Neuronal Signaling

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. ChE Inhibitor

    Aβ1–42 aggregation inhibitor 3 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with IC50 values of 1.634 μM and 0.0285 μM, respectively. This compound effectively inhibits the aggregation of Aβ1-42, making it a valuable tool in Alzheimer's disease research. Its dual inhibitory action on cholinesterases positions it as a promising candidate for studies aimed at understanding and mitigating neurodegenerative processes associated with AD.
  24. hBChE Inhibitor

    hBChE-IN-1 is a potent inhibitor of human butyrylcholinesterase (hBChE) with an IC50 value of 7 nM, demonstrating high selectivity over human acetylcholinesterase (hAChE). This compound also exhibits inhibitory activity against tau and Aβ40 protein aggregation, with IC50 values of 20 μM and 4.3 μM, respectively. hBChE-IN-1 is valuable in Alzheimer's disease research, aiding in the exploration of therapeutic strategies targeting protein aggregation associated with neurodegeneration.
  25. 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.
  26. BuChE Inhibitor

    BuChE-IN-5 is a potent butyrylcholinesterase (BuChE) inhibitor, exhibiting an IC50 value of 1.94 μM. This compound effectively inhibits the aggregation of amyloid-beta (Aβ) and tau proteins in Escherichia coli, demonstrating significant potential in Alzheimer's disease research. Additionally, BuChE-IN-5 possesses free radical scavenging capabilities and antioxidant activity, making it a valuable tool for studying neurodegenerative processes and related therapeutic approaches.
  27. Aβ42 Inhibitor

    CHF5022 is an inhibitor of Aβ42 secretion, exhibiting an IC50 value of 92 μM. In addition to its primary activity, CHF5022 demonstrates modest inhibition of Aβ40 at non-cytotoxic concentrations, achieving a reduction of approximately 22.2% at 100 μM. This compound is valuable for research into Alzheimer's disease and the mechanisms of amyloid-beta peptide regulation.
  28. Amyloid-β42 Inhibitor

    Kayaflavone is a biflavonoid of the amentoflavone type known for its inhibitory activity against amyloid-β42 cytotoxicity in PC-12 cells, exhibiting an EC50 value of 5.29 μM. This compound holds potential for research applications in Alzheimer’s disease, contributing to the understanding of amyloid-related neurotoxicity and its implications in neurodegenerative processes.
  29. RAGE Inhibitor

    Azeliragon dihydrochloride is a selective inhibitor of the receptor for advanced glycation end products (RAGE). This compound demonstrates the ability to cross the blood-brain barrier and has been investigated for its potential to mitigate disease progression in patients with mild Alzheimer's disease. Its mechanism of action involves reducing neuroinflammation and promoting neuronal health, making it a promising candidate for research focused on Alzheimer's disease therapeutics.
  30. BCA

    BACE1 Inhibitor

    BCA (Disodium bicinchoninate) is a non-competitive inhibitor of Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), with an IC50 value of 28 µM and a Ki value of 43 µM. This compound exhibits anticancer properties and has potential applications in Alzheimer's disease research, making it a valuable tool for studying mechanisms of amyloid pathology and therapeutic strategies.
  31. BACE1 Inhibitor

    8-Geranyloxy-5-methoxypsoralen is a selective BACE1 inhibitor, exhibiting an IC50 of 11.1 μM. This compound effectively inhibits the activity of BACE1, an enzyme implicated in the pathogenesis of Alzheimer's disease. It serves as a valuable research tool for investigating mechanisms of neurodegeneration and potential therapeutic strategies in Alzheimer's disease.
  32. BACE2 Inhibitor

    BACE2-IN-1 is a selective inhibitor of the β-site amyloid precursor protein cleaving enzyme 2 (BACE2), demonstrating a Ki value of 1.6 nM. This compound is instrumental in studies targeting the modulation of glucose metabolism and insulin signaling, offering valuable insights into the pathophysiology of Type 2 Diabetes. Researchers can utilize BACE2-IN-1 to explore therapeutic strategies aimed at mitigating the effects of βACE2 in metabolic disorders.
  33. BACE1 Inhibitor

