AChE

Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM.

Donepezil is a noncompetitive acetylcholineesterase inhibitor, which can readily cross the blood brain barrier and increase the concentration of cortical acetylcholine. It is known that Donepezil is a useful tool in the study of Alzheimer's disease.

Rivastigmine tartrate is a dual cholinesterase inhibitor (ChEI). It inhibits both butyrylcholinesterase (BChE) and acetylcholinesterase (AChE).

Desoxypeganine hydrochloride is an AChE (acetylcholinesterase) inhibitor that has been used in the treatment of Alzheimer's dementia.

Rivastigmine, an cholinesterase inhibitor(IC50= 5.5 uM), inhibits both butyrylcholinesterase and acetylcholinesterase.

Pulegone is a monoterpene compound found in a number of essential oils. The unit of Product is ml.

Polygalacic acid (Virgaureagenin G) is a triterpenoid isolated from the root of Polygala tenuifolia Willd that inhibits MMP expression. Polygalacic acid (Virgaureagenin G) can significantly improve the responsiveness of the cholinergic system, such as decreased acetylcholinesterase (AChE) activity, increased choline acetyltransferase (ChAT) activity, and increased acetylcholine (ACh) levels in the hippocampus and frontal cortex. Polygalacic acid (Virgaureagenin G) can also inhibit IL-1β-induced Wnt/β-catenin activation and mitogen-activated protein kinase (MAPK) signaling pathways in chondrocytes, and is used in osteoarthritis (OA) related research

Pitofenone hydrochloride is an antispasmodic agent. It acts as a potent inhibitor of acetylcholinesterase activity.

Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively).

Azamethiphos is an organothiophosphate insecticide. It is a veterinary drug used in Atlantic salmon fish farming to control parasites.

Pralidoxime iodide is a Cholinesterase Reactivator.

Nerolidol is a synthetic AChE inhibitor and F0F1-ATP synthase modulator. It acts as a sedative, inhibits growth of bacteria and fungi, and decreases the mitochondrial transmembrane electric potential to induce cell death in hepatocarcinoma cells.

Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.

Drofenine hydrochloride is a potent competitive inhibitor of BChE, and the ki values of Drofenine is calculated to be 3 uM.

Edrophonium Chloride, also known as Tensilon, is an acetylcholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. Edrophonium Chloride has also been used as an antidote to curare principles.

Malathion is an organophosphorous compound that inhibits cholinesterase enzyme activity. Malathion is an organophosphate insecticide of relatively low human toxicity.

Acotiamide is a drug approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia.

Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.

TAE-1 is an inhibitor of amyloid-β fibril formation and aggregation. TAE-1 inhibits cholinesterases AChE and BuChE with IC50 of 0.3 μM and 3.9 μM, respectively.

Timosaponin AIII is a potent Inhibitor of U46619-induced Rat Platelet Aggregation, Selectively Inhibiting TxA2-induced Platelet Activation, Preferably Suppressing TP-mediated Activation of Gq, not G12/13, Signaling Pathways.

Flavone (2-Phenylchromone, 2-Phenyl-4-chromone, 2-Phenyl-4-benzopyron), a class of flavonoids, mainly found in spices and red or purple plant foods with antioxidant, anti-proliferative, anti-tumor, anti-microbial, estrogenic, acetyl cholinesterase, anti-inflammatory activities and are also used in cancer, cardiovascular disease, neurodegenerative disorders etc.

(+)-Phenserine is a novel selective cholinesterase noncompetitive inhibitor with an IC50 of 45.3 μM.

(±)-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).

Aldicarb sulfone(Temik sulfone) is a carbamate insecticide; is a cholinesterase inhibitor which prevents the breakdown of acetylcholine in the synapse.

(R)-Rivastigmine D6 (tartrate) is the deuterium labeled (R)-Rivastigmine, which is an cholinesterase inhibitor.

MHP 133 is a drug 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.

BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM.

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.

(+)-Corynoline is an acetylcholinesterase inhibitor isolated from Corydalis incisa.

Lactupicrin, a sesquiterpene lactone, primarily targets acetylcholinesterase (AChE), exhibiting an inhibitory activity with an IC50 of 150.3 μM. This compound demonstrates notable analgesic, sedative, and antimalarial effects, alongside its atheroprotective properties. Lactupicrin is an orally active bitter compound, making it valuable for research applications focused on neuropharmacology and cardiovascular health.

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-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-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.

Methiocarb is an orally active carbamate insecticide primarily targeting acetylcholinesterase to induce cholinergic excitation. It exhibits dose-dependent toxic effects on various organisms, including notable oxidative stress through lipid peroxidation in liver, kidney, brain, and testicular tissues, while also altering reduced glutathione levels via reactive oxygen species generation. This compound is utilized for agricultural pest control and serves as a valuable research tool for studying oxidative stress-related cellular damage in mammalian models.

