Beta-secretase

OM99-2, an eight-residue peptidomimetic, is a potent inhibitor of brain Memapsin 2 with a K i value of 9.58nM.

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.

antiepileptic drug

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.

BACE inhibitor

A BACE1 inhibitor

β-Secretase Inhibitor IV binds to the active site of BACE-1 and effectively blocks its proteolytic activity (IC₅₀=15nM).

Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.

BCA (Disodium bicinchoninate) is a colorimetric reagent for the detection of copper.

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.

An inhibitor of BACE1 and PI3K

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.

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.

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.

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

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.

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.

Glabrolide, derived from Glycyrrhiza uralensis Fisch.

(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat.

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.

Aloenin (Aloenin A) is a natural compound, which has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE).

Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor.

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.