    Aloeresin D is a chromone glycoside derived from Aloe vera, functioning as a β-Secretase (BACE1) inhibitor with an IC50 value of 39 μM. This compound demonstrates potential neuroprotective effects through the modulation of amyloid precursor protein processing, making it a valuable tool for Alzheimer's disease research. Its ability to inhibit BACE1 provides implications for developing therapeutic strategies targeting amyloid beta plaque formation.
  34. Beta-secretase Inhibitor

    Aloenin, a natural product, acts as a beta-secretase (BACE) inhibitor with an IC50 of 14.95 μg/mL. This compound exhibits effective free radical scavenging activity, making it beneficial for oxidative stress studies. Additionally, Aloenin has demonstrated the ability to suppress peritoneal hypertrophy in large rats, indicating its potential use in research related to inflammation and tissue remodeling.
  35. BACE1 Inhibitor

    Cassiaside is a naphthopyrone glucoside that acts as a mixed-type inhibitor of BACE1, with an IC50 value of 4.45 μM and a Ki of 9.85 μM. This compound demonstrates potential therapeutic activity against Alzheimer's disease by inhibiting the production of amyloid-beta peptides. Research applications may include studies focused on Alzheimer's pathogenesis and the development of BACE1-targeted therapies.
  36. BACE1 Inhibitor

    Kushenol C is a potent inhibitor of β-site APP cleaving enzyme 1 (BACE1), demonstrating an IC50 value of 5.45 µM. Isolated from the roots of Sophora flavescens, this compound exhibits significant anti-inflammatory and antioxidative stress properties. Kushenol C is relevant for research focusing on neurodegenerative diseases, particularly Alzheimer's disease, due to its role in modulating amyloid beta production.
  37. β-Secretase/BACE1 Inhibitor, BACE1 inhibition

    β-Secretase inhibitor is a selective inhibitor targeting β-secretase (BACE1), exhibiting an IC50 of 25 nM. This compound is primarily utilized in research focused on Alzheimer's disease, as it plays a critical role in reducing amyloid-β peptide generation. Its ability to inhibit BACE1 makes it a valuable tool for studying neurodegenerative processes and developing therapeutic strategies aimed at amyloid plaque formation.
  38. BACE1/2 Inhibitor

    Verubecestat TFA is a potent and selective inhibitor of Beta-site Amyloid Precursor Protein Cleaving Enzyme 1 and 2 (BACE1/2), demonstrating Ki values of 2.2 nM and 0.38 nM, respectively. This compound effectively reduces the accumulation of amyloid-beta peptide (Aβ40), indicating its potential utility in Alzheimer's disease research. Verubecestat TFA serves as a valuable reagent for exploring the pathogenic mechanisms of amyloid-beta in neurodegenerative disorders and evaluating therapeutic strategies targeting BACE activity.
  39. Beta-secretase Inhibitor

    BACE1-IN-5 is a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, exhibiting an IC50 of 9.1 nM. This compound also effectively inhibits the formation of cellular amyloid-β (Aβ), with an IC50 value of 0.82 nM. Additionally, BACE1-IN-5 is designed to enhance its medicinal chemistry, reducing hERG channel inhibition and P-glycoprotein efflux, making it a valuable tool for Alzheimer's disease research and therapeutic investigations targeting amyloid pathology.
  40. BACE-1 Inhibitor

    BACE-1 Inhibitor 2 is a highly effective inhibitor of the beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1), exhibiting an IC50 of 1.5 nM in enzymatic assays. This compound is characterized by its ability to penetrate the central nervous system and is primarily utilized in research focused on Alzheimer's disease and amyloid beta production. Its strong inhibitory activity makes it a valuable tool for investigating BACE-1's role in neurodegeneration and for the development of potential therapeutic strategies.
  41. BACE1 Inhibitor

    AM-6494 is a highly potent, orally active inhibitor of BACE1 (β-site amyloid precursor protein cleaving enzyme 1), exhibiting an IC50 of 0.4 nM and selectivity over BACE2 (IC50 of 18.6 nM). This compound also features an alkyne group, enabling its use as a click chemistry reagent that participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc). AM-6494 is valuable for research in neurodegenerative diseases, particularly Alzheimer's, by elucidating the role of BACE1 in amyloid-beta production.
  42. BACE1 Inhibitor

