1. Signaling Pathways
  2. Neuronal Signaling
  3. Beta-secretase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-RS01334
    Bace1 Mouse Pre-designed siRNA Set A
    Inhibitor

    Bace1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bace1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Bace1 Mouse Pre-designed siRNA Set A
  • 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 and IC50=2.5 μM for 1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease.
    β-Secretase Inhibitor II
  • HY-170938
    AChE-IN-82
    Inhibitor
    AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-82 inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50s of 0.072, 9.81, 14.52, 0.024, 2.42 μM, respectively. AChE-IN-82 inhibits COX-1, COX-2 and 5-LOX with IC50s of 60.41, 0.187, 0.18 μM, respectively. AChE-IN-82 shows an excellent neuroprotective effect by significantly reducing oxidative stress induced by H2 O2.
    AChE-IN-82
  • HY-100740A
    Lanabecestat hydrochloride
    Lanabecestat (AZD-3293) hydrochloride is a potent BACE1 inhibitor that has been investigated for its potential as a modifying treatment for Alzheimer's disease. Lanabecestat (hydrochloride) demonstrated significant dose- and time-dependent reductions in concentrations of amyloid beta peptides in plasma, cerebrospinal fluid, and brain. Lanabecestat (hydrochloride) was also shown to produce reductions in Aβ neuritic plaque burden without demonstrating clinical benefits or slowing the progression of Alzheimer's disease pathophysiology.
    Lanabecestat hydrochloride
  • 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-P5274
    BACE1 (485-501)
    BACE1 (485-501) is the carboxyl terminal of BACE1 (Beta-site APP cleaving enzyme 1). BACE1 (485-501) can be used as antigen to produce anti-BACE1-C antibody.
    BACE1 (485-501)
  • 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-114937
    (R)-Eslicarbazepine acetate
    Control
    (R)-Eslicarbazepine acetate (BIA 2-059) is the R-enantiomer of Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate is an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    (R)-Eslicarbazepine acetate
  • HY-114703S1
    Eslicarbazepine-d4
    Inhibitor
    Eslicarbazepine-d4 (BIA 2-194-d4) is deuterium labeled Eslicarbazepine. Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
    Eslicarbazepine-d<sub>4</sub>
  • HY-N0702R
    Tenuifolin (Standard)
    Inhibitor
    Tenuifolin (Standard) is the analytical standard of Tenuifolin. This product is intended for research and analytical applications. Tenuifolin is effective and has a protective action. Tenuifolin inhibits β-secretase decreases Aβ protein secretion, suppresses Aβ25-35 secretion, and subsequently caspase-3 and caspase-9 become active. Tenuifolin's ability to lower AChE activity, increase at the same time, increase the ability of the upper glands, and improve the ability to read and remember. Research on tenuifolin's potential for use in urinary disease (AD).
    Tenuifolin (Standard)
  • HY-N0495R
    Aloenin (Standard)
    Inhibitor
    Aloenin (Standard) is the analytical standard of Aloenin. This product is intended for research and analytical applications. Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
    Aloenin (Standard)
  • HY-164958
    TB-11
    Inhibitor
    TB-11 is a Cathepsin D inhibitor, with IC50s of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), 48.8 nM (BACE1), respectively. TB-11 can be used for tumor research.
    TB-11
  • HY-114245R
    Se-Methylselenocysteine (Standard)
    Inhibitor
    Risedronic acid (Standard) is the analytical standard of Risedronic acid. This product is intended for research and analytical applications. 0
    Se-Methylselenocysteine (Standard)
  • 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
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