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Aβ42 Inhibitor
Doliroside A is an Aβ42-binding agent that exhibits an IC50 of 26.57 μM for Aβ42. By binding to Aβ42 nuclei and oligomers, it forms stable complexes that suppress Aβ42 fibrillation, redirecting it into off-pathway, amorphous oligomers. This compound serves as a valuable tool in Alzheimer's disease research, aiding in the understanding of Aβ42 aggregation mechanisms and potential therapeutic strategies. -
BACE1/2 Inhibitor
BACE1/2-IN-1 is a potent dual inhibitor of BACE1 and BACE2, exhibiting IC50 values of 0.01 μM and 0.0053 μM, respectively. This compound demonstrates a favorable pharmacokinetic profile characterized by a lower P-glycoprotein efflux ratio and enhanced passive permeability. In addition, BACE1/2-IN-1 is associated with increased metabolic stability in liver microsomes, making it a valuable tool for researching therapeutic strategies targeting amyloid precursor protein processing in Alzheimer's disease. -
BACE1 Inhibitor
2,2′,4,4′-Tetrahydroxychalcone is a selective and potent inhibitor of Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) with an IC50 of 0.62 μM. This compound, derived from Isoliquiritigenin found in Glycyrrhiza uralensis, effectively inhibits the β-cleavage of amyloid precursor protein (APP), leading to a reduction in β-amyloid (Aβ) peptide production. 2,2′,4,4′-Tetrahydroxychalcone is used in research related to Alzheimer's disease, providing insights into potential therapeutic avenues for neurodegenerative conditions. -
Cholinesterase (ChE) Inhibitor
hAChE/Aβ1-42-IN-1 is a potent cholinesterase (ChE) inhibitor that effectively inhibits human acetylcholinesterase (hAChE) and prevents the aggregation of Aβ1-42 peptides. This compound demonstrates favorable relative safety in HepG2 cell lines and exhibits excellent blood-brain barrier (BBB) penetration, exhibiting a wide safety margin. hAChE/Aβ1-42-IN-1 is a valuable tool for research focusing on Alzheimer's disease (AD) and related neurodegenerative conditions. -
BACE1 Inhibitor
AZ3971 is a selective BACE1 inhibitor that effectively penetrates the blood-brain barrier, while leaving γ-secretase activity unaffected. By reducing the production of amyloid-beta (Aβ), AZ3971 serves as a valuable tool in the study of Alzheimer's disease and related neurodegenerative disorders. Its oral bioavailability makes it particularly suitable for in vivo research applications. -
Aβ oligomerization Inhibitor
Aβ aggregation-IN-4 is an Aβ oligomerization inhibitor that targets and mitigates the neurotoxicity associated with amyloid-β protein (Aβ). By significantly reducing the formation of oligomeric complexes of Aβ (Aβ-OCs) without affecting total Aβ levels, it effectively attenuates Aβ oligomerization. This compound provides a valuable tool for researching the pathophysiology of Alzheimer's disease (AD) and exploring potential therapeutic strategies. Additionally, Aβ aggregation-IN-4 protects primary cortical neurons from oligomer-induced cell death, highlighting its relevance in neuroprotective studies. -
Tau/Amyloid-β Aggregation Inhibitor
TRV-1387 is a benzofurazan compound that functions as an inhibitor of tau and amyloid-β aggregation. It demonstrates significant biological activity in preventing the formation of toxic aggregates associated with neurodegenerative diseases, making it a valuable tool for research in Alzheimer's disease and related pathologies. TRV-1387 can be utilized to study the mechanisms of amyloid-related toxicity and to explore potential therapeutic strategies targeting protein aggregation. -
Tau/Aβ Inhibitor
D-687 is a selective inhibitor of Tau and amyloid-beta (Aβ) aggregation. It has demonstrated the ability to reverse Aβ1–42-induced neurotoxicity in SH-SY5Y neuronal cells, highlighting its significant neuroprotective effects. This compound is valuable for research focused on Alzheimer's disease and related neurodegenerative disorders. -
QC Inhibitor
