2. Signaling Pathways
  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
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114245
    Se-Methylselenocysteine
    		Inhibitor 99.95%
    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-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-N0226A
    Epiberberine chloride
    		Inhibitor 98.91%
    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-13240
    LY2886721
    		Inhibitor 99.72%
    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-15908
    BCA
    		Inhibitor 99.99%
    BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD).
    BCA
  • HY-N1255A
    Scoulerine hydrochloride
    		Inhibitor
    Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer.
    Scoulerine hydrochloride
  • HY-183796
    GFAP/NF-κB/APOE/NLRP3-IN-1
    		Inhibitor
    GFAP/NF-κB/APOE/NLRP3-IN-1 (Compound 11a) is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC50 of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC50 of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ1-42 aggregation with an IC50 of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma.
    GFAP/NF-κB/APOE/NLRP3-IN-1
  • HY-N18261
    8-Geranyloxy-5-methoxypsoralen
    		Inhibitor
    8-geranyloxy-5-methoxypsoralen is a BACE1 inhibitor with an IC50 of 11.1 μM. 8-geranyloxy-5-methoxypsoralen potently inhibits BACE1 activity. 8-Geranyloxy-5-methoxypsoralen can be used for the research of Alzheimer's disease.
    8-Geranyloxy-5-methoxypsoralen
  • HY-N1255
    Scoulerine
    		Inhibitor 99.99%
    Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine is applicable to research related to leukemia, ovarian cancer, and colorectal cancer.
    Scoulerine
  • HY-100740
    Lanabecestat
    		Inhibitor 99.87%
    Lanabecestat (AZD3293; LY3314814) 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-119689
    Umibecestat
    		Inhibitor 99.81%
    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. Umibecestat can be used for the research of alzheimer's disease.
    Umibecestat
  • HY-109055
    Elenbecestat
    		Inhibitor 99.82%
    Elenbecestat (E2609) is a potent, orally bioavailable and BBB-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
    Elenbecestat
  • HY-10472
    LY2811376
    		Inhibitor 99.64%
    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-136742
    BACE2-IN-1
    		Inhibitor 99.4%
    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-10133
    β-Secretase Inhibitor IV
    		Inhibitor 99.19%
    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-13769A
    TPT-260 Dihydrochloride
    		98.0%
    TPT-260 Dihydrochloride (NSC55712), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 Dihydrochloride increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 Dihydrochloride inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 Dihydrochloride improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 Dihydrochloride exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 Dihydrochloride can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease.
    TPT-260 Dihydrochloride
  • HY-B0703
    Eslicarbazepine acetate
    		Inhibitor 99.92%
    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-13438
    AZD3839 free base
    		Inhibitor 99.97%
    AZD3839 is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 can be used in the field of Alzheimer's disease research.
    AZD3839 free base
  • HY-N0702
    Tenuifolin
    		Inhibitor 99.73%
    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 99.94%
    Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
    Eslicarbazepine
Cat. No. Product Name / Synonyms Application Reactivity
Beta-secretase Isoform Comparison

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