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Beta-Secretase

Beta-secretase is a protein family that includes in humans Beta-secretase 1 and Beta-secretase 2. Beta-secretase 1, also known as beta-site amyloid precursor protein cleaving enzyme 1, beta-site APP cleaving enzyme 1 (BACE1), membrane-associated aspartic protease 2, memapsin-2, aspartyl protease 2, and ASP2, is an enzyme that in humans is encoded by the BACE1 gene. Expression of BACE1 is observed mainly in neurons. BACE1 is an aspartic acid protease important in the formation of myelin sheaths in peripheral nerve cells: in mice the expression of BACE1 is high in the postnatal stages, when myelination occurs. The transmembrane protein contains two active site aspartate residues in its extracellular protein domain and may function as a dimer, its cytoplasmic tail is required for the correct maturation and an efficient intracellular trafficking, but doesn't affect the activity. It is produced as a pro-enzyme, the endoproteolitc removal occurs after BACE leaves Endoplasmic reticulum, in the Golgi apparatus. In addition the pro-peptide receives additional sugars to increase the molecular mass. and the tail became a palmitoylated. Beta-secretase 2 (also known as Memapsin-1) is an enzyme that cleaves Glu-Val-Asn-Leu!Asp-Ala-Glu-Phe in the Swedish variant of Alzheimer's amyloid precursor protein. BACE2 is a close homolog of BACE1.
Cat No. product name
T6772 AZD3839 free base AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
TN2217 Sophoflavescenol Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , the...
T7011 Verubecestat Verubecestat (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.
T2639 LY2811376 LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity...
T3769 Tenuifolin Tenuifolin has no inherent toxicity to either the transfected or wild type cells at the effective concentrations, it inhibits amyloid-β secretion in vitro.
T8179 Aloeresin D Aloeresin D, a natural chromone glycoside, inhibits β-Secretase (BACE1) activity (IC50: 39 μM).
T11175 Elenbecestat Elenbecestat is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.
T2S1181 Aloenin 1. Aloenin and aloe-emodin are active principles for inhibition of c-ADH and c-ALDH activities in vitro.
T5S2361 Epiberberine 1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/...
T8306 Epiberberine chloride Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor (IC50s: 1.07...
T6058 LY2886721 LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.
T4398 LX2343 LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343...
T3161 BACE-IN-1 BACE-IN-1 is amyloid precursor protein beta-secretase inhibitor
T3285 Eslicarbazepine Acetate Eslicarbazepine acetate (ESL) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset...
AZD3839 free base
T6772
AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
Sophoflavescenol
TN2217
Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , the...
Verubecestat
T7011
Verubecestat (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.
LY2811376
T2639
LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivi...
Tenuifolin
T3769
Tenuifolin has no inherent toxicity to either the transfected or wild type cells at the effective concentrations, it inhibits amyloid-β secretion in vitro.
Aloeresin D
T8179
Aloeresin D, a natural chromone glycoside, inhibits β-Secretase (BACE1) activity (IC50: 39 μM).
Elenbecestat
T11175
Elenbecestat is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.
Aloenin
T2S1181
1. Aloenin and aloe-emodin are active principles for inhibition of c-ADH and c-ALDH activities in vitro.
Epiberberine
T5S2361
1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/...
Epiberberine chloride
T8306
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor (IC50s: 1.07...
LY2886721
T6058
LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.
LX2343
T4398
LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX...
BACE-IN-1
T3161
BACE-IN-1 is amyloid precursor protein beta-secretase inhibitor
Eslicarbazepine Acetate
T3285
Eslicarbazepine acetate (ESL) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset...