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BACE1 Inhibitor
AZD3839 fumarate is a selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme (BACE1) that effectively crosses the blood-brain barrier. With a Ki of 26.1 nM, it inhibits recombinant human BACE1 and demonstrates an IC50 of 4.8 nM in the reduction of Aβ40 production in SH-SY5Y cells. AZD3839 fumarate’s ability to bind BACE1 and decrease amyloid beta production derived from amyloid precursor protein cleavage makes it a valuable tool for research focused on Alzheimer's disease pathology. -
BACE1 Inhibitor
BACE1-IN-13 is a potent inhibitor of β-secretase 1 (BACE1), exhibiting an IC50 value of 2.9 nM. It demonstrates notable efficacy in hAβ42 cell lines with an IC50 of 1.3 nM, making it a valuable tool for studying Alzheimer's disease pathology. BACE1-IN-13 has shown cardiovascular safety and produces sustained reductions in Aβ42 levels in both mouse and dog models, supporting its potential use in neurological research applications. -
BACE1 Inhibitor
Lanabecestat camsylate is a potent, orally active inhibitor of beta-secretase 1 (BACE1), demonstrating a Ki value of 0.4 nM. This compound effectively penetrates the blood-brain barrier, making it an essential tool for investigating the pathophysiology of Alzheimer's disease. Lanabecestat camsylate is utilized in research aimed at understanding the therapeutic potential of BACE1 inhibition in neurodegenerative conditions. -
BACE Inhibitor
BACE-IN-3 is a selective inhibitor of beta-secretase (BACE) with an IC50 of 0.004 μM. This compound plays a critical role in the modulation of amyloid-beta peptide production, making it a valuable tool for research in Alzheimer's disease and related neurodegenerative disorders. Its potent inhibitory activity against BACE makes it suitable for studying the mechanisms of amyloidogenic processes and evaluating potential therapeutic strategies. -
BACE1 Inhibitor
BACE1-IN-11 is a potent inhibitor of beta-secretase 1 (BACE1), exhibiting an IC50 value of 72 μM. This compound has been identified as a valuable tool for Alzheimer's disease research, specifically in the study of amyloid precursor protein processing and beta-amyloid peptide generation. Through its selective inhibition of BACE1, BACE1-IN-11 aids in exploring therapeutic strategies aimed at mitigating the impact of Alzheimer's pathology. -
β-secretase Inhibitor
GRL-8234 is a potent β-secretase (BACE1) inhibitor with a high affinity for its target (Ki = 1.8 nM) and the ability to penetrate the blood-brain barrier. This compound has demonstrated efficacy in rescuing age-related cognitive decline in Tg2576 mice, making it a valuable tool for Alzheimer's disease research. GRL-8234 is suitable for investigations focused on the mechanisms of AD and potential therapeutic interventions. -
AChE/BACE1 Inhibitor
2-Acetoxyacorenone is a sesquiterpenoid that functions as a potent inhibitor of acetylcholinesterase (AChE) and β-secretase 1 (BACE1). Isolated from the rhizome of Acorus tatarinowii, this compound exhibits significant biological activity relevant to the modulation of cholinergic signaling and amyloid precursor protein processing. It serves as a valuable tool in Alzheimer's disease research, allowing for investigations into therapeutic strategies targeting these key enzymes. -
BACE1 Inhibitor
BACE1-IN-12 is a potent inhibitor of Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), exhibiting an IC50 of 8.9 µM. This compound demonstrates selective inhibition of butyrylcholinesterase (BuChE) with an IC50 of 3.2 µM and possesses antioxidant activity with an IC50 of 10.2 μM, as assessed by the DPPH assay. BACE1-IN-12 may serve as a potentially valuable agent in Alzheimer's disease research. -
Beta-secretase Inhibitor
β-Secretase Inhibitor III is a highly selective inhibitor of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), with a Ki value of 0.13 nM. This compound effectively reduces the production of amyloid-beta peptides, making it a valuable tool for research on Alzheimer's disease and related neurodegenerative disorders. Its specificity for BACE1 allows for precise investigations into amyloid pathology and the development of therapeutics targeting this crucial step in amyloidogenesis. -
Memapsin 2 Inhibitor
OM99-2 is a potent peptidomimetic inhibitor of human brain memapsin 2, exhibiting a tight-binding affinity with a Ki value of 9.58 nM. This compound plays a crucial role in the advancement of BACE1 inhibitor research and has significant implications in the study of Alzheimer's disease. OM99-2 is valuable for investigating the pathogenic mechanisms of neurodegenerative disorders and may contribute to the development of therapeutic strategies. -
