiotensin-Converting Enzyme (ACE) inhibitor that demonstrates protective effects on blood pressure, with an IC50 of 20 μM. Additionally, this fragment exhibits activity against Cholinesterase (ChE), highlighting its potential relevance in Alzheimer's disease research. Its dual inhibitory mechanisms make it a valuable tool for studying cardiovascular health and neurodegenerative disorders. -
Cholinesterase (ChE) Inhibitor
(-)-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. -
Bacterial Inhibitor
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. -
Antioxidant/Antimicrobial Agent/Cholinesterase Inhibitor
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. -
AChE Inhibitor
Coumaran, also known as 2,3-Dihydrobenzofuran, is an inhibitor of acetylcholinesterase (AChE) and exhibits notable antileishmanial activity. Its mechanisms include the activation of macrophages, contributing to its antiparasitic effects and immunomodulatory properties. Coumaran is also applicable in the field of biopesticides, providing a potential tool for agricultural and biological research. -
ChE Inhibitor
N-p-trans-Coumaroyltyramine is a natural phenolic amide compound that acts as an inhibitor of acetylcholinesterase (AChE) with an IC50 of 122 μM and α-glucosidase with an IC50 of 2.7 μM. It demonstrates significant anti-trypanosomal activity, exhibiting an IC50 of 13.3 µM against Trypanosoma brucei rhodesiense. This compound is valuable for research into neurodegenerative diseases such as Alzheimer's disease, as well as for studies focusing on trypanosomiasis. -
Parasite Inhibitor
Diazinon is an irreversible acetylcholinesterase (AChE) inhibitor with primary applications in pest control as an insecticide. By inhibiting AChE, Diazinon leads to the accumulation of acetylcholine, resulting in overstimulation of acetylcholine receptors and disruption of nervous system function. Additionally, Diazinon generates reactive oxygen species (ROS), contributing to oxidative stress across various biological tissues. This compound is predominantly utilized in agricultural settings but may also hold implications for human and animal health research. -
AChE Inhibitor
Carbosulfan is an orally active acetylcholinesterase (AChE) inhibitor that hydrolyzes to carbofuran, leading to significant insecticidal properties. This compound demonstrates broad-spectrum insecticidal activity while inducing oxidative stress through increases in lipid peroxidation and impairment of antioxidant defenses. Carbosulfan is associated with reproductive toxicity in male rats and developmental disorders in offspring, making it a relevant subject in studies focused on reproductive toxicity and environmental risk assessment. Its persistence in aquatic environments raises concerns regarding potential hazards to non-target organisms. -
Parasite Inhibitor
8-Deoxygartanin, a prenylated xanthone derived from Garcinia mangostana, serves as a selective inhibitor of butyrylcholinesterase (BChE). This compound demonstrates significant antiplasmodial activity, with an IC50 value of 11.8 μM against the W2 strain of Plasmodium falciparum. Additionally, 8-Deoxygartanin inhibits NF-κB (p65) activation, displaying an IC50 of 11.3 μM, making it a valuable reagent for research in parasitic infections and inflammation pathways. -
Cholinesterase (ChE) Inhibitor
Fenchlorphos is an organophosphate compound that acts as a potent inhibitor of acetylcholinesterase (AChE), an important enzyme in cholinergic signaling. By disrupting AChE activity, Fenchlorphos leads to the accumulation of acetylcholine, resulting in increased cholinergic neurotransmission. Additionally, this compound has been shown to induce mitochondrial dysfunction, making it a valuable tool for research on neurobiology and toxicology. Its applications include studies on the mechanisms of insecticide action and investigations into the impacts of cholinergic inhibition on cellular metabolism. -
Parasite Inhibitor
Phosalone is an organophosphate insecticide that primarily targets acetylcholinesterase, leading to the inhibition of neurotransmission in parasites. Its potent biological activity makes it effective in controlling a wide range of insect pests. Phosalone is utilized in entomological research and in studies focusing on pest management strategies and the biochemical pathways of insecticide resistance. -
ChE Inhibitor
Isogarcinol is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 1.13 μM and 8.30 μM, respectively. This compound also demonstrates significant leishmanicidal activity, with an IC50 of 0.33 μM against Leishmania donovani. Isogarcinol's dual action makes it a valuable tool for research in neurodegenerative disorders and parasitic diseases. -
AChE Inhibitor
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. -
SMase Inhibitor
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. -
AChE/Dopamine 2 Inhibitor
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. -
BChE Inhibitor/CB2R Agonist
hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation. -
Topoisomerase I Inhibitor
RPR121056 is a topoisomerase I inhibitor that functions as a metabolite of the chemotherapy agent Irinotecan (CPT-11), produced by the enzyme CYP3A4. This compound induces cell death by disrupting DNA replication, making it relevant for cancer research, particularly in the context of colorectal cancer treatment. Additionally, RPR121056 demonstrates direct inhibition of acetylcholinesterase (AChE), further expanding its potential applications in pharmacological studies. -
COX-2 Inhibitor
COX-2-IN-22 is a selective inhibitor of Cyclooxygenase-2 (COX-2) with an IC50 of 8.6 µM. In addition to its primary activity, COX-2-IN-22 also exhibits inhibitory effects on Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), β-Secretase, Lipoxygenase-5 (LOX-5), and DPPH, with IC50 values of 2.8 µM, 6.3 µM, 15.3 µM, 13.9 µM, and 6.8 µM, respectively. This compound is capable of crossing the blood-brain barrier, making it a valuable tool for research in neuroinflammatory and neurodegenerative disease models. -
μ-Opioid Receptor Agoinst/AChE Inhibitor
Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling.
