-
CaMKIIδ Inhibitor
CaMKIIδ-IN-1 is a potent inhibitor of calcium/calmodulin-dependent protein kinase II delta (CaMKIIδ) with an IC50 of 12 nM. This pyrimidine-based compound is valuable for studying the role of CaMKIIδ in various cellular processes, including synaptic plasticity and cardiac function. Its selective inhibition makes it a useful tool for investigating the biochemical pathways regulated by CaMKIIδ in both physiological and pathological contexts. -
CaMKK Inhibitor
TIM-063 is a selective, cell-permeable CaMKK inhibitor that functions as an ATP-competitive antagonist, specifically targeting the catalytic domain of CaMKK. It exhibits Ki values of 0.35 μM for CaMKKα and 0.2 μM for CaMKKβ, with corresponding IC50 values of 0.63 μM and 0.96 μM. This compound is useful for exploring CaMKK-mediated signaling pathways and evaluating its potential therapeutic applications in various cellular models. -
CaMKIIα Inhibitor
CaMKIIα-IN-1 is an orally active inhibitor of calcium/calmodulin-dependent protein kinase II alpha (CaMKIIα), exhibiting a dissociation constant (KD) of 219 nM for the wild-type hub. This compound demonstrates good metabolic stability, making it suitable for in vivo studies. It can be utilized in research focused on CaMKIIα-mediated pathways, with applications in understanding neurological diseases and cellular signaling mechanisms. -
CaMKIIα inhibitor
HOCPCA is a selective inhibitor of CaMKIIα, a key regulator of calcium-dependent signaling pathways. This compound exhibits neuroprotective properties, enhancing sensorimotor functions and promoting hippocampal neuronal activity following experimental stroke in murine models. It effectively modulates abnormal CaMKII signaling, normalizes Thr286 autophosphorylation post-ischemia, and downregulates specific active CaMKII fragments associated with ischemic conditions. Additionally, HOCPCA demonstrates superior binding affinity to the GHB site, alongside excellent blood-brain barrier permeability, making it a valuable tool for research into neuroprotection and cognitive function. -
CaMKII Inhibitor
CaMKII-IN-3 is a potent inhibitor of Calcium/Calmodulin-dependent protein kinase II (CaMKII), demonstrating an IC50 of less than 10 nM. This compound is valuable in research focused on the role of CaMKII in cardiac function and related heart diseases. Its application may provide insights into disease mechanisms and potential therapeutic strategies. -
CaMKII Inhibitor
Protein kinase inhibitor 8 (Compound CK59) is a selective inhibitor of calmodulin-dependent protein kinase II (CaMKII). This compound effectively reduces cytotoxicity induced by perfluorooctane sulfonic acid (PFOS) and mitigates the downregulation of GLT-1 expression, leading to decreased neuronal damage. Protein kinase inhibitor 8 is a valuable tool for research into neurodegenerative diseases and the molecular mechanisms underlying neuronal stress responses. -
Acetylcholinesterase Inhibitor
TAK-802 is a potent orally active inhibitor of acetylcholinesterase, a key enzyme in neurotransmitter regulation. This compound demonstrates significant nonlinear pharmacokinetics, with its distribution in red blood cells showing concentration-dependent behavior. TAK-802 is primarily utilized in research applications focused on neurodegenerative disorders and cognitive function enhancement. -
Transporter Inhibitor
Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU), exhibiting a Ki value of 25 nM. It acts as a neuromuscular blocking agent by inhibiting both the synthesis and release of acetylcholine (ACh). Hemicholinium 3 demonstrates key biological activities, including the inhibition of Epibatidine-induced contraction and [3H]acetylcholine release, with IC50 values of 897 nM and 693 nM, respectively. This compound is useful in research applications focused on neurotransmitter modulation and neuromuscular transmission studies. -
BuChE inhibitor
Iso-OMPA (Tetraisopropyl pyrophosphoramide) is a selective inhibitor of butyrylcholinesterase (BuChE), functioning through irreversible inhibition. This compound is primarily utilized in research to investigate the mechanisms of BuChE and the resulting effects on acetylcholine metabolism. Iso-OMPA has been shown to enhance soman toxicity in rat models, linked to the inhibition of plasma carboxylesterase (CarbE), making it a valuable tool in studies of nerve agent effects and cholinergic signaling. -
Cholinesterase (ChE) Inhibitor
Physostigmine salicylate is a reversible acetylcholinesterase (AChE) inhibitor that effectively crosses the blood-brain barrier, enhancing central cholinergic neurotransmission. It has demonstrated the ability to reverse memory deficits in transgenic mice models of Alzheimer's disease, making it a valuable tool in neurodegeneration research. Additionally, Physostigmine salicylate serves as an antidote for anticholinergic poisoning, highlighting its significance in pharmacological studies and therapeutic applications. -
