2. Neuronal Signaling
  3. Beta-secretase

Beta-secretase

Beta-secretase

Related Products

PDF 0.56 MB

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 Related Products (71):

Cat. No. Product Name Effect Purity
  • 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[1].
  • 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[1][2].
  • HY-N0226A
    Epiberberine chloride Inhibitor 99.02%
    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[1]. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways[2]. Epiberberine has the potential effect in the research of diabetic disease[3].
  • HY-114245
    Se-Methylselenocysteine Inhibitor
    Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis[1][2].
  • 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[1].
  • 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[1].
  • 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[1].
  • HY-161359
    BACE1-IN-14 Inhibitor
    BACE1-IN-14 (compound 27f) is a BACE1 inhibitor, with the EC50 values of 0.7 μM and 1.6 μM for BACE1 and BACE2. BACE1-IN-14 is can be used in Alzheimer's disease (AD) research[1].
  • HY-119689
    Umibecestat Inhibitor 99.88%
    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[1]. Umibecestat can be used for the research of alzheimer's disease.
  • 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[1].
  • 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[1].
  • 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[1][2].
  • 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[1].
  • 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[1].
  • HY-145345
    BACE1-IN-6 Inhibitor
    BACE1-IN-6 is a BACE1 inhibitor with an IC50 value of 1.5 nM.
  • 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[1].
  • 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[1][2].
  • 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[1].
  • HY-112157
    PF-06751979 Inhibitor 99.23%
    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.
  • HY-151260
    AChE/BACE1/GSK3β-IN-1 Inhibitor
    AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD)[1].