Glutaminyl Cyclase Inhibitor 5 is a potent and selective inhibitor of human glutaminyl cyclase (hQC), exhibiting an IC50 value of 3.2 nM. This compound serves as a valuable tool for investigating the role of hQC in neurodegenerative diseases and related biological processes. It is applicable in various research studies focused on glutamate signaling and its implications in disease mechanisms. -
Tau/Aβ Inhibitor
D-688 is a potent inhibitor of Tau and amyloid-beta (Aβ), demonstrating significant neuroprotective properties. This compound effectively reverses Aβ1–42-induced toxicity in SH-SY5Y neuronal cells, making it a valuable tool for studying neurodegenerative processes. Additionally, D-688 improves the survival rate of Drosophila melanogaster models expressing the human tau protein isoform (2N4R), underscoring its potential in Alzheimer's disease research and related disorders. -
BuChE Inhibitor
BuChE-IN-6 is a potent and selective inhibitor of butyrylcholinesterase (BuChE), exhibiting IC50 values of 0.46 μM and 0.51 μM for equine and human BuChE, respectively. This compound also demonstrates the ability to inhibit self-aggregation of amyloid-beta 42 (Aβ42), making it a valuable tool for research related to neurodegenerative diseases. Its unique properties support investigations into cholinergic dysfunction and the pathogenesis of Alzheimer's disease. -
Lipid Droplet Formation Inhibitor
Beauveriolide III is a specific inhibitor of lipid droplet formation, effectively reducing lipid accumulation in mouse macrophages. This compound plays a significant role in studies focused on lipid metabolism and its implications in metabolic disorders. Its utility in research can aid in understanding the biological pathways regulating lipid storage and inflammation in macrophage-associated pathologies. -
hAChE/hBACE Inhibitor
hAChE/hBACE-1-IN-4 is a quinazoline derivative that functions as a dual inhibitor of human acetylcholinesterase (hAChE) and human β-site amyloid precursor protein cleaving enzyme 1 (hBACE-1). It exhibits potent inhibitory activity with IC50 values of 0.283 μM for hAChE and 0.231 μM for hBACE-1. This compound demonstrates the ability to inhibit amyloid-beta (Aβ) aggregation and shows favorable properties such as non-neurotoxicity, blood-brain barrier permeability, and oral bioavailability. hAChE/hBACE-1-IN-4 is suitable for research applications related to Alzheimer's disease. -
RAGE/SERT Inhibitor
RAGE/SERT-IN-1 is a potent inhibitor of receptor for advanced glycation end products (RAGE) and serotonin transporter (SERT), demonstrating IC50 values of 8.26 μM and 31.09 nM, respectively. This compound exhibits significant neuroprotective properties against Aβ25-35-induced neuronal damage and has been shown to alleviate depressive behaviors in murine models. RAGE/SERT-IN-1 is a valuable tool for studying the interplay between Alzheimer's disease and depression comorbidity. -
Aβ Aggregation Inhibitor
SEN 304 is an Aβ aggregation inhibitor that directly binds to Aβ(1-42), effectively delaying β-sheet formation while promoting the aggregation of toxic oligomers into a nontoxic form. This compound is primarily utilized in research focused on Alzheimer’s disease, providing insights into the mechanisms of neurodegeneration and potential therapeutic strategies. The ability of SEN 304 to modulate Aβ aggregation makes it a valuable tool for studying amyloid pathology. -
AChE Inhibitor
AChE-IN-19 is a potent inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 value of 0.56 μM. This compound also demonstrates the ability to inhibit amyloid beta (Aβ) aggregation, contributing to its neuroprotective properties. AChE-IN-19 has been shown to exert minimal toxicity on SH-SY5Y neuronal cells, making it a valuable tool for research applications related to Alzheimer's disease. -
Amyloid-β Inhibitor
Aβ Fibrillization Modulator 1 targets amyloid-β (Aβ) by stabilizing Aβ monomers, thus inhibiting the formation of toxic fibrils associated with neurodegenerative diseases. This compound demonstrates potential in research applications focused on Alzheimer's disease and other amyloid-related disorders. By modulating fibrillization, it provides a valuable tool for investigating the mechanisms of amyloid aggregation and the development of therapeutic strategies. -
