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BACE-1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Beta-secretase (64) Akt (1) Amyloid-β (9) Antibiotic (2) Apoptosis (3) Autophagy (3) Bacterial (2) Cathepsin (2) Cholinesterase (ChE) (17) DYRK (1) Endogenous Metabolite (1) GABA Receptor (1) GSK-3 (1) Microtubule/Tubulin (1) Monoamine Oxidase (1) NF-κB (2) PERK (2) Phosphatase (1) Phosphodiesterase (PDE) (1) PI3K (1) Potassium Channel (1) Reactive Oxygen Species (1) ROS Kinase (2) γ-secretase (1)
By Research Areas:	Cancer (9) Infection (2) Inflammation/Immunology (4) Metabolic Disease (3) Neurological Disease (70)
Click Chemistry:	Azide (1) Alkynes (1)

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Targets Recommended: Beta-secretase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100182

BACE1-IN-1	Beta-secretase	Neurological Disease
BACE1-IN-1 is a potent and highly brain penetrant *BACE1* inhibitor with IC₅₀s of 32 and 47 nM for human BACE1 and BACE2, respectively.

HY-131068

BACE-1 inhibitor 2	Beta-secretase	Neurological Disease
BACE-1 inhibitor 2 is a potent and CNS permeable *BACE-1* inhibitor with an IC₅₀ of 1.5 nM in BACE-1 enzymatic assay .

HY-112297

BACE-1 inhibitor 1	Beta-secretase	Neurological Disease
BACE-1 inhibitor 1 (Compound 8a) is a potent *BACE-1* inhibitor with an IC₅₀ of 56 nM .

HY-160037

SEW06622	Beta-secretase	Neurological Disease
SEW06622 is a *BACE-1* inhibitor with an IC₅₀ value of 6.3 μM and can be used in Alzheimer's disease research .

HY-P3426

BACE1-IN-10	Beta-secretase	Cancer
BACE1-IN-10 is a potent *BACE1* Inhibitor. BACE1-IN-10 shows sub-micromolar activity against recombinant BACE1 (rBACE1) .

HY-151348

BACE1-IN-11	Beta-secretase	Neurological Disease
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) .

HY-145345

BACE1-IN-6	Beta-secretase	Neurological Disease
BACE1-IN-6 is a *BACE1* inhibitor with an IC₅₀ value of 1.5 nM.

HY-161359

BACE1-IN-14	Beta-secretase	Neurological Disease
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 .

HY-147851

BACE1-IN-12	Beta-secretase	Neurological Disease
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 .

HY-128594

BACE1-IN-4	Beta-secretase	Neurological Disease
BACE1-IN-4 is a potent and highly selective *BACE1* inhibitor, with an IC₅₀ of 3.8 nM and a K_i of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer’s disease .

HY-119689

Umibecestat CNP520	Beta-secretase	Neurological Disease
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC₅₀s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively . Umibecestat can be used for the research of alzheimer's disease.

HY-153255

BACE1-IN-13	Beta-secretase	Neurological Disease
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 .

HY-112444

BACE1-IN-2	Beta-secretase	Neurological Disease
BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC₅₀ of 22 nM .

HY-10133

β-Secretase Inhibitor IV	Beta-secretase	Neurological Disease
β-Secretase Inhibitor IV is a potent, cell-active *BACE-1* inhibitor with IC₅₀s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.

HY-130244

BACE1-IN-5	Beta-secretase	Neurological Disease
BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC₅₀ of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .

HY-144739

BACE1-IN-8	Beta-secretase	Neurological Disease
BACE1-IN-8 (compound 70b) is a potent *BACE1* (β-site APP cleaving enzyme 1) inhibitor, with an IC₅₀ of 3.9 µM .

HY-144741

BACE1-IN-9	Beta-secretase	Neurological Disease
BACE1-IN-9 (compound 82b) is a potent *BACE1* (β-site APP cleaving enzyme 1) inhibitor, with an IC₅₀ of 1.2 µM .

