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Catalog No.
Product Name
Application
Product Information
Citations
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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 β42 inhibitor
Ro 90-7501 is an inhibitor of amyloid β42 (Aβ42) fibril assembly; reduces Aβ42-induced toxicity (EC50 = 2 μM). -
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. -
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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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. -
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. -
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. -
Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
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. -
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. -
Aβ Aggregation Inhibitor
TDI-2760 is an Aβ aggregation inhibitor with an IC50 of 1.67 μM, specifically targeting the aggregation of amyloid-beta peptides. This compound effectively inhibits Aβ-fibrinogen interactions and modulates contact system activation induced by Aβ42. TDI-2760 is suitable for research focused on Alzheimer's disease, particularly in the study of vascular abnormalities associated with Aβ aggregation. -
BACE1/BACE2 Inhibitor
NB-360 is a potent dual inhibitor of β-secretase 1 and 2 (BACE1/BACE2) with IC50 values of 5 nM and 6 nM, respectively. This compound is brain-penetrable and orally active, effectively inhibiting the accumulation of amyloid-β proteins. NB-360 is valuable for research in inflammation and neurological diseases, particularly Alzheimer's disease. -
Amyloid Inhibitor
4-Hydroxyindole is an amyloid inhibitor that plays a critical role in the disruption of amyloid fibrillization. This compound has been shown to induce alterations in liver function, thyroid activity, and blood glucose levels in preclinical models. Its unique properties make 4-Hydroxyindole a valuable tool for investigating neurodegenerative diseases and metabolic disorders. Researchers can leverage its potential to explore therapeutic avenues for amyloid-related pathologies. -
TDP-43 Inhibitor
ACI-19626 is a TDP-43 inhibitor that targets TDP-43 aggregation. This compound is valuable for investigating the role of TDP-43 in neurodegenerative diseases, including amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). Its utility in preclinical studies helps elucidate the molecular mechanisms underlying these conditions and aids in the identification of potential therapeutic strategies. -
QPCTL Inhibitor
QP5038 is a specific inhibitor of the enzyme QPCTL, exhibiting an IC50 value of 3.8 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology. QP5038 can be utilized in studies focused on understanding the role of QPCTL in tumor metabolism and potential therapeutic strategies. -
Glutaminyl Cyclase Inhibitor
PBD-150 is a selective inhibitor of human glutaminyl cyclase (hQC), specifically targeting the Y115E-Y117E variant with a Ki value of 490 nM. This compound exhibits significant inhibitory activity, making it a valuable tool for studying the role of glutaminyl cyclase in neurodegenerative diseases. PBD-150 can be applied in research focused on pathologies associated with abnormal protein aggregation and its therapeutic potential. -
Amyloid-β Inhibitor
D-KLVFFA is a potent inhibitor of Amyloid-β assembly, exhibiting an IC50 value of 2.6 μM. This peptide is utilized in research focused on Alzheimer's disease, providing insights into the mechanisms of amyloid plaque formation and potential therapeutic interventions. Its application can contribute to the understanding of neurodegenerative processes and the development of Alzheimer’s disease treatments. -
Amyloid-Beta and Tau Inhibitor
Aβ/tau aggregation-IN-1 is a selective inhibitor of amyloid-beta (Aβ1-42) β-sheet formation and tau protein aggregation. With KD values of 160 μM for Aβ1-42 and 337 μM for tau, this compound demonstrates significant potential in research related to neurodegenerative disorders such as Alzheimer's disease. Its ability to cross the blood-brain barrier further supports its use in studies aimed at understanding the pathophysiology of amyloid and tau accumulation in the central nervous system. -
Aβ/tau Protein Aggregation Inhibitor
DN5355 is a small molecule inhibitor of amyloid β protein (Aβ) and hyperphosphorylated tau protein aggregation. It effectively inhibits the formation of Aβ and tau fibrils while also promoting the disaggregation of pre-formed aggregates. This compound is valuable for research applications focused on Alzheimer's disease and the underlying mechanisms of protein aggregation associated with neurodegeneration. -
Aβ40 Aggregation Inhibitor
Biphenyl-3′,3,4,4′-tetrol (BPT) is a potent inhibitor of Aβ40 aggregation, targeting the aggregation process associated with amyloid-beta peptides. This compound is relevant for research into neurodegenerative diseases, particularly Alzheimer's disease, by facilitating studies aimed at understanding and potentially mitigating the pathological effects of amyloid plaque formation. -
Amyloid-β Inhibitor