Propoxur-d3 is the deuterated form of Propoxur, a reversible and competitive acetylcholinesterase (AChE) inhibitor. It crosses the blood-brain barrier and exerts neurotoxic effects by inhibiting AChE activity, leading to increased acetylcholine levels and resultant neurological dysfunction. Additionally, Propoxur-d3 promotes the expression of matrix metalloproteinase-2 (MMP-2) and enhances tumor cell migration and invasion through the generation of intracellular reactive oxygen species (ROS) and the activation of the ERK/Nrf2 signaling pathway. This compound has applications in neurotoxicity studies and cancer research, as well as in assessing pesticide effects in ecological studies.

Propoxur-d7 is the deuterium-labeled analog of Propoxur, a reversible and competitive inhibitor of acetylcholinesterase (AChE). This compound exhibits significant neurotoxic effects by inhibiting AChE activity, leading to increased levels of acetylcholine and subsequent neurological dysfunction. Propoxur-d7 also enhances tumor cell migration and invasion through the promotion of matrix metalloproteinase-2 (MMP-2) expression, driven by reactive oxygen species (ROS) generation and activation of the ERK/Nrf2 signaling pathway. Additionally, Propoxur serves as a carbamate insecticide effective against a variety of pests in turf, forestry, and household settings.

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.

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.

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.

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.

Trimyristin-d15 is a deuterium-labeled derivative of Trimyristin, a naturally occurring compound extracted from Myristica fragrans. This reagent effectively inhibits acetylcholinesterase (AChE), as well as acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata, with IC50 values of 0.11 mM, 0.16 mM, and 0.18 mM, respectively. Trimyristin-d15 serves as a valuable tool for biochemical research and enzyme activity studies, particularly in exploring the mechanisms of neurotoxicity and molluscicidal action.

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.

Galanthamine-O-methyl-d3 is a deuterium-labeled derivative of Galanthamine, a potent inhibitor of acetylcholinesterase (AChE) with an IC50 value of 500 nM. This stable isotope-labeled compound is primarily utilized in pharmacokinetic and metabolic studies. It serves as a valuable tool for investigating the pharmacological dynamics and biochemical pathways associated with cholinergic activity.

Carbaryl-d7 is a deuterium-labeled derivative of Carbaryl, which functions as an acetylcholinesterase inhibitor. By suppressing the breakdown of acetylcholine in the synaptic cleft, Carbaryl-d7 leads to an accumulation of acetylcholine, potentially resulting in neurotoxic effects. This stable isotope is primarily utilized in chemical research to study the enzymatic action and biological effects of Carbaryl and its derivatives.

Galanthamine-d3 hydrochloride is a deuterium-labeled derivative of Galanthamine, primarily used as a stable isotope. This compound serves as a useful tool in pharmacokinetic studies and metabolic research, enabling the investigation of drug metabolism and distribution. Galanthamine-d3 hydrochloride plays a significant role in understanding the mechanisms of action of acetylcholinesterase inhibitors and their effects on neurological processes.

Lanuginosine is an alkaloid with demonstrated anticancer activity. It induces apoptosis and inhibits acetylcholinesterase (AChE) with an IC50 of 10.9 μM, in addition to preventing amyloid-beta (Aβ) aggregation. This compound exhibits potent anticancer effects against various malignancies, including hepatocellular carcinoma, human promyelocytic leukemia, chronic myeloid leukemia, melanoma, and brain tumors. Lanuginosine is also valuable for research related to Alzheimer's disease and its therapeutic strategies.

Carbaryl-d3 is a deuterium-labeled variant of Carbaryl, characterized as an acetylcholinesterase inhibitor. This compound prevents the breakdown of acetylcholine in the synaptic cleft, resulting in its accumulation and subsequent neurotoxic effects. Carbaryl-d3 is employed in research related to neurotoxicity mechanisms and may serve as a tool for studying the pharmacokinetics and metabolic pathways of Carbaryl. Its stable isotope labeling enhances analytical precision in experimental applications.

Pamiparib maleate is a highly potent and selective inhibitor of poly (ADP-ribose) polymerase (PARP), targeting apoptotic pathways. This compound effectively penetrates the blood-brain barrier, inducing neurotoxicity manifesting as cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos. It regulates critical enzymes such as acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase), leading to increased oxidative stress that triggers apoptosis and affects the expression of neurodevelopment-related genes. Additionally, pamiparib maleate downregulates the Notch signaling pathway, providing insights into its potential neurotoxic effects during embryonic development and its relevance in neuropharmacology research.

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.

Diallyl tetrasulfide functions as an antioxidant, primarily by mitigating cadmium-induced neurotoxicity and oxidative liver injury. This compound has demonstrated the ability to regulate acetylcholinesterase and adenosine triphosphatase activities, as well as protect against oxidative stress in the brain and liver tissues of animal models. Diallyl tetrasulfide also inhibits lipid peroxidation and reduces reactive oxygen species (ROS) production, thereby enhancing cell viability and decreasing apoptosis. It is a valuable reagent for studies focused on cadmium-induced cellular damage and neuroprotection.