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
- Cat.No. Product Name Information
- GC38489 (1α,1'S,4β)-Lanabecestat (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat.
- GC64554 Aloenin Aloenin (Aloenin A) is a natural compound, which has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE).
- GC35299 Aloeresin D Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC50 of 39 μM.
- 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.
- 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.
- 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.
- 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.
- GC64967 Elenbecestat Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor.
- GN10716 Epiberberine
- 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.
- GC13809 Eslicarbazepine acetate antiepileptic drug
- GC36145 Glabrolide Glabrolide, derived from Glycyrrhiza uralensis Fisch.
- 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.
- GC30884 LX2343 An inhibitor of BACE1 and PI3K
- GC50672 LY 2886721 Hydrochloride
- GC17791 LY2811376 A BACE1 inhibitor
- GC17227 LY2886721 BACE inhibitor
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
-
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).