Semilicoisoflavone B is an isoflavone derived from Glycyrrhiza uralensis Fisch, functioning primarily as an inhibitor of amyloid-β (Aβ) secretion. It reduces Aβ levels by inhibiting the expression and activity of β-secretase-1 (BACE1). This compound enhances PPARγ expression while simultaneously inhibiting STAT3 phosphorylation, leading to decreased BACE1 levels. Semilicoisoflavone B is relevant for research into Alzheimer's disease and mechanisms of neurodegeneration. -
Aβ Inhibitor
Aβ aggregation-IN-1 is a selective inhibitor of amyloid-beta aggregation, effectively targeting the fibrillogenesis process. It demonstrates significant biological activity with IC50 values of 3.92 µM for aggregation and 7.19 µM for disaggregation. Additionally, Aβ aggregation-IN-1 inhibits malondialdehyde formation, enhances intracellular reduced glutathione levels, and reduces caspase 3 activity in neuronal cells. This compound is valuable for research in Alzheimer's disease and related neurodegenerative disorders. -
β-Amyloid Inhibitor
RI-OR2-TAT is a potent inhibitor of β-Amyloid oligomerization, enhanced by the incorporation of the HIV protein transduction domain TAT. This compound exhibits a binding affinity to Aβ42 fibrils with a Kd value ranging from 58 to 125 nM. RI-OR2-TAT effectively reduces Aβ aggregation and plaque formation, mitigates microglial activation and oxidative stress, and promotes neurogenesis by increasing the proliferation of young neurons in the dentate gyrus. It is a valuable tool for research focused on neurodegenerative diseases, particularly Alzheimer's disease. -
Aβ1-40 Aggregation Inhibitor
QR-0217 is a potent inhibitor of Aβ1-40 aggregation, exhibiting an IC50 value of 7.5 µM. This compound also demonstrates the ability to inhibit α-synuclein aggregation, making it useful in studies related to neurodegenerative diseases. Additionally, QR-0217 has been shown to mitigate memory impairments associated with Aβ neurotoxicity, providing a valuable tool for research on Alzheimer's disease and related conditions. -
Amyloid-β Inhibitor
2-Hydroxy-5-(phenyldiazenyl)benzoic acid-d5 is a deuterated derivative of 2-Hydroxy-5-(phenyldiazenyl)benzoic acid that primarily targets amyloid-β. This compound exhibits significant inhibitory activity against amyloid-β aggregation, making it valuable for research related to Alzheimer's disease and other neurodegenerative disorders. It serves as a useful tool for investigating the mechanisms of amyloid pathology and potential therapeutic strategies. -
Aβ1–42 Aggregation Inhibitor
Aβ1–42 aggregation inhibitor 2 is a potent inhibitor of Aβ1-42 aggregation, which is significant in the study of Alzheimer's disease. This compound demonstrates strong antioxidant properties, effectively chelates metal ions, and alleviates oxidative stress. Additionally, it exhibits neuroprotective and anti-neuroinflammatory activities, making it a valuable tool for research focused on neurodegenerative disorders and potential therapeutic interventions. -
BACE1 Inhibitor
CTS-21166 is a selective inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1), designed to penetrate the blood-brain barrier effectively. It demonstrates the ability to reduce levels of amyloid-beta (Aβ) in the brain, making it a valuable tool for studying the pathogenesis of Alzheimer's disease. CTS-21166 is suitable for use in both in vitro and in vivo research applications focused on Alzheimer's and related neurodegenerative disorders. -
Amyloid-β Inhibitor
YIAD-0205 is an orally bioavailable inhibitor of amyloid-β (Aβ) aggregation, specifically targeting Aβ(1-42). This compound exhibits significant in vivo efficacy in a transgenic mouse model of Alzheimer's disease carrying five familial mutations (5XFAD). Its application lies in Alzheimer's research, particularly in studies exploring therapeutic strategies aimed at mitigating Aβ-related neurodegeneration. -
Amyloid β Inhibitor
Aβ-IN-3 is a potent inhibitor of amyloid β (Aβ) aggregation, specifically targeting Aβ42. This compound effectively inhibits the aggregation of Aβ42, making it a valuable tool in the study of amyloid-related pathologies. However, Aβ-IN-3 does not mitigate the neurotoxicity associated with Aβ42 in SH-SY5Y cells, nor does it alter the aggregation state of Aβ42 into a non-toxic form. Its primary applications lie in research focused on Alzheimer's disease and amyloid aggregation mechanisms. -
Aβ Inhibitor
PPI-1019 is an amyloid beta (Aβ) inhibitor that specifically targets the aggregation of Aβ peptides. This compound demonstrates potential neuroprotective effects, making it a valuable tool for researching neurodegenerative disorders, particularly Alzheimer's disease. Its role in modulating Aβ-related toxicity makes PPI-1019 significant for studies aimed at understanding the pathophysiology of amyloid plaque formation and developing therapeutic strategies. -
Aβ Oligomers Formation Inhibitor
Aβ-IN-6 is an Aβ oligomers formation inhibitor that effectively reduces pro-inflammatory cytokine release from microglia. This compound significantly promotes Nrf2 nuclear translocation, thereby interfering with the aggregation of Aβ oligomers. Aβ-IN-6 offers neuroprotective effects through modulation of redox-sensitive signaling pathways in in vivo oxidative stress models. Its oral bioactivity and combined anti-inflammatory, antioxidant, and anti-oligomeric properties make Aβ-IN-6 a valuable reagent for research into 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.
