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Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
Gamma-secretase inhibitor
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Amyloid-β production inhibitor
gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor. gamma-Secretase Modulators is useful for Alzheimer's disease. -
amyloid β42 inhibitor
Ro 90-7501 is an inhibitor of amyloid β42 (Aβ42) fibril assembly; reduces Aβ42-induced toxicity (EC50 = 2 μM). -
β-amyloid (Aβ) inhibitor
ALZ-801 is an oral, small-molecule inhibitor of beta amyloid (Aβ) oligomer formation for Alzheimer's disease (AD). ALZ-801 is a prodrug of tramiprosate with improved pharmacokinetic properties and gastrointestinal tolerability. -
glutaminyl cyclase inhibitor
Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC50 of 1.23 μM. -
glutaminyl cyclase inhibitor
Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM. -
Oligomeric aggregation inhibitor
Anle138b is an oligomeric aggregation inhibitor. Anle138b is an oligomer modulator for neurodegenerative diseases such Parkinson's disease. -
GC inhibitor
Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer??s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. -
RAGE inhibitor
Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer??s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB). -
Aβ-ABAD inhibitor
Frentizole, an FDA-approved immunosuppressive drug, is a novel inhibitor of the Aβ-ABAD interaction.
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α-synuclein/Amyloid-β Aggregation Inhibitor
Scyllo-Inositol is an aggregation inhibitor that targets misfolded proteins, specifically α-synuclein and Amyloid-β. It effectively stabilizes non-toxic oligomers, preventing their conversion into toxic fibrils, thus supporting protein homeostasis and providing neuroprotective effects. By binding to the hydrophobic regions of pathogenic proteins, Scyllo-Inositol inhibits protein aggregation and enhances lysosome- and proteasome-mediated degradation pathways, ultimately reducing neurotoxicity. This compound is valuable for researching neurodegenerative diseases, including Parkinson’s disease, Alzheimer’s disease, and Huntington’s disease. -
Amyloid-β Inhibitor
Hoechst 34580 tetrahydrochloride is a nuclear marker dye that selectively targets A/T-rich double-stranded DNA. This compound exhibits enhanced fluorescence intensity when bound to nucleic acids, making it valuable for live cell labeling applications. As the pH of the solution increases, the fluorescence intensity of Hoechst 34580 also increases, providing a reliable tool for studying cellular dynamics, DNA distribution, and nuclear morphology in real-time. This reagent is particularly useful in research focused on amyloid-β and related neurodegenerative processes. -
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. -
GSK3β Inhibitor
GSK3β-IN-3 is an ATP-competitive inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 0.90 μM. It effectively lowers the phosphorylation levels of tau protein in the BR5706 strain and reduces the accumulation of amyloid-beta (Aβ) aggregates in the CL2006 strain. This compound is essential for research applications focused on Alzheimer's disease (AD), aiding in the understanding of neurodegenerative mechanisms and potential therapeutic strategies. -
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. -
QPCTL Inhibitor
QP5020 is a selective QPCTL inhibitor with an IC50 value of 15 nM. This compound demonstrates notable antitumor efficacy, making it a valuable tool for cancer research. Its mechanism of action provides insights into the role of QPCTL in tumor biology and offers potential avenues for therapeutic exploration. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Aβ Inhibitor
TPI-1917-49 is an Aβ inhibitor that effectively crosses the blood-brain barrier to decrease levels of amyloid beta (Aβ) peptide segments. By promoting the non-amyloidogenic pathway of amyloid precursor protein (APP), TPI-1917-49 enhances the generation of soluble APPα through α-secretase activity, thereby reducing amyloid plaque formation in murine models. This compound is suitable for research investigating Alzheimer's disease and its related pathologies. -
Aβ1-42 Aggregation Inhibitor
Aβ-IN-1 is an Aβ1-42 aggregation inhibitor that effectively prevents the aggregation of Aβ1-42 peptides in vitro. By delaying the exponential growth phase and reducing the steady-state quantity of fibrils, Aβ-IN-1 serves as a valuable tool for studying conformational disorders. This reagent is particularly relevant for research focused on Alzheimer's disease and other amyloid-related pathologies. -
Amyloid-β Inhibitor
BSBM6 is an amyloid-β (Aβ) inhibitor that effectively prevents Aβ aggregation and modulates its formation. This compound has been shown to reduce soluble oligomers, thereby potentially aiding in the treatment of neurodegenerative diseases associated with amyloid pathology. BSBM6 serves as a valuable tool for researchers studying Aβ dynamics and for the design of novel aggregation-modulating ligands.

