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Beta-Secretase

Beta-secretase is a protein family that includes in humans Beta-secretase 1 and Beta-secretase 2. Beta-secretase 1, also known as beta-site amyloid precursor protein cleaving enzyme 1, beta-site APP cleaving enzyme 1 (BACE1), membrane-associated aspartic protease 2, memapsin-2, aspartyl protease 2, and ASP2, is an enzyme that in humans is encoded by the BACE1 gene. Expression of BACE1 is observed mainly in neurons. BACE1 is an aspartic acid protease important in the formation of myelin sheaths in peripheral nerve cells: in mice the expression of BACE1 is high in the postnatal stages, when myelination occurs. The transmembrane protein contains two active site aspartate residues in its extracellular protein domain and may function as a dimer, its cytoplasmic tail is required for the correct maturation and an efficient intracellular trafficking, but doesn't affect the activity. It is produced as a pro-enzyme, the endoproteolitc removal occurs after BACE leaves Endoplasmic reticulum, in the Golgi apparatus. In addition the pro-peptide receives additional sugars to increase the molecular mass. and the tail became a palmitoylated. Beta-secretase 2 (also known as Memapsin-1) is an enzyme that cleaves Glu-Val-Asn-Leu!Asp-Ala-Glu-Phe in the Swedish variant of Alzheimer's amyloid precursor protein. BACE2 is a close homolog of BACE1.

  • Aloenin
    T2S118138412-46-3
    1. Aloenin (Aloenin A) and aloe-emodin are active principles for inhibition of c-ADH and c-ALDH activities in vitro.
    • $89
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  • Sophoflavescenol
    TN2217216450-65-6
    Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflaves
    • $657
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  • β-Secretase inhibitor-STA
    T3161350228-37-4
    BACE-IN-1 is amyloid precursor protein beta-secretase inhibitor
    • $152
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  • Cassiaside
    TN147213709-03-0
    Cassiaside is a naphthyl ketone glycoside that inhibits BACE1 (IC50= 4.45 μM; Ki=9.85 μM).Cassiaside exhibits significant hepatoprotective effects against galactosamine injury and has potential anti-Alzheimer's disease (AD) activity.
    • $84
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  • Scoulerine
    TN21906451-73-6
    Scoulerine is an inhibitor of ß-site amyloid precursor protein cleaving enzyme 1(BACE1). Scoulerine a potent antimitotic compound that inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
    • $127
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  • AZD3839 free base
    T67721227163-84-9
    AZD3839 free base is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
    • $48
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  • Tenuifolin
    T376920183-47-5
    Tenuifolin has no inherent toxicity to either the transfected or wild type cells at the effective concentrations, it inhibits amyloid-β secretion in vitro.
    • $41
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  • BACE1-IN-13
    T790221397683-26-9
    BACE1-IN-13 (Compound 36), an orally active inhibitor of BACE1, exhibits high potency with an IC50 of 2.9 nM and demonstrates greater efficacy in hAβ42 cells (IC50 = 1.3 nM). It is considered safe for the cardiovascular system and induces a sustained reduction of Aβ42 in both mouse and dog animal models [1].
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  • Epiberberine
    T5S23616873-09-2
    1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.
    • $31
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  • Verubecestat
    T70111286770-55-5
    Verubecestat (MK-8931) (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.
    • $34
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  • LX2343
    T4398333745-53-2
    LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.
    • $36
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  • LY2886721
    T60581262036-50-9
    LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.
    • $31
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  • Epiberberine chloride
    T8306889665-86-5
    Epiberberine chloride (Epiberberine (chloride)) is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor (IC50s: 1.07, 6.03 and 8.55 μM).
    • $54
    5 days
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  • RE(EDANS)EVNLDAEFK(DABCYL)R
    T80128310427-94-2
    RE (EDANS) EVNLDAEFK (DABCYL) R is a double-labeled peptide with EDANS and DABCYL, functioning as a fluorescent substrate for BACE1 with an emission wavelength of 360 nm and an excitation wavelength of 528 nm. Its utility lies in the quantification of BACE1 activity, with the intensity of fluorescence being directly proportional to enzyme activity levels [1].
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  • LY2811376
    T26391194044-20-6
    LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.
    • $48
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  • Aloeresin D
    T8179105317-67-7
    Aloeresin D, a natural chromone glycoside, inhibits β-Secretase (BACE1) activity (IC50: 39 μM).
    • $81
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  • Eslicarbazepine
    T3285L104746-04-5
    Eslicarbazepine (Stedesa) can be used for adjunctive therapy for adults with partial-onset seizures.
    • $47
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  • Se-Methylselenocysteine hydrochloride
    T78587863394-07-4
    Se-Methylselenocysteine hydrochloride, a precursor to Methylselenol, exhibits significant cancer chemopreventive and antioxidant activities. It is orally bioavailable and promotes apoptosis [1] [2].
    • $143
    35 days
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  • Eslicarbazepine Acetate
    T3285236395-14-5
    Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy.
    • $32
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  • BACE1-IN-10
    T730762799658-44-7
    BACE1-IN-10 is a potent inhibitor of BACE1, demonstrating sub-micromolar activity against recombinant BACE1 (rBACE1) [1].
    • $2,120
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  • Elenbecestat
    T111751388651-30-6
    Elenbecestat (E2609) is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.
    • $64
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