AChE Inhibitor
Tacrine is a potent acetylcholinesterase (AChE) inhibitor, with an IC50 value of 109 nM. This compound is recognized for its ability to ameliorate cognitive deficits, particularly in aged rodent models. Additionally, Tacrine is associated with potential hepatotoxicity and is frequently utilized in research focusing on Alzheimer's disease and related neurodegenerative disorders. -
Cholinesterase (ChE) Inhibitor
Chavicol, a cholinesterase (ChE) inhibitor, demonstrates potent inhibition of acetylcholinesterase, with an IC50 of 7.42 μM. This compound exhibits anti-cancer properties, effectively suppressing the growth, survival, migration, and invasion of various cancer cell lines. Notably, Chavicol shows significant cytotoxic effects, evidenced by a notable concentration of approximately 31 μg/mL in A-549 cells. Its dual activities underscore its potential utility in cancer research and therapeutic development. -
Cholinesterase (ChE) Inhibitor
Physostigmine hemisulfate is a reversible inhibitor of acetylcholinesterase (AChE), effectively enhancing cholinergic neurotransmission by crossing the blood-brain barrier. This compound has demonstrated the ability to reverse cognitive deficits in transgenic mouse models of Alzheimer's disease, making it a valuable tool for neurological research. Additionally, Physostigmine hemisulfate serves as an antidote for anticholinergic poisoning, underscoring its significance in pharmacological studies and clinical applications. -
Acetylcholinesterase Inhibitor
N-Boc-4-piperidinemethanol is an acetylcholinesterase (AChE) inhibitor that serves as a valuable tool for neurological research. It is particularly relevant in studies focused on Alzheimer's Disease, aiding in the investigation of cholinergic dysfunction. This compound may contribute to the development of therapeutic strategies targeting AChE activity. -
CYP2D6/AChE Inhibitor
Rhodiosin is a dual inhibitor of CYP2D6 and acetylcholinesterase (AChE), extracted from the root of Rhodiola rosea. It exhibits an IC50 value of 0.761 μM for CYP2D6 and a Ki of 0.769 μM. This compound demonstrates notable antioxidant and neuroprotective properties, contributing to the regulation of the HIF-1α signaling pathway, which is vital for central nervous system protection. Rhodiosin serves as a valuable tool for research in neuropharmacology and metabolic studies. -
Cholinesterase (ChE) Inhibitor
Violanthin is a cholinesterase (ChE) inhibitor derived from the stems of Dendrobium officinale. It exhibits significant antioxidant and antibacterial properties, making it a valuable compound for biological research. Violanthin effectively inhibits acetylcholinesterase (AChE) with an IC50 value of 79.80 μM, indicating its potential application in studies related to neurodegenerative diseases and cholinergic signaling. -
AChE Inhibitor
AChE-IN-84 is a potent inhibitor of acetylcholinesterase (AChE), a key enzyme responsible for the hydrolysis of the neurotransmitter acetylcholine. This compound demonstrates significant biological activity in modulating cholinergic signaling pathways, making it an essential tool for studying neurodegenerative diseases such as Alzheimer's. AChE-IN-84 is useful in research applications focusing on cognitive enhancement and synaptic function restoration. -
Cholinesterase (ChE) Inhibitor
Phenthoate is a cholinesterase (ChE) inhibitor that functions primarily as an organophosphorus pesticide. This compound demonstrates low toxicity in animals while effectively inhibiting acetylcholinesterase (AChE), which can provide insights into neurotoxicity and enzyme regulation. Phenthoate is widely used in research applications examining the biochemical pathways of neurotransmission and potential environmental impacts of pesticide exposure. -
AChE/BchE Inhibitor
ACG548B is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 1.78 µM and 0.496 µM, respectively. It exhibits strong affinity and selectivity for AChE over BChE and choline kinase (ChoK). ACG548B is suitable for research applications focused on myasthenia gravis and the mechanisms of neuromuscular blockade. -
AChE Inhibitor
Pseudocoptisine chloride is a quaternary alkaloid derived from the benzylisoquinoline structure, isolated from Corydalis tuber. This compound functions as an acetylcholinesterase (AChE) inhibitor, demonstrating an IC50 of 12.8 μM. Pseudocoptisine chloride exhibits notable anti-inflammatory and anti-amnestic properties, making it a valuable reagent for research related to neurodegenerative diseases and cognitive function studies. -
