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
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Beta-secretase Related Products (156)
Related Products (156)
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Antibodies (1)
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Beta-secretase Isoform Comparison
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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.
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GL189
0 ImagesCat. No.: HY-P10077CAS No.: 552337-94-7GL189 is a β-secretase inhibitor. GL189 has neuroprotective effect, and can be used for research of neurodegenerative diseases.
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AZD3839
0 ImagesCat. No.: HY-13438ACAS No.: 1421852-78-9AZD3839 is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 can be used in the field of Alzheimer's disease research.
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BACE1-IN-13
0 ImagesCat. No.: HY-153255CAS No.: 1397683-26-9BACE1-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.
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NB-533
0 ImagesCat. No.: HY-182429CAS No.: 1146544-18-4NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces Aβ40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease.
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Lanabecestat camsylate
0 ImagesCat. No.: HY-100740BCAS No.: 1522418-41-2Synonyms: LY3314814 camsylate; AZD3293 camsylateLanabecestat (AZD3293; LY3314814) camsylate is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat camsylate is used for the research of Alzheimer's disease.
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AChE/BChE-IN-38
0 ImagesCat. No.: HY-189414AChE/BChE-IN-38 is a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50 = 1.22 μM and 0.40 μM; Ki = 0.94 μM and 0.60 μM). AChE/BChE-IN-38 decreases BACE1 and HTR6 mRNA expression in neuroblastoma cells. AChE/BChE-IN-38 improves cognitive and behavioral parameters in a Scopolamine-induced Alzheimer's disease zebrafish model. AChE/BChE-IN-38 is useful for research on Alzheimer's disease.
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JNK3/Wnt/β-catenin modulator-1
0 ImagesCat. No.: HY-181160JNK3/Wnt/β-catenin modulator-1 is a brain-penetrant JNK3 inhibitor and Wnt/β-catenin activator. JNK3/Wnt/β-catenin modulator-1 decreases Aβ1-42 production and reduced ROS generation. JNK3/Wnt/β-catenin modulator-1 inhibits the activation of JNK and Puma, promotes Beclin-1 expression, reduces GSK-3β and BACE1 expression and activates Wnt/β-catenin signaling. JNK3/Wnt/β-catenin modulator-1 improves cognitive and memory performance, attenuates histopathological brain damage, preserves structure of hippocampal pyramidal cells and cerebral cortical neurons. JNK3/Wnt/β-catenin modulator-1 can be used for the research of Alzheimer's disease.
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BACE-IN-3
0 ImagesCat. No.: HY-111894CAS No.: 1388149-39-0BACE-IN-3 (Example 3) is a BACE inhibitor, with an IC50 of 0.004 μM.
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NB-216
0 ImagesCat. No.: HY-11014CAS No.: 943924-04-7NB-216 is an orally active and brain-penetrant BACE-1 inhibitor (IC50 = 17 nM). NB-216 has a strong inhibitory effect on cathepsin D (IC50 = 1 nM) and cathepsin E (IC50 = 0.4 nM). NB-216 can be used for the study of Alzheimer's disease.
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Se-Methylselenocysteine hydrochloride
0 ImagesCat. No.: HY-114245BCAS No.: 863394-07-4Synonyms: Methylselenocysteine hydrochloride; Se-Methylseleno-L-cysteine hydrochloride
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Multitarget AD-IN-8
0 ImagesCat. No.: HY-189262Multitarget AD-IN-8 is a blood-brain barrier-penetrant, orally active multitarget inhibitor. Multitarget AD-IN-8 inhibits abnormal Tau phosphorylation at Thr181 and Ser396 sites and attenuates NF-κB phosphorylation. Multitarget AD-IN-8 downregulates BACE1 expression to reduce Aβ production, inhibits the Bax/Bcl-2 pathway, and suppresses Caspase-1 activation. Multitarget AD-IN-8 attenuates p38, ERK1/2, and JNK phosphorylation and inhibits Aβ25-35-induced Apoptosis. Multitarget AD-IN-8 exhibits neuroprotective effects against Aβ25-35-induced injury, ameliorates learning and memory deficits in AD mouse models, and alleviates hippocampal neuronal pathological damage. Multitarget AD-IN-8 can be used for research on Alzheimer's disease.
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AChE/BChE/BACE-1-IN-2
0 ImagesCat. No.: HY-147659CAS No.: 1877000-20-8AChE/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.
