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-161359
    BACE1-IN-14
    		Inhibitor
    BACE1-IN-14 (compound 27f) is a BACE1 inhibitor, with the EC50 values of 0.7 μM and 1.6 μM for BACE1 and BACE2. BACE1-IN-14 is can be used in Alzheimer's disease (AD) research.
    BACE1-IN-14
  • HY-147870
    COX-2-IN-22
    		Inhibitor
    COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB.
    COX-2-IN-22
  • HY-144739
    BACE1-IN-8
    		Inhibitor
    BACE1-IN-8 (compound 70b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 3.9 µM.
    BACE1-IN-8
  • HY-136813
    Multitarget AD inhibitor-1
    		Inhibitor
    Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research.
    Multitarget AD inhibitor-1
  • HY-159151
    AChE/Aβ-IN-6
    		Inhibitor
    BACE1-IN-15 (compound 4j) is a potent inhibitor of BACE1 (β-secretase) that can inhibited the copper ion induced Aβ toxicity, with the EC50 of 0.68 μM.
    AChE/Aβ-IN-6
  • HY-151348
    BACE1-IN-11
    		Inhibitor
    BACE1-IN-11 is a BACE1 inhibitor. BACE1-IN-11 has the BACE1 inhibitory activity with an IC50 value of 72 μM. BACE1-IN-11 can be used for the research of Alzheimer’s disease (AD) .
    BACE1-IN-11
  • HY-158261
    AChE-IN-63
    		Inhibitor
    AChE-IN-63 (Compound 5AD) is a selective inhibitor of hAChE (IC50=0.103 μM). AChE-IN-63 also inhibits hBChE and hBACE-1 (IC50= 10 μM (hBChE); 1.342 μM (hBACE-1)). AChE-IN-63 inhibits Aβ aggregation, preventing the formation and deposition of Aβ1-42. AChE-IN-63 can effectively penetrate the blood-brain barrier and is orally effective. It is primarily used in Alzheimer's disease research.
    AChE-IN-63
  • HY-147851
    BACE1-IN-12
    		Inhibitor
    BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent.
    BACE1-IN-12
  • HY-139720
    β-Secretase Inhibitor III
    		Inhibitor
    β-Secretase Inhibitor III is an extremely selective BACE1 inhibitor (Ki = 0.13 nM).
    β-Secretase Inhibitor III
  • HY-163885
    SSZ
    		Inhibitor
    SSZ is a multi-target inhibitor, which targets multiple pathological mechanisms of Alzheimer's disease (AD). SSZ targets acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. SSZ ameliorates Alzheimer’s diseases and exhibits neuroprotective effect in mice.
    SSZ
  • HY-P2713
    OM99-2
    		Inhibitor
    OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM. OM99-2 is significantly advanced the development of BACE1 inhibitor. OM99-2 has the potential for the research of the Alzheimer's disease.
    OM99-2
  • HY-N4186
    Glabrolide
    		Inhibitor
    Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor[1].
    Glabrolide
  • HY-136736
    β-Secretase Inhibitor II
    		Inhibitor
    β-Secretase Inhibitor II is a β-Secretase inhibitor. β-Secretase Inhibitor II is a simple tripeptide aldehyde (IC50=700 nM for inhibition of total Aβ and IC50=2.5 μM for Aβ1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease.
    β-Secretase Inhibitor II
  • HY-N2215R
    Aloeresin D (Standard)
    		Inhibitor
    Aloeresin D (Standard) is the analytical standard of Aloeresin D. This product is intended for research and analytical applications. Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC50 of 39 μM.
    Aloeresin D (Standard)
  • HY-P1962
    β-Secretase inhibitor
    		Inhibitor
    β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) is a β-secretase and BACE1 inhibitor (IC50: 25 nM for β-secretase).
    β-Secretase inhibitor
  • HY-P4899
    RE(EDANS)EVNLDAEFK(DABCYL)R
    RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide，serves as a fluorescent substrate for BACE1(Em=360nm，Ex=528nm). RE (EDANS) EVNLDAEFK (DABCYL) R can be used for BACE1 activity measurement and the enzyme activity level is directly proportional to the fluorescence reaction.
    RE(EDANS)EVNLDAEFK(DABCYL)R
  • HY-144741
    BACE1-IN-9
    		Inhibitor
    BACE1-IN-9 (compound 82b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 1.2 µM.
    BACE1-IN-9
  • HY-149288
    hAChE/hBACE-1-IN-2
    		Inhibitor
    hAChE/hBACE-1-IN-2 is a potent, orally active, blood-brain barrier transboundary triple inhibitor of hAChE, hBChE, and HACE-1 with IC50s of 0.113 μM, 1.48 μM and 0.38 μM, respectively. hAChE/hBACE-1-IN-2 has antioxidant activity. hAChE/hBACE-1-IN-2 also inhibits Aβ11-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease.
    hAChE/hBACE-1-IN-2
  • HY-118098
    LY3202626
    		Inhibitor
    LY3202626 is a CNS penetrant BACE inhibitor with IC50s of 0.615 nM and 0.871 nM against BACE1 and BACE2, respectively.
    LY3202626
  • HY-16759A
    Verubecestat TFA
    		Inhibitor
    Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
    Verubecestat TFA
Cat. No. Product Name / Synonyms Application Reactivity
Beta-secretase Isoform Comparison

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