Cholinesterase (ChE) Inhibitor
Dehydronuciferine acts as an inhibitor of cholinesterase, specifically targeting acetylcholinesterase (AChE) with an IC50 value of 25 μg/mL. This compound is derived from the leaves of Nelumbo nucifera (lotus) and demonstrates potential in research applications related to neurodegenerative diseases and cognitive disorders. Its ability to modulate cholinergic signaling makes it a valuable tool for studying cholinergic system functions and developing therapeutic strategies. -
Cholinesterase (ChE) Inhibitor
Galanthaminone is a competitive and reversible inhibitor of cholinesterase (ChE), primarily targeting acetylcholinesterase (AChE). This compound demonstrates significant biological activity in enhancing cholinergic transmission and is utilized in the study of mild to moderate Alzheimer's disease and related memory impairments. Its application in research aids in understanding the mechanisms underlying cognitive decline and potential therapeutic interventions. -
Cholinesterase (ChE) Inhibitor
Picfeltarraenin IB is a triterpenoid derived from Picria fel-terrae Lour that acts as a cholinesterase (ChE) inhibitor. This compound exhibits significant biological activity by inhibiting acetylcholinesterase (AChE), thereby modulating cholinergic signaling. It is primarily utilized in research settings focusing on therapeutic applications for herpes infections, cancer, and inflammation. -
Cholinesterase (ChE) Inhibitor
Huperzine B is a Lycopodium alkaloid that acts primarily as a selective inhibitor of acetylcholinesterase (AChE). This compound demonstrates significant potential for enhancing cholinergic neurotransmission, which is crucial in the context of neurodegenerative disorders such as Alzheimer's disease. Research applications include studies focused on cognitive enhancement and memory preservation. -
Dual MAO/AChE Inhibitor
Ladostigil hemitartrate is a dual inhibitor of monoamine oxidase (MAO) and acetylcholinesterase (AChE), with established IC50 values of 37.1 μM for MAO-B and 31.8 μM for AChE. This compound is capable of crossing the blood-brain barrier and exhibits neuroprotective, antioxidant, and anti-inflammatory properties. Ladostigil hemitartrate is relevant for research into neurological disorders, including depression and Alzheimer's disease. Additionally, it functions as a click chemistry reagent, featuring an alkyne group that participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
AChE Inhibitor
Phenoxyacetone is a competitive inhibitor of acetylcholinesterase (AChE), targeting the enzyme responsible for the hydrolysis of the neurotransmitter acetylcholine. By inhibiting AChE, phenoxyacetone enhances cholinergic signaling, making it valuable for studying neurological conditions characterized by impaired neurotransmission. This compound is suitable for research applications focused on neuropharmacology and the exploration of treatments for Alzheimer's disease and other memory-related disorders. -
AChE Inhibitor
Vincosamide is a potent acetylcholinesterase (AChE) inhibitor derived from the extract of Psychotria leiocarpa. It exhibits anti-inflammatory properties, making it a valuable compound for studying neurodegenerative diseases related to cholinergic dysfunction. Research applications include exploring potential therapeutic strategies for conditions such as Alzheimer's disease and other disorders characterized by altered AChE activity. -
Cholinesterase (ChE) Inhibitor
Isoprocarb is a cholinesterase (ChE) inhibitor that functions as a carbamate insecticide. It effectively targets pests such as rice paddy lice and leafhoppers, making it valuable in agricultural research. Its role in inhibiting acetylcholinesterase (AChE) provides insights into neuromuscular function and the mechanisms of toxicity, contributing to studies on pest control and environmental impact assessments. -
BChE Inhibitor
BChE-IN-17 is a potent and selective inhibitor of butyrylcholinesterase (BChE) with IC50 values of 10.5 nM for equivalent BChE and 32.5 nM for human BChE. This compound demonstrates a remarkable over 1000-fold selectivity for BChE compared to acetylcholinesterase (AChE). Additionally, BChE-IN-17 exhibits low neurotoxicity and offers moderate neuroprotective effects, making it a valuable reagent for research in neurodegenerative diseases and cholinergic signaling pathways. -
AChE Inhibitor
Neoeriocitrin, a potent acetylcholinesterase (AChE) inhibitor isolated from Drynaria Rhizome, demonstrates significant biological activity in promoting proliferation and osteogenic differentiation in MC3T3-E1 cells. This compound is valuable for research in neurodegenerative diseases, where AChE inhibition is critical, as well as in studies focused on bone biology and regenerative medicine. -