HY-159151

AChE/Aβ-IN-6	Beta-secretase Amyloid-β	Neurological Disease
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 .

HY-147758

BACE1/2-IN-1	Beta-secretase Amyloid-β	Neurological Disease
BACE1/2-IN-1 (compound 34) is a potent *BACE1* and *BACE2* inhibitor, with an IC₅₀ of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability .

HY-N4186

Glabrolide	Beta-secretase	Neurological Disease
Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor[1].

HY-112157

PF-06751979 1 Publications Verification	Beta-secretase	Neurological Disease
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ of 7.3 nM in BACE1 binding assay.

HY-151260

AChE/BACE1/GSK3β-IN-1	Beta-secretase Cholinesterase (ChE) GSK-3	Neurological Disease
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of *AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1* and GSK3β with IC₅₀ values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD) .

HY-162933

AChE-IN-77	Cholinesterase (ChE)	Metabolic Disease
AChE-IN-77 (5d) is a potent AChE and *BACE1* inhibitor, with IC₅₀ values of 29.46 µM ans 2.85 µM for AChE and BACE1 in vitro metal chelating ability against Fe ³⁺ .

HY-139720

β-Secretase Inhibitor III	Beta-secretase	Neurological Disease
β-Secretase Inhibitor III is an extremely selective *BACE1* inhibitor (K_i = 0.13 nM).

HY-109055

Elenbecestat E2609	Beta-secretase	Neurological Disease
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant *BACE-1* inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research .

HY-12938

AMG-8718	Beta-secretase	Neurological Disease
AMG-8718 is a potent, selective and orally active *BACE1* inhibitor with IC₅₀ values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ₄₀ levels in the CSF and brain .

HY-132895

JNJ-67569762	Beta-secretase	Neurological Disease
JNJ-67569762 is a selective *BACE1* inhibitor targeting the S3 pocket (IC₅₀ = 2.7 nM).

HY-N1280

Semilicoisoflavone B	Amyloid-β	Neurological Disease
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation .

HY-N2215

Aloeresin D	Beta-secretase	Neurological Disease
Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC₅₀ of 39 μM .

HY-118098

LY3202626	Beta-secretase	Neurological Disease
LY3202626 is a CNS penetrant *BACE* inhibitor with IC₅₀s of 0.615 nM and 0.871 nM against BACE1 and BACE2, respectively .

HY-10472

LY2811376 Maximum Cited Publications 11 Publications Verification	Beta-secretase	Neurological Disease
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC₅₀ of 239 nM-249 nM, that acts to decrease Aβ secretion with EC₅₀ of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.

HY-100740

Lanabecestat AZD3293; LY3314814	Beta-secretase	Neurological Disease
Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating *BACE1* inhibitor with a K_i of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease .

HY-100740B

Lanabecestat camsylate LY3314814 camsylate; AZD3293 camsylate	Beta-secretase	Neurological Disease
Lanabecestat camsylate is a potent, orally active and blood-brain barrier penetrating *BACE1* inhibitor with a K_i of 0.4 nM. Lanabecestat camsylate is used for the research of Alzheimer's disease .

HY-13240

LY2886721 2 Publications Verification	Beta-secretase	Neurological Disease
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ of 20.3 nM for recombinant human *BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2* (IC₅₀ of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment .

HY-13240A

LY2886721 hydrochloride	Beta-secretase	Neurological Disease
LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ of 20.3 nM for recombinant human *BACE1. LY2886721 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2* (IC₅₀ of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment .

HY-116580

AZD-3289	Endogenous Metabolite	Neurological Disease
AZD-3289 is a potent BACE1 inhibitor with potential Alzheimer's disease inhibitory activity. The application of AZD-3289 is intended to slow the pathological progression of Alzheimer's disease by inhibiting the production of β-amyloid protein. The development of AZD-3289 responds to the need to reduce neurodegenerative changes associated with Alzheimer's disease. As a BACE1 inhibitor, AZD-3289 can effectively reduce the accumulation of β-amyloid peptide in the brain, which may improve cognitive function .

