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  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • 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-N13064
    2,2′,4,4′-Tetrahydroxychalcone
    		Inhibitor
    2,2′,4,4′-Tetrahydroxychalcone (Compound 18) is a selective and potent BACE1 inhibitor with an IC50 of 0.62 μM. 2,2′,4,4′-Tetrahydroxychalcone is a derivative of Isoliquiritigenin (HY-N0102) found in Glycyrrhiza uralensis. 2,2′,4,4′-Tetrahydroxychalcone can block the β-cutting step of amyloid precursor protein (APP), thereby reducing the production of β-amyloid (Aβ) peptide. 2,2′,4,4′-Tetrahydroxychalcone can be used for research of Alzheimer’s disease.
    2,2′,4,4′-Tetrahydroxychalcone
  • HY-125405
    AZ3971
    		Inhibitor
    AZ3971 is an orally active, blood-brain barrier permeable BACE1 inhibitor that does not affect the activity of γ-secretase. AZ3971 reduces the production of Aβ. AZ3971 can be used for the research of Alzheimer's disease.
    AZ3971
  • 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-RS01337
    Bace2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Bace2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bace2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Bace2 Mouse Pre-designed siRNA Set A
  • 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-172176
    RA-PR058
    		Inhibitor
    RA-PR058 is an orally active Ramalin derivative with blood-brain barrier permeability, exhibiting multi-target regulatory effects and favorable pharmacokinetic properties. RA-PR058 demonstrates potential as a multi-target modulator for Alzheimer's disease by reducing the expression of BACE1, tau protein hyperphosphorylation, and anxiety-like behaviors.
    RA-PR058
  • 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-d<sub>4</sub>
  • 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-175661
    SRI-22136
    		Inhibitor
    SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.
    SRI-22136
  • HY-RS01335
    Bace1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Bace1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bace1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Bace1 Rat Pre-designed siRNA Set A
  • HY-178374
    BACE-1/Mpro-IN-1
    		Inhibitor
    BACE-1/Mpro-IN-1 is a high brain-penetrant BACE-1 (IC50 = 0.26 μM) and SARS-CoV-2 Mpro (IC50 = 0.91 μM) dual inhibitor. BACE-1/Mpro-IN-1 binds to the aspartyl protease and cysteine protease as a mixed-type inhibitor. BACE-1/Mpro-IN-1 exhibits the most favorable docking score and a strong interaction profile. BACE-1/Mpro-IN-1 can be used for the study of COVID-19 exacerbated Neuroinflammation and Alzheimer’s disease.
    BACE-1/Mpro-IN-1
  • 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-165226
    β-Secretase-IN-5
    		Inhibitor
    β-Secretase-IN-5 is a Beta-secretase inhibitor. β-Secretase-IN-5 reduces the production of Aβ1-40 and Aβ1-42. β-Secretase-IN-5 is applicable to research related to Alzheimer's disease.
    β-Secretase-IN-5
  • HY-114703S
    Eslicarbazepine-d3
    Eslicarbazepine-d3 (BIA 2-194-d3) is the deuterium labeled Eslicarbazepine (HY-114703). Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
    Eslicarbazepine-d<sub>3</sub>
  • HY-RS01338
    Bace2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Bace2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bace2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Bace2 Rat Pre-designed siRNA Set A
  • 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-176132
    BI 1181181 MZ
    		Inhibitor
    BI 1181181 MZ is a potent and selective BACE1 inhibitor. BI 1181181 MZ can be used in the research for Alzheimer’s disease.
    BI 1181181 MZ
Art. -Nr. Produktname / Synonyms Application Reactivity
Beta-secretase Isoform Comparison

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