1. Signaling Pathways
  2. Neuronal Signaling
  3. Beta-secretase

Beta-secretase

BACE; β-Secretase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16759
    Verubecestat
    Inhibitor 99.56%
    Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
    Verubecestat
  • HY-114245
    Se-Methylselenocysteine
    Inhibitor ≥98.0%
    Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis.
    Se-Methylselenocysteine
  • HY-100740
    Lanabecestat
    Inhibitor 99.82%
    Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease.
    Lanabecestat
  • HY-13240
    LY2886721
    Inhibitor 99.74%
    LY2886721 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 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
    LY2886721
  • HY-N0226A
    Epiberberine chloride
    Inhibitor 99.03%
    Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO- scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.
    Epiberberine chloride
  • 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-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-10472
    LY2811376
    Inhibitor 99.89%
    LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
    LY2811376
  • HY-124322
    NB-360
    Inhibitor 99.22%
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E.
    NB-360
  • HY-109052
    Atabecestat
    Inhibitor 99.77%
    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. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment.
    Atabecestat
  • HY-N1255
    Scoulerine
    Inhibitor 99.27%
    Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
    Scoulerine
  • HY-109055
    Elenbecestat
    Inhibitor 99.94%
    Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
    Elenbecestat
  • HY-10133
    β-Secretase Inhibitor IV
    Inhibitor 99.87%
    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.
    β-Secretase Inhibitor IV
  • HY-13438
    AZD3839 free base
    Inhibitor 99.98%
    AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease.
    AZD3839 free base
  • HY-136742
    BACE2-IN-1
    Inhibitor 99.34%
    BACE2-IN-1 (compound 3l) is a highly selective BACE2 inhibitor with a Ki value of 1.6 nM. BACE2 inhibitors can be used to research of Type 2 Diabetes.
    BACE2-IN-1
  • HY-N0702
    Tenuifolin
    Inhibitor ≥99.0%
    Tenuifolin is effective and has a protective action. Tenuifolin inhibits β-secretase decreases Aβ protein secretion, suppresses Aβ25-35 secretion, and subsequently caspase-3 and caspase-9 become active. Tenuifolin's ability to lower AChE activity, increase at the same time, increase the ability of the upper glands, and improve the ability to read and remember. Research on tenuifolin's potential for use in urinary disease (AD).
    Tenuifolin
  • HY-114703
    Eslicarbazepine
    Inhibitor 99.43%
    Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
    Eslicarbazepine
  • HY-B0703
    Eslicarbazepine acetate
    Inhibitor 99.98%
    Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    Eslicarbazepine acetate
  • HY-100182
    BACE1-IN-1
    Inhibitor 99.02%
    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-IN-1

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