Cholinesterase Inhibitor
Cyclanoline chloride is a potent cholinesterase inhibitor that disrupts the breakdown of acetylcholine, thereby enhancing cholinergic neurotransmission. This compound is primarily utilized in research applications focusing on neurodegenerative diseases and paralysis, as it contributes to understanding the role of neurotransmitter regulation in synaptic function. Its inhibitory effects on cholinesterase make it a valuable tool for studying cholinergic signaling pathways. -
Cholinesterase (ChE) Inhibitor
9-Acridinecarboxylic acid is a potent cholinesterase (ChE) inhibitor, acting on both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). It serves as a precursor for various derivatives that exhibit nanomolar inhibitory activity. This compound is crucial for research in neurodegenerative diseases and provides insights into the modulation of cholinergic signaling pathways. -
MAO/AChE Inhibitor
Ladostigil hydrochloride is a potent dual inhibitor of acetylcholinesterase (AChE) and monoamine oxidase-B (MAO-B), exhibiting IC50 values of 37.1 µM and 31.8 µM, respectively. This compound demonstrates neuroprotective, antioxidant, and anti-inflammatory properties, making it valuable for research related to depression and Alzheimer's disease. Additionally, Ladostigil hydrochloride functions as a click chemistry reagent, featuring an alkyne group that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating diverse chemical applications. -
Cholinesterase (ChE) Inhibitor
Ebeiedinone is a steroidal alkaloid obtained from Fritillaria species that functions as a cholinesterase (ChE) inhibitor. At a concentration of 0.1 mM, it demonstrates a substantial inhibitory effect of 69.0% on human whole blood cholinesterase activity. This compound is valuable for research involving neuropharmacology and the study of cholinergic signaling pathways. -
AChE Inhibitor
AChE-IN-65 is a mixed inhibitor of acetylcholinesterase (AChE) with a Ki of 556.4 μM, demonstrating potency against the AChE from Electrophorus electricus. This compound is valuable for research applications focused on the modulation of cholinergic signaling and the study of neurodegenerative diseases. AChE-IN-65 can aid in understanding the role of AChE in synaptic transmission and its potential as a therapeutic target. -
AChE Inhibitor
(R)-Donepezil is a specific and potent inhibitor of acetylcholinesterase (AChE). As the R-enantiomer of Donepezil, it demonstrates notable efficacy in enhancing cholinergic neurotransmission. This compound is primarily utilized in neuropharmacological research, particularly in studies related to Alzheimer's disease and other cognitive disorders, where modulation of AChE activity is critical for therapeutic development. -
Cholinesterase (ChE) Inhibitor
Dihydrowithaferin A is a withanolide derived from Withania somnifera, acting primarily as an acetylcholinesterase (AChE) inhibitor. This compound demonstrates significant biological activity by modulating cholinergic transmission, making it useful in research related to neurodegenerative disorders such as Alzheimer’s disease. Its ability to inhibit AChE positions Dihydrowithaferin A as a valuable tool in the exploration of therapeutic approaches targeting cholinergic dysfunction. -
AChE Inhibitor
(S)-Donepezil is an S-enantiomer of Donepezil, serving as a specific and potent inhibitor of acetylcholinesterase (AChE). This compound enhances cholinergic neurotransmission by preventing the degradation of acetylcholine, making it a valuable tool in neuropharmacological research. It is primarily utilized in studies related to neurodegenerative diseases, particularly Alzheimer's disease, where modulation of AChE activity is of significant interest. -
AChE Inhibitor
AChE-IN-23 is a potent acetylcholinesterase (AChE) inhibitor, demonstrating an IC50 value of 48.3 μM. This compound effectively inhibits the breakdown of acetylcholine, thereby enhancing cholinergic signaling. AChE-IN-23 has potential applications in research focused on neurological disorders, including Alzheimer's disease and other conditions associated with cholinergic dysfunction. -
Cholinesterase (ChE) Inhibitor
Isomerazin is a coumarin compound known for its inhibitory effects on cholinesterase (ChE). This compound has demonstrated significant biological activity in the modulation of cholinergic neurotransmission, making it valuable for research into neurodegenerative diseases and cognitive disorders. Its application in studies related to Alzheimer's disease further highlights its potential as a therapeutic agent in cholinergic system-related research. -
Serine Hydrolase Inhibitor
