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BACE1 inhibitor
LY2886721 is a novel potent agent that is used to treat Alzheimer's Disease in preclinical experiments.- Naomi Ito, .et al. , Br J Pharmacol, 2017, Mar; 174(5): 386-395 PMID: 28012171
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BACE1 inhibitor
BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively. -
BACE1 inhibitor
Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. -
BACE1 Inhibitor
Timosaponin B-II is a major active component of Anemarrhena asphodeloides Bunge (Liliaceae, rhizome) that has protective effects against cerebral ischaemic damage. -
β-secretase/BACE1 inhibitor
Verubecesta is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. -
BACE1 inhibitor
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer's disease. -
BACE-1 inhibitor
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. - Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
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BACE1 inhibitor
BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM. -
BACE-1 inhibitor
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor for the treatment of Alzheimer's disease (AD). -
BACE-1 inhibitor
BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC50 of 56 nM. -
BACE1 inhibitor
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay. -
BACE-1 inhibitor
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively. -
BACE1 inhibitor
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.