Amyloid-β Inhibitor
AChE/Aβ-IN-5 is a bifunctional inhibitor that targets acetylcholinesterase (AChE) and reduces the auto-induced aggregation of amyloid-β (Aβ) peptides. This compound has demonstrated the ability to significantly ameliorate cognitive deficits induced by scopolamine and Aβ in murine models. It serves as a valuable tool for research into neurodegenerative diseases, particularly Alzheimer's disease, by providing insights into the mechanisms underlying cognitive impairment. -
Aβ42 Inhibitor
2002-G12 is an Aβ42 inhibitor that effectively reduces Aβ42 toxicity by 76%. Its mechanism of action makes it a valuable tool for investigating Alzheimer's disease and studying the role of Aβ42 in neurodegenerative processes. Researchers can utilize 2002-G12 to explore potential therapeutic strategies targeting amyloid-beta aggregation and toxicity. -
Amyloid-β Inhibitor
KMS88009 is a potent amyloid-β oligomer inhibitor that directly disrupts the formation of these aggregates. This compound demonstrates significant potential in preserving cognitive function when administered preventively and reversing cognitive decline therapeutically. In studies using the APP/PS1 double transgenic mouse model, KMS88009 effectively reduced amyloid-β oligomer assembly and improved cognitive performance. Comprehensive evaluations of its physicochemical properties, pharmacokinetics, and toxicity further underscore KMS88009's promise as a therapeutic candidate for Alzheimer's disease. -
AChE Inhibitor
Memoquin is an AChE inhibitor with significant anti-amyloid and antioxidant properties. It exhibits oral bioavailability and selectively inhibits BACE-1 and AChE, with IC50 values of 108 nM and 1.55 nM, respectively. Memoquin is noted for its ability to enhance cognitive function while preventing Aβ-induced neurotoxicity associated with oxidative stress. This compound is valuable for research into Alzheimer's disease and related neurodegenerative disorders. -
Beta-secretase inhibitor
β-Secretase-IN-5 is a potent inhibitor of beta-secretase, a key enzyme involved in the cleavage of amyloid precursor protein (APP). By selectively reducing the production of amyloid-beta peptides Aβ1-40 and Aβ1-42, this compound is essential for research into Alzheimer's disease mechanisms and therapeutic strategies. Its application in neurodegenerative studies provides valuable insights into potential treatments for Alzheimer's. -
AChE Inhibitor
Phenserine tartrate is a selective, noncompetitive inhibitor of acetylcholinesterase (AChE) derived from Physostigmine. This compound has been shown to reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ), key factors involved in Alzheimer's disease pathology. Phenserine tartrate has demonstrated potential in improving cognitive performance and may help slow the progression of Alzheimer's disease, making it a valuable tool for research in neurodegenerative disorders. -
ChE/Aβ1-42 Aggregation Inhibitor
ChE/Aβ1-42-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and amyloid-beta peptide (Aβ1-42) aggregation, exhibiting IC50 values of 0.062 µM, 0.767 µM, and 1.227 µM, respectively. This compound demonstrates significant blood-brain barrier (BBB) penetration, making it a promising candidate for research into Alzheimer's disease. ChE/Aβ1-42-IN-1's multi-targeted mechanism positions it as a valuable tool for studying therapeutic strategies in neurodegenerative disorders. -
Aβ Aggregation Inhibitor
SEN-1269 is a potent inhibitor of Aβ aggregation, specifically targeting Aβ(1-42) oligomers. This compound protects neuronal cell lines from the detrimental effects of Aβ(1-42) exposure and mitigates deficits in long-term potentiation (LTP) and memory associated with Aβ oligomer toxicity. SEN-1269 serves as a valuable tool for research investigating the pathophysiology of Alzheimer's disease. -
AChE Inhibitor
