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-100740B
    Lanabecestat camsylate
    Inhibitor
    Lanabecestat camsylate is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat camsylate is used for the research of Alzheimer's disease.
    Lanabecestat camsylate
  • 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-P2714
    SEVNLDAEFR
    SEVNLDAEFR is a substrate for BACE1.
    SEVNLDAEFR
  • HY-114234A
    TAK-070 Free base
    Inhibitor
    TAK-070 Free base is a noncompetitive and orally active BACE1 inhibitor (IC50: 3.15 μM). TAK-070 Free base can be used for research of Alzheimer’s disease (AD). TAK-070 Free base inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model.
    TAK-070 Free base
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity

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