HY-124322

NB-360	Beta-secretase	Neurological Disease Inflammation/Immunology
NB-360 is a potent, brain penetrable, and orally bioavailable dual *BACE1/BACE2* inhibitor (IC₅₀: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .

HY-P1962

β-Secretase inhibitor [Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)	Beta-secretase	Neurological Disease
β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) is a β-secretase and *BACE1* inhibitor (IC₅₀: 25 nM for β-secretase) .

HY-147659

AChE/BChE/BACE-1-IN-2	Cholinesterase (ChE) Beta-secretase ROS Kinase	Neurological Disease
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 .

HY-147658

AChE/BChE/BACE-1-IN-1	Cholinesterase (ChE) Beta-secretase ROS Kinase	Neurological Disease
AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and *BACE-1* with IC₅₀ values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 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-1 has remarkable antioxidant potential .

HY-16759B

Verubecestat tosylate MK-8931 tosylate	Beta-secretase	Neurological Disease
Verubecestat tosylate is an orally active, high-affinity *BACE1* and *BACE2* inhibitor with K_i values of 2.2 nM and 0.38 nM. Verubecestat tosylate effectively reduces Aβ40 and has the potential for Alzheimer's Disease .

HY-122080

Memoquin	Cholinesterase (ChE) Beta-secretase Amyloid-β	Neurological Disease
Memoquin 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) .

HY-N1255

Scoulerine (-)-Scoulerine; Discretamine	Microtubule/Tubulin Beta-secretase Apoptosis	Cancer
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of *BACE1* (?-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .

HY-164956

TB-9	Cathepsin Beta-secretase	Cancer
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 .

HY-16759

Verubecestat 3 Publications Verification MK-8931	Beta-secretase	Neurological Disease
Verubecestat (MK-8931) is an orally active, high-affinity *BACE1* and *BACE2* inhibitor with K_i values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease .

HY-164958

TB-11	Cathepsin Beta-secretase	Cancer
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 .

HY-N2215R

Aloeresin D (Standard)	Beta-secretase	Neurological Disease
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 .

HY-N0231

Bavachalcone 2 Publications Verification Broussochalcone B	Bacterial Antibiotic NF-κB PERK Akt Autophagy Apoptosis	Infection Neurological Disease Inflammation/Immunology Cancer
Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro .

HY-108966

Kushenol C	Beta-secretase	Inflammation/Immunology
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC₅₀ of 5.45 µM .

HY-16759A

Verubecestat TFA MK-8931 TFA	Beta-secretase	Neurological Disease
Verubecestat (MK-8931) TFA is an orally active, high-affinity *BACE1* and *BACE2* inhibitor with K_i values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease .

Cat. No.	Product Name	Type

HY-15908

BCA 5 Publications Verification Disodium bicinchoninate	Biochemical Assay Reagents
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ value of 28 µM, a K_i value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .

Cat. No.	Product Name	Target	Research Area

HY-P3426

BACE1-IN-10	Beta-secretase	Cancer
BACE1-IN-10 is a potent *BACE1* Inhibitor. BACE1-IN-10 shows sub-micromolar activity against recombinant BACE1 (rBACE1) .

HY-P1962

β-Secretase inhibitor [Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)	Beta-secretase	Neurological Disease
β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) is a β-secretase and *BACE1* inhibitor (IC₅₀: 25 nM for β-secretase) .

HY-P2713

OM99-2	Beta-secretase	Neurological Disease
OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a K_i 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 .

HY-P2713A

OM99-2 TFA	Beta-secretase	Neurological Disease
OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a K_i 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 .

Cat. No.	Product Name		Classification

HY-159151

AChE/Aβ-IN-6		Azide
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 .

HY-128774

AM-6494		Alkynes
AM-6494 is a potent and orally active *BACE1* (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC₅₀=0.4 nM) with in vivo selectivity over BACE2 (IC₅₀=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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BACE-1 inhibitor

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