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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.

Epiberberine
T5S23616873-09-2
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 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.
  • $31
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Se-Methylselenocysteine
T772726046-90-2
Se-Methylselenocysteine (Se-MSC) is a potent chemopreventive agent in many test systems and has been shown to inhibit tumor promotion and induce apoptosis.
  • $33
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NB-360
T121881262857-73-7
NB-360 is a potent and brain-penetrable inhibitor of BACE1 and BACE2 with IC50s of 5, 5, and 6 nM for mouse and human BACE1 and BACE2. NB-360 exhibits excellent selectivity over the related aspartyl proteases pepsin, cathepsin E, and cathepsin D.
  • $112
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Umibecestat
T132531387560-01-1
Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), 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.
  • $175
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Atabecestat
T143381200493-78-2In house
Atabecestat (JNJ-54861911) is a potent, brain-penetrant, and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor that achieves robust and high CSF Aβ reduction, is well-tolerated, and displays sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment[1].
  • $132
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Eslicarbazepine
T3285L104746-04-5
Eslicarbazepine (Stedesa) can be used for adjunctive therapy for adults with partial-onset seizures.
  • $40
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Scoulerine
TN21906451-73-6
Scoulerine is an inhibitor of ß-site amyloid precursor protein cleaving enzyme 1(BACE1). Scoulerine a potent antimitotic compound that inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
  • $44
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Epiberberine chloride
T8306889665-86-5
Epiberberine chloride, a natural pro-berberine from Coptis chinensis Franch. is an AChE, BChE, and BACE1 inhibitor with IC50 values of 1.07, 6.03, and 8.55 μM, respectively.Epiberberine chloride has antioxidant effects and inhibits the effects of Ca9-22 and Fa2R. Epiberberine chloride has antioxidant effects, inhibits the motility of Ca9-22 and FaDu cell lines, and can be used to study hyperlipidemia, Alzheimer's disease and diabetes.
  • $32
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Verubecestat
T70111286770-55-5
Verubecestat (MK-8931) (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.
  • $34
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Aloeresin D
T8179105317-67-7
Aloeresin D, a natural chromone glycoside, inhibits β-Secretase (BACE1) activity (IC50: 39 μM).
  • $56
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Elenbecestat
T111751388651-30-6
Elenbecestat (E2609) is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.
  • $64
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Aloenin
T2S118138412-46-3
1. Aloenin (Aloenin A) and aloe-emodin are active principles for inhibition of c-ADH and c-ALDH activities in vitro.
  • $38
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LY2886721
T60581262036-50-9
LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.
  • $43
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SEW06622
T83616261349-28-4
SEW06622 is a potent inhibitor of acetylcholinesterase (AChE) and beta-secretase-1 (BACE-1) and is a potential candidate for the treatment of Alzheimer's disease.
  • $195
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Cassiaside
TN147213709-03-0
Cassiaside is a naphthyl ketone glycoside that inhibits BACE1 (IC50= 4.45 μM; Ki=9.85 μM).Cassiaside exhibits significant hepatoprotective effects against galactosamine injury and has potential anti-Alzheimer's disease (AD) activity.
  • $84
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Tenuifolin
T376920183-47-5
Tenuifolin has no inherent toxicity to either the transfected or wild type cells at the effective concentrations, it inhibits amyloid-β secretion in vitro.
  • $41
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AZD3839 free base
T67721227163-84-9
AZD3839 free base is a potent and selective BACE1 inhibitor with a Ki of 26.1 nM, demonstrating approximately 14-fold selectivity over BACE2. [Phase 1]
  • $83
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Lanabecestat
TQ02381383982-64-6
Lanabecestat (AZD3293) is a highly potent and highly permeable, orally active BACE1 inhibitor (Ki: 0.4 nM) that crosses the blood-brain barrier, Lanabecestat can be used for the study of neurological diseases like Alzheimer's disease.
  • $149
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Eslicarbazepine Acetate
T3285236395-14-5
Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy.
  • $32
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LX2343
T4398333745-53-2
LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM and acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. Additionally, LX2343 stimulates autophagy, promoting Aβ clearance.
  • $31
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LY2811376
T26391194044-20-6
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 towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.
  • $48
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Sophoflavescenol
TN2217216450-65-6
Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflaves
  • $657
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β-Secretase inhibitor-STA
T3161350228-37-4
BACE-IN-1 is amyloid precursor protein beta-secretase inhibitor
  • $152
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BCA
T14514979-88-4
BCA is 2,2-Biquinoline-4,4-dicarboxylic acid disodium salt.
  • $42
7-10 days
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TargetMol | Citations Cited