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Beta-secretase

Beta-secretase (BACE) is an aspartic-acid protease important in the formation of myelin sheaths in peripheral nerve cells. The transmembrane protein contains two active site aspartate residues in its extracellular protein domain and may function as a dimer. Alzheimer's disease (AD) is caused by aggregates of the amyloid peptide (Abeta), which is generated by cleavage of the Abeta protein precursor (APP) by beta-secretase (BACE-1) followed by gamma-secretase. BACE-1 cleavage is limiting for the production of Abeta, Drugs to block this enzyme (BACE inhibitors) prevent the build up of beta-amyloid and may help slow or stop Alzheimers disease.

Targets for  Beta-secretase

Products for  Beta-secretase

  1. Cat.No. Product Name Information
  2. GC38489 (1α,1'S,4β)-Lanabecestat (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. (1α,1'S,4β)-Lanabecestat  Chemical Structure
  3. GC64554 Aloenin Aloenin (Aloenin A) is a natural compound, which has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE). Aloenin  Chemical Structure
  4. GC35299 Aloeresin D Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC50 of 39 μM. Aloeresin D  Chemical Structure
  5. GC14130 AZD3839 AZD3839 is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 can be used for the research of Alzheimer's disease. AZD3839  Chemical Structure
  6. GC31260 BACE-IN-1 BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. BACE-IN-1  Chemical Structure
  7. GC31158 BACE1-IN-1 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. BACE1-IN-1  Chemical Structure
  8. GC35455 BACE1-IN-4 BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. BACE1-IN-4  Chemical Structure
  9. GC64967 Elenbecestat Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat  Chemical Structure
  10. GN10716 Epiberberine Epiberberine  Chemical Structure
  11. GC35996 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, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride  Chemical Structure
  12. GC13809 Eslicarbazepine acetate antiepileptic drug Eslicarbazepine acetate  Chemical Structure
  13. GC36145 Glabrolide Glabrolide, derived from Glycyrrhiza uralensis Fisch. Glabrolide  Chemical Structure
  14. GC19217 Lanabecestat Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat  Chemical Structure
  15. GC30884 LX2343 An inhibitor of BACE1 and PI3K LX2343  Chemical Structure
  16. GC50672 LY 2886721 Hydrochloride LY 2886721 Hydrochloride  Chemical Structure
  17. GC17791 LY2811376 A BACE1 inhibitor LY2811376  Chemical Structure
  18. GC17227 LY2886721 BACE inhibitor LY2886721  Chemical Structure
  19. GC65970 NB-360 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. NB-360  Chemical Structure
  20. GC30876 PF-06751979 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. PF-06751979  Chemical Structure
  21. GC39798 Scoulerine 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. Scoulerine  Chemical Structure
  22. GC33067 Sophoflavescenol Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 ?M, 0.17 ?M, 17.89 ?g/mL, 10.98 ?M, 8.37 ?M and 8.21 ?M, respectively. Sophoflavescenol  Chemical Structure
  23. GC65361 Umibecestat 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  Chemical Structure
  24. GC11098 Verubecestat (MK-8931) Verubecestat (MK-8931) (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat (MK-8931)  Chemical Structure
  25. GC18464 β-Secretase Inhibitor IV

    β-Secretase inhibitor IV is an inhibitor of β-site amyloid protein cleaving enzymes (BACE/β-secretase) 1 and 2 (IC50s = 15 and 230 nM for human BACE1 and 2, respectively).

    β-Secretase Inhibitor IV  Chemical Structure

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