    LY2886721 hydrochloride is a selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor. It demonstrates potent inhibition with an IC50 of 20.3 nM for recombinant human BACE1 while showing reduced activity towards cathepsin D, pepsin, and renin. Due to its ability to cross the blood-brain barrier, LY2886721 hydrochloride is a promising candidate for therapeutic applications in Alzheimer's disease research.
  43. BACE Inhibitor

    LY3202626 is a potent beta-secretase (BACE) inhibitor, exhibiting IC50 values of 0.615 nM for BACE1 and 0.871 nM for BACE2. This compound effectively penetrates the central nervous system, making it valuable for research focused on Alzheimer's disease and other neurodegenerative disorders where BACE activity is implicated. Its specific inhibition of BACE enzymes allows for the exploration of therapeutic strategies aimed at reducing amyloid-beta peptide production.
  44. Beta-secretase Inhibitor

    JNJ-67569762 is a selective beta-secretase (BACE1) inhibitor that targets the S3 pocket, exhibiting an IC50 value of 2.7 nM. This compound is primarily used in Alzheimer's disease research, aimed at reducing the production of amyloid-beta peptides. Its specificity and potency make it a valuable tool for investigating the role of BACE1 in neurodegenerative disorders and for the development of therapeutic strategies.
  45. Beta-secretase Inhibitor

    BACE1-IN-6 is a potent inhibitor of beta-secretase (BACE1) with an IC50 of 1.5 nM. This compound effectively impedes the cleavage of amyloid precursor protein, making it a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. Its specificity and efficacy make it an important reagent for investigating the proteolytic pathways involved in amyloid-beta production.
  46. hAChE/hBuChE Inhibitor

    hAChE-IN-7 is a mixed inhibitor targeting both the catalytic active site and peripheral anionic site of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE). It exhibits potent inhibitory activity with IC50 values of 69.8 nM for hAChE and 68.0 nM for hBuChE, along with a notable inhibitory effect on β-secretase-1 (BACE-1) at an IC50 of 3.6 μM. This compound is valuable for research related to Alzheimer's disease, facilitating studies on cholinergic system modulation and potential therapeutic strategies.
  47. BACE1 Inhibitor

    BACE1-IN-10 is a potent inhibitor of Beta-site Amyloid precursor protein Cleaving Enzyme 1 (BACE1). It demonstrates sub-micromolar activity against recombinant BACE1, making it a valuable tool for research focused on Alzheimer's disease and amyloid-beta peptide processing. This compound is suitable for studies investigating the modulation of amyloidogenic pathways and facilitating the development of therapeutic strategies targeting cognitive decline associated with neurodegenerative disorders.
  48. Beta-secretase Inhibitor

    β-Secretase Inhibitor I is a highly effective inhibitor of β-secretase, a key enzyme involved in the production of amyloid-beta, a hallmark of Alzheimer’s disease. This compound exhibits strong biological activity with minimal cardiovascular and hepatic toxicity, making it suitable for neurodegenerative research. Its application includes studying the mechanisms of Alzheimer’s disease and developing potential therapeutic strategies to mitigate its progression.
  49. Memapsin 2 Inhibitor

    OM99-2 TFA is a potent, tight-binding inhibitor of human brain memapsin 2, exhibiting a Ki value of 9.58 nM. This eight-residue peptidomimetic is instrumental in advancing research on BACE1 inhibitors. OM99-2 TFA holds significant potential for studying the pathophysiology of Alzheimer's disease and may contribute to the development of therapeutic strategies targeting this condition.
  50. β-Secretase Inhibitor

    GL189 is a potent β-secretase inhibitor that exerts neuroprotective effects. This compound is valuable for investigating therapeutic strategies in neurodegenerative diseases, particularly in the context of amyloid plaque formation in Alzheimer's disease. Its ability to modulate β-secretase activity makes it a critical tool for researchers studying mechanisms of neurodegeneration and potential interventions.

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