hAChE-IN-10 is a potent inhibitor of human acetylcholinesterase (AChE), demonstrating an IC50 of 6.34 nM. This compound exhibits significant antioxidant properties and effectively scavenges free radicals. Additionally, hAChE-IN-10 has been shown to inhibit Cu2+-induced aggregation of Aβ1-42, reduce amyloid plaque formation, and provide neuroprotective effects. It has also been linked to the improvement of cognitive deficits in mouse models induced by scopolamine, making it a valuable tool for studying neurodegenerative diseases and cognitive impairment. -
Aβ42 Inhibitor
GL-522, a 4-sulfocalix[8]arene derivative, functions as an Aβ42 inhibitor by engaging in nonspecific and multipoint hydrophobic interactions, exhibiting a Kd of 276 μM. This compound effectively inhibits the fibrillation of Aβ42 and mitigates its cytotoxic effects, making it a valuable tool for research in Alzheimer's disease. Its ability to modulate amyloid aggregation and toxicity positions GL-522 as a significant reagent in neurodegenerative disease studies. -
Aβ Aggregation Inhibitor
AY1511 is an amyloid β (Aβ) aggregation inhibitor that demonstrates low cytotoxicity. This compound is utilized in research focusing on neurodegenerative diseases, particularly Alzheimer's disease, by inhibiting the aggregation of Aβ peptides. AY1511 serves as a valuable tool for studying the mechanisms of amyloid pathology and the development of potential therapeutic strategies. -
Aβ40/tau Aggregation Inhibitor
Tau/Aβ40 aggregation-IN-1 is a potent inhibitor of tau and Aβ40 aggregation, exhibiting IC50 values of 1.8 μM and 1.3 μM, respectively. This compound is of significant interest in Alzheimer's disease research, as it targets the pathological aggregation of tau protein and amyloid-beta peptides. Its effectiveness in modulating these protein interactions makes it a valuable tool for studying neurodegenerative mechanisms and potential therapeutic interventions. -
MAO-B Inhibitor
MAO-B-IN-50 is a selective inhibitor of monoamine oxidase B (MAO-B), demonstrating an IC50 value of 0.06 μM. This compound is effective in inhibiting the aggregation of amyloid-beta (Aβ40/42) and Tau proteins, with overall IC50 values near 1 μM. Additionally, MAO-B-IN-50 shows potent selective inhibition of acetylcholinesterase (AChE) with an IC50 of 1.78 μM. It is suitable for use in research related to Alzheimer's disease. -
Amyloid β Inhibitor
Aβ-IN-4 is a potent inhibitor of amyloid β (Aβ) aggregation, specifically targeting Aβ42. It effectively halts the aggregation process of Aβ42, which is central to the pathogenesis of Alzheimer’s disease. However, Aβ-IN-4 does not mitigate the neurotoxicity associated with Aβ42 in SH-SY5Y cells, nor does it modify the aggregation state of Aβ42 into a non-toxic form. This compound is valuable for research investigating Aβ-related mechanisms and the development of Alzheimer’s therapeutics. -
AChE Inhibitor
AChE-IN-12 is a selective acetylcholinesterase (AChE) inhibitor that effectively penetrates the blood-brain barrier, exhibiting IC50 values of 0.41 μM for rat AChE and 1.88 μM for electric eel AChE. This compound also demonstrates antioxidant properties (ORAC = 3.3 eq), selectively chelates metals, and inhibits human monoamine oxidase B (MAO-B) with an IC50 of 8.8 μM. AChE-IN-12 significantly inhibits both self- and Cu2+-induced aggregation of Aβ1-42 and displays neuroprotective effects, making it a valuable tool for research related to Alzheimer’s disease. -
AChE/BuChE Inhibitor
AChE/BuChE-IN-3 is a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), exhibiting IC50 values of 0.65 μM and 5.77 μM, respectively. This compound effectively inhibits the aggregation of amyloid beta peptide Aβ1-42 and demonstrates neuroprotective properties with minimal toxicity in SH-SY5Y cells. AChE/BuChE-IN-3 is suitable for research applications related to Alzheimer's disease, providing insight into cholinergic system modulation and potential therapeutic strategies. -
Aβ Fibrillogenic Inhibitor
