2. シグナル伝達
  3. Neuronal Signaling
  4. Beta-secretase

Beta-secretase

BACE; β-Secretase

Beta-secretase

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Beta-secretase (BACE) is a transmembrane aspartic proteinase responsible for cleaving the amyloid precursor protein (APP) to generate the soluble ectodomain sAPPbeta and its C-terminal fragment CTFbeta. BACE is a major target of Alzheimer's disease (AD) therapeutics. There are two forms of the enzyme: BACE1 and BACE2.

Deposition of amyloid-β protein (Aβ) to form neuritic plaques is the characteristic neuropathology of Alzheimer's disease (AD). Aβ is generated from APP by β- and γ-secretase cleavages. BACE1 is the β-secretase and its inhibition induces severe side effects, whereas its homolog BACE2 normally suppresses Aβ by cleaving APP/Aβ at the θ-site (Phe20) within the Aβ domain.

Beta-secretase Isoform Specific Products:

Beta-secretase Isoform Comparison
製品番号 製品名 製品効果 純度 構造式
  • HY-130244
    BACE1-IN-5 Inhibitor
    BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.
    BACE1-IN-5
  • HY-112444
    BACE1-IN-2 Inhibitor
    BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM.
    BACE1-IN-2
  • HY-131068
    BACE-1 inhibitor 2 Inhibitor
    BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay.
    BACE-1 inhibitor 2
  • HY-128594
    BACE1-IN-4 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.
    BACE1-IN-4
  • HY-128774
    AM-6494 Inhibitor
    AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM). AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AM-6494
  • HY-13240A
    LY2886721 hydrochloride Inhibitor
    LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
    LY2886721 hydrochloride
  • HY-118098
    LY3202626 Inhibitor
    LY3202626 is a CNS penetrant BACE inhibitor with IC50s of 0.615 nM and 0.871 nM against BACE1 and BACE2, respectively.
    LY3202626
  • HY-112297
    BACE-1 inhibitor 1 Inhibitor
    BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC50 of 56 nM.
    BACE-1 inhibitor 1
  • HY-132895
    JNJ-67569762 Inhibitor
    JNJ-67569762 is a selective BACE1 inhibitor targeting the S3 pocket (IC50 = 2.7 nM).
    JNJ-67569762
  • HY-147658
    AChE/BChE/BACE-1-IN-1 Inhibitor
    AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-1 has remarkable antioxidant potential.
    AChE/BChE/BACE-1-IN-1
  • HY-P990343
    Anti-BACE1 Antibody
    Anti-BACE1 Antibody is a CHO-expressed human antibody that targets BACE1. The predicted molecular weight (MW) of Anti-BACE1 Antibody is 145 kDa. The isotype control for Anti-BACE1 Antibody can be referred to as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-BACE1 Antibody
  • HY-112313
    CTS-21166 Inhibitor
    CTS-21166 is a blood-brain barrier-permeable and orally active BACE1 inhibitor. CTS-21166 reduces brain Aβ levels. CTS-21166 can be used in the research of Alzheimer's disease.
    CTS-21166
  • HY-162127
    hAChE/hBACE-1-IN-3 Inhibitor
    hAChE/hBACE-1-IN-3 (Compound 23a) is a mixed-type inhibitor of hAChE and hBACE-1 with IC50 values of 0.32 μM and 0.39 μM, respectively, Ki values of 0.26 μM and 0.46 μM, respectively. hAChE/hBACE-1-IN-3 can penetrate the blood-brain barrier.
    hAChE/hBACE-1-IN-3
  • HY-114937
    (R)-Eslicarbazepine acetate Control
    (R)-Eslicarbazepine acetate (BIA 2-059) is the R-enantiomer of Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate is an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    (R)-Eslicarbazepine acetate
  • HY-182786
    MAO-B-IN-56 Inhibitor
    MAO-B-IN-56 is a multi-target-directed ligand with AChE, BChE, MAO-B, and BACE1 inhibitory activity, with IC50 values of 0.35 μM, 3.22 μM, 0.14 μM, and 3.85 μM respectively, and shows selectivity for AChE over BChE and MAO-B over MAO-A.MAO-B-IN-56 reduces amyloid-beta production, reduces paw edema, improves spatial memory, and enhances Alzheimer's disease hallmarks and associated histopathological alterations.MAO-B-IN-56 can be used for the research of alzheimer's disease.
    MAO-B-IN-56
  • HY-145345
    BACE1-IN-6 Inhibitor
    BACE1-IN-6 is a BACE1 inhibitor with an IC50 value of 1.5 nM.
    BACE1-IN-6
  • HY-157527
    hAChE-IN-7 Inhibitor
    hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research.
    hAChE-IN-7
  • HY-155305
    BuChE-IN-9 Inhibitor
    BuChE-IN-9 (compound 22a) is a potent equine serum-derived BuChE (eqBuChE) inhibitor with an IC50 of 173 nM. BuChE-IN-9 also inhibits human BACE1, Aβ aggregation, mouse GABA transporter 1 (mGAT1) and mGAT4. BuChE-IN-9 has significant antiamnesic properties.
    BuChE-IN-9
  • HY-12938
    AMG-8718 Inhibitor
    AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain.
    AMG-8718
  • HY-147758
    BACE1/2-IN-1 Inhibitor
    BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability.
    BACE1/2-IN-1
製品番号 製品名 / Synonyms Application Reactivity
Beta-secretase Isoform Comparison

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