BACE1
BACE1 (β-site APP-cleaving enzyme 1) is a type I transmembrane aspartyl protease that initiates amyloid precursor protein (APP) processing by cleaving APP at the β-secretase site, thereby generating the N-terminus of amyloid-β (Aβ) peptides and promoting subsequent γ-secretase-dependent Aβ production[1][2]. BACE1 localizes predominantly to acidic intracellular compartments, including endosomes and the trans-Golgi network, where its catalytic activity supports amyloidogenic APP processing and contributes directly to Alzheimer’s disease (AD)-associated amyloid pathology[1][3]. Mechanistically, genetic and biochemical studies demonstrate that BACE1 is the principal β-secretase in the central nervous system, and BACE1 deficiency markedly reduces cerebral Aβ generation, amyloid deposition, and Aβ-associated cognitive impairments in experimental AD models[3]. Beyond APP processing, BACE1 cleaves multiple neuronal membrane proteins involved in axon guidance, synaptic function, neurogenesis, and myelination, indicating broader physiological roles in nervous system development and maintenance[3]. Compared with the closely related isoform BACE2, which preferentially cleaves APP within the Aβ domain and thereby limits Aβ formation, BACE1 functions as the dominant amyloidogenic β-secretase in neurons and remains the primary therapeutic target for reducing pathological Aβ production[3]. Therefore, selective BACE1 inhibitors have been extensively developed as experimental and clinical tools to suppress Aβ generation, although long-term inhibition requires consideration of BACE1-dependent physiological pathways and substrate processing functions[3][4].
References:
- [1]. Yan R. Physiological Functions of the β-Site Amyloid Precursor Protein Cleaving Enzyme 1 and 2. Front Mol Neurosci. 2017 Apr 19;10:97. doi: 10.3389/fnmol.2017.00097. PMID: 28469554; PMCID: PMC5395628. et al. Physiological Functions of the β-Site Amyloid Precursor Protein Cleaving Enzyme 1 and 2. Front Mol Neurosci. 2017 Apr 19;10:97. [Content Brief]
- [2]. Vassar R. BACE1 inhibitor drugs in clinical trials for Alzheimer's disease. Alzheimers Res Ther. 2014 Dec 24;6(9):89. doi: 10.1186/s13195-014-0089-7. PMID: 25621019; PMCID: PMC4304279. et al. BACE1 inhibitor drugs in clinical trials for Alzheimer's disease. Alzheimers Res Ther. 2014 Dec 24;6(9):89. [Content Brief]
- [3]. Bartolić M, et al. BACE1: Biological Functions and Involvement in the Pathophysiology of Alzheimer's Disease and Other Neurological Disorders. Biofactors. 2025 Nov-Dec;51(6):e70071. [Content Brief]
All Product Categories
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BACE1 Related Products (64)
Related Products (64)
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(1α,1'S,4β)-Lanabecestat
0 ImagesCat. No.: HY-100740CCAS No.: 1384082-96-5Synonyms: (1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
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Epiberberine
0 ImagesEpiberberine 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 has antioxidant activity, with peroxynitrite ONOO- scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberinecan be used for the research of diabetic disease.
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BACE1-IN-5
0 ImagesCat. No.: HY-130244CAS No.: 2581114-83-0
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BACE1-IN-2
0 ImagesCat. No.: HY-112444CAS No.: 1352416-78-4BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM.
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AM-6494
0 ImagesCat. No.: HY-128774CAS No.: 1874232-80-0AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM). AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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GFAP/NF-κB/APOE/NLRP3-IN-1
0 ImagesCat. No.: HY-183796GFAP/NF-κB/APOE/NLRP3-IN-1 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.
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8-Geranyloxy-5-methoxypsoralen
0 ImagesCat. No.: HY-N18261CAS No.: 17182-52-48-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.
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MAO-B-IN-56
0 ImagesCat. No.: HY-182786MAO-B-IN-56 is a multi-target-directed ligand with AChE, BChE, MAO-B, and BACE1 inhibitory activity, with IC50 values of 0.35 μM, 3.22 μM, 0.14 μM, and 3.85 μM respectively, and shows selectivity for AChE over BChE and MAO-B over MAO-A.MAO-B-IN-56 reduces amyloid-beta production, reduces paw edema, improves spatial memory, and enhances Alzheimer's disease hallmarks and associated histopathological alterations.MAO-B-IN-56 can be used for the research of alzheimer's disease.
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Ambrosin
0 ImagesAmbrosin is an orally active NF-κβ and BACE1 inhibitor. Ambrosin reduces pro-inflammatory and nitrosative mediators, increases PPARγ levels, inhibits apoptosis (Apoptosis), enhances autophagy (Autophagy), and ameliorates oxidative stress. Ambrosin reduces Amyloid plaque deposition. Ambrosin improves lipopolysaccharide-induced memory impairment and colonic histopathological changes. Ambrosin can be used in research related to Alzheimer's disease and colitis.
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BACE1/2-IN-1
0 ImagesCat. No.: HY-147758CAS No.: 2671036-34-1
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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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BACE1-IN-10
0 ImagesCat. No.: HY-P3426CAS No.: 2799658-44-7
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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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BACE1-IN-16
0 ImagesCat. No.: HY-189149BACE1-IN-16 is a BACE1 inhibitor with pIC50 values ranging from 7.09 to 9.70. BACE1-IN-16 can be used for research on Alzheimer's disease.
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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.
