bace2

BACE2-IN-1, a potent BACE2 inhibitor characterized by its exceptional selectivity and a Ki value of 1.6 nM, is utilized in the investigation of Type 2 Diabetes.

AChE/BChE/BACE-1-IN-2 (Compound 4o) exhibits remarkable antioxidant potential and considerable binding capability towards PAS-AChE. AChE/BChE/BACE-1-IN-2 is an orally active AChE, BACE-1 and BChE inhibitor with IC 50 values of 0.069, 0.097 and 0.127 μM against hAChE, hBACE-1 and hBChE, respectively. AChE/BChE/BACE-1-IN-2 shows potential disassembly of Aβ aggregates and neuroprotective activity against Aβ-induced stress with excellent brain permeation [1].

BACE-1 Inhibitor 2 is a potent, CNS-permeable inhibitor of BACE-1, exhibiting an IC50 value of 1.5 nM in enzymatic assays [1].

AM-6494 is a potent and orally active BACE1 inhibitor (IC50: 0.4 nM) with in vivo selectivity over BACE2 (IC50: 18.6 nM).

BACE1-IN-1 is a high brain penetrant BACE1 inhibitor (IC50s: 32 and 47 nM for human BACE1 and BACE2).

Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.

AZD3839 free base is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

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.

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.

AMG-8718 is a selective, orally active and potent BACE1 inhibitor that acts on both BACE1 (IC50: 0.0007 μM) and BACE2 (IC50: 0.005 μM). AMG-8718 significantly reduces CSF and Aβ40 levels in the brain.

LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.

BACE1/2-IN-1 (compound 34) is an effective BACE1 and BACE2 inhibitor with IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 has lower Pgp efflux ratio and improved passive permeability. The metabolic stability of BACE1/2-IN-1 in liver microsomes is decreased.

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1(IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively).

BACE1-IN-4 is a potent and highly selective BACE1 inhibitor (IC50: 3.8 nM; Ki: 1.9 nM), more selective at BACE1 over BACE2.

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

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.