Acetyl-Tau Peptide (273-284) amide is an acetylated fragment of the Tau protein that acts as an inhibitor of Aβ fibrillogenesis. It effectively reduces the aggregation of Ac-Aβ(25–35)-NH2, facilitating studies on the interplay between Aβ and Tau proteins. This peptide serves as a valuable experimental tool for investigating the mechanisms underlying Alzheimer's disease and related neurodegenerative conditions. -
Amyloid-β Inhibitor
AZ4800 is an amyloid-β inhibitor that targets the processing of amyloid precursor protein. It effectively reduces Aβ42 levels, demonstrating additive lowering activity both in vitro and in vivo. This compound is valuable for research focusing on Alzheimer's disease and related neurodegenerative disorders. -
Aβ1-42/AChE Inhibitor
AChE-IN-59 is a potent acetylcholinesterase (AChE) inhibitor, displaying an IC50 value of 0.05 μM. This compound effectively inhibits the aggregation of amyloid-beta peptide Aβ1-42, offering protective effects on neuronal cells and demonstrating favorable penetration of the blood-brain barrier. AChE-IN-59 is a valuable tool for research focused on Alzheimer's disease and related neurodegenerative disorders. -
BACE1 Inhibitor
TAK-070 hydrochloride hydrate is a noncompetitive inhibitor of BACE1 with an IC50 value of 3.15 μM. This compound is actively researched for its potential therapeutic effects in Alzheimer's disease, demonstrating the ability to reduce brain levels of soluble Aβ. Additionally, TAK-070 hydrochloride hydrate has shown promise in ameliorating cognitive impairments in preclinical models of Alzheimer's disease, making it a valuable tool for studying neurodegenerative disorders. -
AChE Inhibitor
AP2238 is a dual-function acetylcholinesterase (AChE) inhibitor that demonstrates Ki values of 21.7 μM for human AChE and 48.9 μM for butyrylcholinesterase (BuChE). This compound effectively inhibits the pro-fibrotic interaction between the peripheral site of AChE and amyloid-beta (Aβ), as well as Aβ aggregation. AP2238 is primarily utilized in Alzheimer's disease research, contributing to studies focused on neurodegeneration and cholinergic dysfunction. -
Amyloid-β Oligomerization Inhibitor
RI-OR2 is an amyloid-β (Aβ) oligomerization inhibitor that functions as a retro-inverso peptide. It has been shown to bind effectively to immobilized β-Amyloid (1-42) monomers and fibrils, demonstrating an apparent dissociation constant (Kd) of 9-12 μM. Additionally, RI-OR2 inhibits the extension of Aβ(1-42) fibrils, making it a valuable tool for research into Alzheimer’s disease and the mechanisms of amyloid pathology. -
AChE/BuChE Inhibitor
AChE/BuChE-IN-2 is a selective inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), demonstrating IC50 values of 0.72 μM and 0.16 μM, respectively. This compound exhibits non-competitive inhibition of AChE and effectively inhibits β-amyloid (Aβ) aggregation, with an IC50 of 62.52 μM. Notably, AChE/BuChE-IN-2 is capable of crossing the blood-brain barrier, making it a valuable tool for studying neurodegenerative conditions, such as Alzheimer's disease. -
BuChE Inhibitor
Multitarget AD inhibitor-1 is a selective and reversible inhibitor of butyrylcholinesterase (BuChE), exhibiting IC50 values of 7.22 μM for human BuChE and 1.55 μM for equine BuChE. This compound also inhibits β-secretase activity (IC50 = 41.60 μM) and demonstrates a strong capacity to inhibit amyloid β aggregation (IC50 = 3.09 μM) as well as tau aggregation. As a diphenylpropylamine derivative, it holds promise for multifunctional disease-modifying applications in Alzheimer’s research. -
Aβ-Fibrinogen Inhibitor
RU-505 is a potent inhibitor of the β-amyloid (Aβ) and fibrinogen interaction, demonstrating IC50 values of 5.00 μM and 2.72 μM in fluorescence polarization and AlphaLISA assays, respectively. This compound exhibits high permeability across the blood-brain barrier (BBB), making it a valuable tool in targeting cerebral amyloid angiopathy (CAA). RU-505 is applicable in research studies focused on Alzheimer's disease (AD) pathogenesis and potential therapeutic interventions. -
AChE Inhibitor