β-Secretase Inhibitor
β-Secretase Inhibitor II is a potent inhibitor of β-Secretase, designed to impede the enzyme's activity in the amyloidogenic pathway. It has an IC50 value of 700 nM for total Aβ inhibition and an IC50 of 2.5 μM for the specific inhibition of Aβ1–42. This compound is valuable for research into Alzheimer's disease and the mechanisms underlying amyloid plaque formation. -
BACE1 Inhibitor
BACE1-IN-9 is a potent inhibitor of β-site APP cleaving enzyme 1 (BACE1), exhibiting an IC50 of 1.2 µM. This compound is significant in the context of Alzheimer's disease research, as it inhibits the cleavage of amyloid precursor protein, thereby potentially reducing amyloid beta production. BACE1-IN-9 can be utilized in studies aimed at elucidating the role of BACE1 in neurodegeneration and assessing therapeutic approaches for Alzheimer's disease. -
BACE1 Inhibitor
AZ-4217 is a potent inhibitor of β-site amyloid precursor protein cleavage enzyme 1 (BACE1), exhibiting an IC50 of 160 pM in human SH-SY5Y cells. This compound effectively reduces amyloid deposition in Tg2576 mouse models, making it a valuable tool for Alzheimer’s Disease research and related neurodegenerative studies. Its ability to modulate BACE1 activity underscores its potential significance in therapeutic applications targeting amyloid pathology. -
BACE1/2 Inhibitor
Verubecestat tosylate is a potent inhibitor of BACE1 and BACE2, displaying high affinity with Ki values of 2.2 nM and 0.38 nM, respectively. This compound effectively reduces levels of Aβ40, making it a potential therapeutic agent for Alzheimer's Disease research. Verubecestat tosylate is utilized in studies exploring the modulation of amyloid-beta peptide production and its implications in neurodegenerative disorders. -
BACE-1 Inhibitor
SEW06622 is a selective inhibitor of beta-secretase 1 (BACE-1) with an IC50 value of 6.3 μM. This compound plays a crucial role in Alzheimer's disease research by modulating amyloid precursor protein processing, thereby reducing amyloid-beta plaque formation. SEW06622 is valuable for studies focused on neurodegenerative processes and therapeutic interventions in Alzheimer's disease. -
BACE1 Inhibitor
PF-06663195 is a selective β-secretase 1 (BACE1) inhibitor, exhibiting IC50 values of 53 nM for the BACE1 CFA assay and 15 nM for the BACE1 WCA assay. This compound is a valuable tool for investigating the role of BACE1 in the pathogenesis of Alzheimer’s disease and can aid in the discovery of potential therapeutic strategies targeting amyloid precursor protein processing. -
Beta-secretase Inhibitor
BACE-IN-1 is a selective β-secretase inhibitor, designed to target the β-site amyloid precursor protein cleaving enzyme (BACE). By inhibiting BACE activity, this compound has potential applications in the treatment of Alzheimer's disease and other disorders associated with amyloid plaque formation. Its unique imidazo[1,2-a]pyridine structure enhances its efficacy in this specific biological context. -
Calcineurin Inhibitor
Mevalonolactone is a sesquiterpene lactone that acts as a calcineurin inhibitor, demonstrating inhibitory activity with an IC50 value of 134.29 μM against p-Nitrophenyl phosphate. This compound is primarily used in research exploring cellular signaling pathways, immune response modulation, and potential therapeutic applications for disorders involving calcineurin activity. Its ability to inhibit calcineurin makes it valuable for investigations into T cell activation and cytokine production. -
Calcineurin NFAT Inhibitor
NFAT Inhibitor-2 is a selective inhibitor of calcineurin, targeting the calcium-regulated NFAT signaling pathway. This compound demonstrates significant potential in research related to inflammatory diseases, autoimmune disorders, cardiovascular conditions, neurodegenerative diseases, and disorders characterized by uncontrolled cell proliferation or differentiation. Additionally, NFAT Inhibitor-2 may provide insights into angiogenesis-related diseases, allergies, anaphylaxis, and alopecia. -
CaMK1D Inhibitor
CS587 is a selective inhibitor of Calcium/calmodulin-dependent protein kinase 1D (CaMK1D), demonstrating neurocytotoxic effects at concentrations of 10 μM. This compound modulates neuronal cell sensitivity to amyloid-beta (Aβ) oligomer toxicity, making it a valuable tool for studying neurodegenerative disorders and related cellular pathways. Its specificity and mechanism of action position CS587 as a significant reagent for research into neuronal health and disease mechanisms. -
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.

