Beta-secretase
BACE; β-Secretase
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
All Product Categories
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Beta-secretase Related Products (143)
Related Products (143)
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Antibodies (1)
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Beta-secretase Isoform Comparison
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AChE/BACE1/GSK3β-IN-1
0 ImagesCat. No.: HY-151260CAS No.: 2866066-81-9AChE/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).
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2,2′,4,4′-Tetrahydroxychalcone
0 ImagesCat. No.: HY-N13064CAS No.: 123702-96-52,2′,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.
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AZ3971
0 ImagesCat. No.: HY-125405CAS No.: 1260248-03-0AZ3971 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.
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BACE1-IN-10
0 ImagesCat. No.: HY-P3426CAS No.: 2799658-44-7
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β-Secretase Inhibitor I
0 ImagesCat. No.: HY-126548CAS No.: 1818239-19-8β-Secretase Inhibitor I is an extremely potent β-secretase inhibitor with reduced cardiovascular and liver toxicity.
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BACE1-IN-1 hydrochloride
0 ImagesCat. No.: HY-100182ACAS No.: 1310349-35-9BACE1-IN-1 hydrochloride is an orally active, blood-brain barrier penetrant dual-target inhibitor of BACE1/2, with IC50 values of 23 nM and 24 nM against human BACE1 and BACE2, respectively. BACE1-IN-1 hydrochloride reduces cerebral Aβ40 levels in mice. BACE1-IN-1 hydrochloride can be used in studies related to Alzheimer's disease and type 2 diabetes.
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RA-PR058
0 ImagesCat. No.: HY-172176RA-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.
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Eslicarbazepine acetate-d4
0 ImagesCat. No.: HY-B0703SSynonyms: BIA 2-093-d4Eslicarbazepine 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.
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Deoxyneocryptotanshinone
0 ImagesCat. No.: HY-N3734CAS No.: 27468-20-8Deoxyneocryptotanshinone, 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.
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AChE/BChE-IN-12
0 ImagesCat. No.: HY-149211AChE/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.
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SRI-22136
0 ImagesCat. No.: HY-175661SRI-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.
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BACE-1/Mpro-IN-1
0 ImagesCat. No.: HY-178374BACE-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.
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OM99-2 TFA
0 ImagesCat. No.: HY-P2713ACAS No.: 2504147-81-1OM99-2 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.
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Memoquin
0 ImagesCat. No.: HY-122080CAS No.: 616885-87-1Memoquin 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).
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β-Secretase-IN-5
0 Imagesβ-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.
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Eslicarbazepine-d3
0 ImagesCat. No.: HY-114703SSynonyms: BIA 2-194-d3Eslicarbazepine-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.
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Mca-SEVNLDAEFK(Dnp)
0 ImagesCat. No.: HY-P4919CAS No.: 1802078-31-4Mca-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.