hAChE-IN-3 is a potent acetylcholinesterase (AChE) inhibitor with demonstrated blood-brain barrier permeability. It exhibits significant inhibitory effects against butyrylcholinesterase (BuChE), monoamine oxidase B (MAO-B), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), with IC50 values of 0.44, 0.08, 5.15, and 0.38 μM, respectively. Additionally, hAChE-IN-3 possesses antioxidant properties and metal chelating ability, enabling it to interact with peripheral anion sites and influence β-amyloid accumulation. This compound holds promise for advancing research in Alzheimer's disease and related neurodegenerative disorders. -
Multi-target Inhibitor
AChE-IN-63 is a multi-target inhibitor with a primary action as a selective inhibitor of human acetylcholinesterase (hAChE), exhibiting an IC50 of 0.103 μM. This compound also demonstrates inhibitory activity against human butyrylcholinesterase (hBChE) and human beta-site amyloid precursor protein cleaving enzyme 1 (hBACE-1) with IC50 values of 10 μM and 1.342 μM, respectively. AChE-IN-63 effectively inhibits Aβ aggregation, thereby preventing the formation and deposition of Aβ1-42. Due to its ability to penetrate the blood-brain barrier and oral bioavailability, it is primarily utilized in research related to Alzheimer's disease. -
BACE1 Inhibitor
TAK-070 Free base is a noncompetitive inhibitor of BACE1 with an IC50 of 3.15 μM. This compound exhibits significant potential in Alzheimer's disease research by reducing brain levels of soluble Aβ and ameliorating cognitive deficits in AD models. Its ability to modulate amyloid-beta processing makes it a valuable tool for investigating therapeutic strategies targeting Alzheimer's pathology. -
BChE Inhibitor
BChE-IN-8 is a potent and orally active inhibitor of butyrylcholinesterase (BChE), demonstrating IC50 values of 0.15 nM against equine serum BChE and 45.2 nM against human BChE. Its high stability ensures enhanced blood concentration and tissue exposure. BChE-IN-8 exhibits neuroprotective and cognitive-enhancing effects through modulation of the cholinergic system, amyloid beta (Aβ) aggregation, and neuropeptide levels. This compound is particularly relevant for research into Alzheimer's disease. -
AChE/MAO-B Inhibitor
AChE/MAO-B-IN-9 is a selective, reversible, non-competitive inhibitor of acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B), exhibiting an IC50 of 0.156 μM against electric eel AChE. This compound effectively inhibits the formation of Aβ40/42 fibrils, promotes the depolymerization of Aβ fibrils, and suppresses Tau protein fibril formation. Additionally, AChE/MAO-B-IN-9 demonstrates antioxidant and neuroprotective properties, while alleviating memory deficits induced by scopolamine in murine models. This reagent is valuable for research related to Alzheimer’s disease. -
AChE Inhibitor
AChE-IN-88 is a novel pyridazine derivative that functions as an acetylcholinesterase (AChE) inhibitor. It exhibits potent inhibitory activity against AChE and additionally targets amyloid β protein (Aβ) aggregation, making it relevant for Alzheimer's disease research. With a pIC50 value of 7.16, AChE-IN-88 is a promising candidate for studying multi-target approaches in neurodegenerative conditions. -
BuChE Inhibitor
BuChE-IN-2 is a potent inhibitor of butyrylcholinesterase (BuChE), exhibiting IC50 values of 1.28 μM and 0.67 μM against BuChE and nitric oxide production, respectively. This compound has demonstrated the ability to inhibit amyloid-beta aggregation, reduce reactive oxygen species formation, and chelate copper ions, all while effectively crossing the blood-brain barrier. BuChE-IN-2 is a valuable tool for research focused on Alzheimer's disease and related neurodegenerative disorders. -
BACE Inhibitor
LY-2434074 is a selective β-secretase (BACE) inhibitor, exhibiting an IC50 value of less than 100 nM. This compound effectively inhibits the production of amyloid-β (Aβ40 and Aβ42), making it a valuable tool for studying the pathophysiology of neurological disorders. Its primary research applications include investigations into Alzheimer's disease and related conditions, enabling insights into potential therapeutic strategies.

