Signaling Pathway



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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) in theory would prevent the build up of beta-amyloid and may help slow or stop Alzheimers disease.

Beta-secretase Inhibitors & Modulators (7)

Product Name Catalog No. Brief Description
AZD3839 free base


AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.

Epiberberine chloride


Epiberberine (chloride), a natural alkaloid, is a BACE1 inhibitor, which also exhibits inhibition activity on CYP2D6 and aldose reductase, alpha-adrenoceptors, acetylcholinesterase (AChE), butyrylcholinesterase, and b-site amyloid precursor protein cleaving enzyme 1.

Eslicarbazepine acetate


Eslicarbazepine acetate (BIA 2-093) is an antiepileptic drug.



LY2811376 is a BACE1 inhibitor with marked Ab-lowering effects in animal models.



LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease.



Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 13 nM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 μM, 0.17 μM, 17.89 μg/mL, 10.98 μM, 8.37 μM and 8.21 μM, respectively.



MK-8931 is a BACE1 inhibitor.