Serine Hydrolase Inhibitor-21 is a potent inhibitor of serine hydrolases, exhibiting a Ki value of 429 nM for butyrylcholinesterase (BuChE). This compound is particularly relevant for research into Alzheimer’s disease, as it may help to elucidate the role of serine hydrolase activity in neurodegeneration. Its mechanism of action may provide insights into potential therapeutic strategies for the treatment of Alzheimer's and related disorders. -
AChE Inhibitor
Zanapezil fumarate is a potent, reversible, and selective inhibitor of acetylcholine esterase (AChE). It exhibits significant inhibition of AChE activity in rat cerebral cortex homogenates, with an IC50 value of 51.2 nM, while also displaying moderate inhibition of muscarinic M1 and M2 receptor binding, with Ki values of 234 and 340 nM respectively. This compound is utilized in research focusing on the early stages of Alzheimer's disease, aiding in the exploration of therapeutic strategies for cognitive decline. -
Cholinesterase Inhibitor
Kuwanon U is a potent cholinesterase inhibitor that demonstrates effective inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 19.69 µM and 10.11 µM, and inhibition constants (Ki) of 6.48 µM and 9.59 µM, respectively. This compound shows promise for research applications concerning Alzheimer’s disease (AD), providing a valuable tool for studying cholinergic function and neurodegeneration. -
AChE Inhibitor
P11149 is a competitive inhibitor of acetylcholinesterase (AChE) that exhibits weak oral bioavailability and the ability to penetrate the blood-brain barrier. With an IC50 of 1.3 μM against rat butyrylcholinesterase (BChE) and AChE, P11149 displays significant cholinergic activity and behavioral efficacy. This Galanthamine derivative is primarily used in research related to Alzheimer's disease, aiding in the exploration of therapeutic strategies for cognitive impairment associated with this neurodegenerative disorder. -
AChE Inhibitor
Galanthamine N-Oxide is an acetylcholinesterase (AChE) inhibitor derived from the bulbs of Zephyranthes concolor. It exhibits a potent inhibitory effect on electric eel AChE with an EC50 value of 26.2 μM. Additionally, Galanthamine N-Oxide effectively hampers substrate accommodation in the active sites of Torpedo californica AChE, human AChE, and human butyrylcholinesterase (hBChE), making it a valuable tool for research in neuropharmacology and cholinergic signaling pathways. -
AChE Inhibitor
O-Desmethyl Galanthamine is an acetylcholinesterase (AChE) inhibitor with an IC50 of 1.83 μM. As a galanthamine-type alkaloid, it effectively modulates cholinergic signaling by preventing the breakdown of acetylcholine. This compound is primarily utilized in research focused on neurodegenerative diseases, including Alzheimer's disease, where AChE inhibition is of therapeutic interest. -
Dual MAO and AChE Inhibitor
Ladostigil is a dual inhibitor of monoamine oxidase (MAO) and acetylcholinesterase (AChE), demonstrating IC50 values of 37.1 μM for MAO-B and 31.8 μM for AChE. This compound exhibits neuroprotective, antioxidant, and anti-inflammatory properties, making it valuable for research in conditions such as depression and Alzheimer's disease. Additionally, Ladostigil features an alkyne functional group, enabling it to serve as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
AChE Inhibitor
Norneostigmine is a potent inhibitor of acetylcholinesterase (AChE) with the ability to penetrate the blood-brain barrier. It demonstrates a 50% inhibition of mouse brain AChE within 10 minutes of treatment, exhibiting efficacy comparable to other known AChE inhibitors. This reagent is valuable for investigating memory disorders, including Alzheimer's disease and related cognitive impairments, facilitating research into potential therapeutic strategies. -
AChE Inhibitor
Zanapezil is a potent, reversible, and selective inhibitor of acetylcholine esterase (AChE). With an IC50 of 51.2 nM in rat cerebral cortex homogenates, Zanapezil effectively inhibits AChE activity, while also demonstrating moderate inhibition of muscarinic M1 and M2 receptor binding, with Ki values of 234 nM and 340 nM, respectively. This compound serves as a valuable tool for research focused on the early stages of Alzheimer's disease (AD). -
BChE Inhibitor
Broussonin A is a potent butyrylcholinesterase (BChE) inhibitor, exhibiting an IC50 of 4.16 µM. This diarylpropane natural product is derived from the bark of Broussonetia papyrifera through solid fermentation processes. Broussonin A is primarily utilized in research investigating neurodegenerative diseases and the modulation of cholinergic signaling pathways. Its inhibitory activity makes it a valuable tool for studying the role of BChE in various biological contexts.

