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-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.
    hAChE-IN-7
  • 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.
    BuChE-IN-9
  • HY-12938
    AMG-8718
    		Inhibitor
    AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain.
    AMG-8718
  • 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.
    BACE1/2-IN-1
  • 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).
    AChE/BACE1/GSK3β-IN-1
  • HY-P3426
    BACE1-IN-10
    		Inhibitor
    BACE1-IN-10 is a potent BACE1 Inhibitor. BACE1-IN-10 shows sub-micromolar activity against recombinant BACE1 (rBACE1).
    BACE1-IN-10
  • HY-126548
    β-Secretase Inhibitor I
    		Inhibitor
    β-Secretase Inhibitor I is an extremely potent β-secretase inhibitor with reduced cardiovascular and liver toxicity.
    β-Secretase Inhibitor I
  • HY-B0703S
    Eslicarbazepine acetate-d4
    		Inhibitor
    Eslicarbazepine acetate-d4 is deuterated labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    Eslicarbazepine acetate-d4
  • HY-108966
    Kushenol C
    		Inhibitor
    Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM.
    Kushenol C
  • HY-N3734
    Deoxyneocryptotanshinone
    		Inhibitor
    Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research.
    Deoxyneocryptotanshinone
  • HY-149211
    AChE/BChE-IN-12
    		Inhibitor
    AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.
    AChE/BChE-IN-12
  • HY-P2713A
    OM99-2 TFA
    		Inhibitor
    OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM. OM99-2 TFA is significantly advanced the development of BACE1 inhibitor. OM99-2 has the potential for the research of the Alzheimer's disease.
    OM99-2 TFA
  • HY-122080
    Memoquin
    		Inhibitor
    Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD).
    Memoquin
  • HY-P4919
    Mca-SEVNLDAEFK(Dnp)
    Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (APP) β-secretase cleavage site. Cleavage at -Leu-Asp- of Mca-SEVNLDAEFK(Dnp) liberates the highly fluorescent 7-methoxycoumarin (Mca) fragment from the proximity quenching effect of the 2,4-dinitrophenyl (Dnp) internal quencher resulting in a large and easily detectable increase in fluorescence intensity.
    Mca-SEVNLDAEFK(Dnp)
  • HY-P10077
    GL189
    		Inhibitor
    GL189 is a β-secretase inhibitor. GL189 has neuroprotective effect, and can be used for research of neurodegenerative diseases.
    GL189
  • HY-153255
    BACE1-IN-13
    		Inhibitor
    BACE1-IN-13 (Compound 36) is an orally active BACE1 inhibitor with an IC50 value of 2.9 nM. BACE1-IN-13 is highly potent in hAβ42 cell (IC50 = 1.3 nM). BACE1-IN-13 has cardiovascularly safty and elicits sustained Aβ42 reduction in mouse and dog animal models.
    BACE1-IN-13
  • HY-N2215
    Aloeresin D
    		Inhibitor 99.69%
    Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC50 of 39 μM.
    Aloeresin D
  • HY-111894
    BACE-IN-3
    		Inhibitor
    BACE-IN-3 (Example 3) is a BACE inhibitor, with an IC50 of 0.004 μM.
    BACE-IN-3
  • HY-114245B
    Se-Methylselenocysteine hydrochloride
    		Inhibitor
    Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis.
    Se-Methylselenocysteine hydrochloride
  • HY-147659
    AChE/BChE/BACE-1-IN-2
    		Inhibitor
    AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 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-2 has remarkable antioxidant potential.
    AChE/BChE/BACE-1-IN-2
Cat. No. Product Name / Synonyms Application Reactivity
Beta-secretase Isoform Comparison

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