Beta-secretase (BACE)

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  1. BACE1 inhibitor

    LY2886721 is a novel potent agent that is used to treat Alzheimer's Disease in preclinical experiments.
  2. BACE1 inhibitor

    Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  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. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. Lanabecestat Enantiomer

    (1α,1'S,4β)-Lanabecestat is the less active enantiomer of the BACE1 inhibitor, Lanabecestat. This compound exhibits effective inhibition of BACE1, a key enzyme involved in the amyloidogenic pathway associated with Alzheimer's disease. With a potent Ki of 0.4 nM for its active form, (1α,1'S,4β)-Lanabecestat serves as a valuable tool for research on Alzheimer's therapeutics and the role of BACE1 in neurodegenerative processes.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. Beta-secretase

    Lanabecestat hydrochloride is a potent inhibitor of beta-secretase (BACE1), primarily employed in the research of Alzheimer's disease. This compound effectively reduces amyloid beta peptide concentrations in plasma, cerebrospinal fluid, and brain tissue in a dose- and time-dependent manner. While demonstrating a reduction in Aβ neuritic plaque burden, lanabecestat has not shown clinical benefits or the ability to slow Alzheimer's disease progression. It serves as a valuable tool for studying the mechanisms underlying amyloid pathology and evaluating potential therapeutic approaches.
  41. 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.
  42. 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.
  43. 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.
  44. BACE1 Substrate

    SEVNLDAEFR is a specific substrate for the beta-site amyloid precursor protein cleaving enzyme 1 (BACE1). This peptide is utilized in biochemical assays to study BACE1 activity and amyloid beta peptide generation, which are crucial in Alzheimer's disease research. Its application in research facilitates the investigation of potential therapeutic strategies targeting BACE1-mediated pathways.
  45. 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.
  46. 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.
  47. 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.
  48. BACE1 inhibitor

    AZD3839 is a potent and selective inhibitor of human BACE1 with Ki of 26.1 nM.
  49. nonsteroidal glucocorticoid receptor agonist

    AZD5423 is a novel nonsteroidal glucocorticoid receptor agonist.
  50. BACE1 inhibitor

    LY2811376 is the first orally available non-peptidic BACE1 inhibitor that produces profound Aβ-lowering effects in animals.

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