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

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-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
    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-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-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-d<sub>4</sub>
  • 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
  • HY-100740B
    Lanabecestat camsylate
    Inhibitor
    Lanabecestat 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-18112
    AZ-4217
    Inhibitor
    AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research.
    AZ-4217
  • HY-16759B
    Verubecestat tosylate
    Inhibitor
    Verubecestat tosylate is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat tosylate effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
    Verubecestat tosylate
Cat. No. Product Name / Synonyms Application Reactivity

BACE1

BACE2

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Beta-secretase Inhibitors
Product NameBACE1BACE2Purity    
Se-Methylselenocysteine
BACE1
 99.60%
Verubecestat
BACE1
BACE2
99.56%
LY2886721
BACE1
 99.74%
BCA
BACE1, IC50: 28 μM
BACE1, Ki: 43 μM
 99.76%
Epiberberine chloride
BACE1
 99.02%
TB-9
BACE1, IC50: 54.2 nM
 
LY2811376
BACE1
 99.89%
Lanabecestat
BACE1
 99.67%
BACE2-IN-1
BACE1, Ki: 815.1 nM
BACE2, Ki: 1.6 nM
99.4%
Elenbecestat
BACE1
 99.82%
Atabecestat
BACE1
 99.77%
Scoulerine
BACE1
 99.27%
AZD3839 free base
BACE1
 99.91%
BACE1-IN-1
BACE1
 99.02%
PF-06751979
BACE1
 99.23%
(1α,1'S,4β)-Lanabecestat
BACE1
 
LX2343
BACE1, IC50: 11.43 μM
 99.80%
Epiberberine
BACE1
 98.46%
Aloeresin D
BACE1
 99.51%
Sophoflavescenol
BACE1
 98.78%
BACE1-IN-5
BACE1
 
BACE1-IN-2
BACE1
 
BACE1-IN-4
BACE1
 
AM-6494
BACE1
 
AMG-8718
BACE1, IC50: 0.0007 μM
BACE2, IC50: 0.005 μM
BACE1/2-IN-1
BACE1
BACE2
AChE/BACE1/GSK3β-IN-1
BACE1, IC50: 20 μM
 
BACE1-IN-10
BACE1
 
AChE/BChE-IN-12
BACE1, IC50: 10.65 ± 0. μM
 
Memoquin
BACE1, IC50: 108 nM
 
BACE1-IN-14
BACE1, EC50: 0.7 μM
BACE2, EC50: 1.6 μM
BACE1-IN-11
BACE1, IC50: 72 μM
 
β-Secretase Inhibitor III
BACE1
 
OM99-2
BACE1
 
AChE-IN-82
BACE1, IC50: 2.42 μM
 
BACE1-IN-9
BACE1
 
TB-11
BACE1, IC50: 48.8 nM