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-N0702R
    Tenuifolin (Standard)
    Inhibitor
    Tenuifolin (Standard) is the analytical standard of Tenuifolin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-100182R
    BACE1-IN-1 (Standard)
    Inhibitor
    BACE1-IN-1 (Standard) is the analytical standard of BACE1-IN-1 (HY-100182). This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0495R
    Aloenin (Standard)
    Inhibitor
    Aloenin (Standard) is the analytical standard of Aloenin. This product is intended for research and analytical applications. Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
    Aloenin (Standard)
  • HY-100740CR
    (1α,1'S,4β)-Lanabecestat (Standard)
    Inhibitor
    (1α,1'S,4β)-Lanabecestat (Standard) is the analytical standard of (1α,1'S,4β)-Lanabecestat (HY-100740C). This product is intended for research and analytical applications. (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
    (1α,1'S,4β)-Lanabecestat (Standard)
  • HY-126047
    (S)-(-)-Anatabine
    Inhibitor
    (S)-(-)-Anatabine is an NFκB/BACE-1 inhibitor with blood-brain barrier penetration. (S)-(-)-Anatabine inhibits NFκB activation via phosphorylation of its p65 subunit. (S)-(-)-Anatabine inhibits BACE-1 transcription and reduces BACE-1 protein levels. (S)-(-)-Anatabine lowers production of 1-40 and 1-42 by reducing β-cleavage of amyloid precursor protein without affecting α-cleavage. (S)-(-)-Anatabine can be used for the research of Alzheimer's disease.
    (S)-(-)-Anatabine
  • HY-164958
    TB-11
    Inhibitor 98.71%
    TB-11 is a Cathepsin D inhibitor, with IC50s of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), 48.8 nM (BACE1), respectively. TB-11 can be used for tumor research.
    TB-11
  • HY-13769
    TPT-260
    TPT-260 (TPU260), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease.
    TPT-260
  • HY-18112
    AZ-4217
    Inhibitor
    AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research.
    AZ-4217
  • HY-16759B
    Verubecestat tosylate
    Inhibitor
    Verubecestat tosylate is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat tosylate effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
    Verubecestat tosylate
  • HY-10472R
    LY2811376 (Standard)
    Inhibitor
    LY2811376 (Standard) is the analytical standard of LY2811376 (HY-10472). This product is intended for research and analytical applications. 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 (Standard)
  • HY-100740R
    Lanabecestat (Standard)
    Inhibitor
    Lanabecestat (Standard) is the analytical standard of Lanabecestat. This product is intended for research and analytical applications. 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 (Standard)
  • HY-10133R
    β-Secretase Inhibitor IV (Standard)
    Inhibitor
    β-Secretase Inhibitor IV (Standard) is the analytical standard of β-Secretase Inhibitor IV (HY-10133). This product is intended for research and analytical applications. 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 (Standard)
  • HY-114703R
    Eslicarbazepine (Standard)
    Inhibitor
    Eslicarbazepine (Standard) is the analytical standard of Eslicarbazepine. This product is intended for research and analytical applications. Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
    Eslicarbazepine (Standard)
  • HY-P2714
    SEVNLDAEFR
    SEVNLDAEFR is a substrate for BACE1.
    SEVNLDAEFR
  • HY-160037
    SEW06622
    Inhibitor
    SEW06622 is a BACE-1 inhibitor with an IC50 value of 6.3 μM and can be used in Alzheimer's disease research.
    SEW06622
  • HY-N2215R
    Aloeresin D (Standard)
    Inhibitor
    Aloeresin D (Standard) is the analytical standard of Aloeresin D. This product is intended for research and analytical applications. Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC50 of 39 μM.
    Aloeresin D (Standard)
  • HY-138013
    PF-06663195
    Inhibitor
    PF-06663195 is a β-secretase (BACE1) inhibitor, with BACE1 CFA and BACE1 WCA IC50 values of 53 and 15 nM, respectively. PF-06663195 can be used for Alzheimer's disease research.
    PF-06663195
  • HY-16759R
    Verubecestat (Standard)
    Inhibitor
    Verubecestat (Standard) is the analytical standard of Verubecestat. This product is intended for research and analytical applications. 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 (Standard)
  • HY-109055R
    Elenbecestat (Standard)
    Inhibitor
    Elenbecestat (Standard) is the analytical standard of Elenbecestat (HY-109055). This product is intended for research and analytical applications. Elenbecestat (E2609) is a potent, orally bioavailable and BBB-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
    Elenbecestat (Standard)
  • HY-U00287
    BACE-IN-1
    Inhibitor
    BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
    BACE-IN-1
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