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-P10077
    GL189
    		Inhibitor
    GL189 is a β-secretase inhibitor. GL189 has neuroprotective effect, and can be used for research of neurodegenerative diseases.
    GL189
  • HY-13438A
    AZD3839 fumarate
    		Inhibitor
    AZD3839 fumarate 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 fumarate inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 fumarate inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 fumarate binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 fumarate can be used in the field of Alzheimer's disease research.
    AZD3839 fumarate
  • HY-153255
    BACE1-IN-13
    		Inhibitor
    BACE1-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.
    BACE1-IN-13
  • HY-182429
    NB-533
    		Inhibitor
    NB-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.
    NB-533
  • HY-100740B
    Lanabecestat camsylate
    		Inhibitor
    Lanabecestat (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.
    Lanabecestat camsylate
  • HY-181160
    JNK3/Wnt/β-catenin modulator-1
    		Inhibitor
    JNK3/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.
    JNK3/Wnt/β-catenin modulator-1
  • HY-111894
    BACE-IN-3
    		Inhibitor
    BACE-IN-3 (Example 3) is a BACE inhibitor, with an IC50 of 0.004 μM.
    BACE-IN-3
  • HY-11014
    NB-216
    		Inhibitor
    NB-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.
    NB-216
  • HY-114245B
    Se-Methylselenocysteine hydrochloride
    		Inhibitor
    Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis.
    Se-Methylselenocysteine hydrochloride
  • HY-147659
    AChE/BChE/BACE-1-IN-2
    		Inhibitor
    AChE/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.
    AChE/BChE/BACE-1-IN-2
  • 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-W744263
    Eslicarbazepine Acetate-d3
    Eslicarbazepine Acetate-d3 is the deuterium 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>3</sub>
  • 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-114234
    TAK-070 hydrochloride hydrate
    		Inhibitor
    TAK-070 hydrochloride hydrate is a noncompetitive and orally active BACE1 inhibitor (IC50 = 3.15 μM). TAK-070 hydrochloride hydrate can be used for research of Alzheimer’s disease (AD). TAK-070 hydrochloride hydrate inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model.
    TAK-070 hydrochloride hydrate
  • 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-173226
    BACE1-IN-15
    		Inhibitor
    BACE1-IN-15 (Compound 72) is a selective inhibitor of beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1) with oral activity and the ability to penetrate the blood-brain barrier. Its IC50 value is 121.65 nM (the IC50 value for BACE-2 is 480.92 nM). BACE1-IN-15 can be used in the research of the Alzheimer's disease field
    BACE1-IN-15
  • 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-164956
    TB-9
    		Inhibitor
    TB-9, a Tasiamide B (HY-N15154) derivative, is a potent cathepsin D, cathepsin E, and BACE1 inhibitor with IC50s of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively.
    TB-9
Cat. No. Product Name / Synonyms Application Reactivity
Beta-secretase Isoform Comparison

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