bace-2

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1, with IC50 values of 15.6 nM and 16.3 nM at BACE-1 concentrations of 2 nM and 100 pM, respectively.

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

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

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.

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

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

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.

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

BACE1-IN-14 (compound 27f) is a BACE1 inhibitor with an EC50 value of 0.7 μM, and it exhibits an EC50 value of 1.6 μM against BACE2. BACE1-IN-14 is applicable in Alzheimer's disease (AD) research.

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.

Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy.

BACE1-IN-2 is a BACE1 inhibitor (IC50: 22 nM).

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. It inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50 values of 0.072, 9.81, 14.52, 0.024, and 2.42 μM, respectively. Additionally, AChE-IN-82 inhibits COX-1, COX-2, and 5-LOX with IC50 values of 60.41, 0.187, and 0.18 μM, respectively. The compound also demonstrates strong neuroprotective effects by significantly reducing H2O2-induced oxidative stress.

BACE1-IN-15 (Compound 72) is a selective β-secretase 1 (BACE-1) inhibitor with oral bioavailability and blood-brain barrier permeability, exhibiting an IC50 value of 121.65 nM, and an IC50 of 480.92 nM for BACE-2. BACE1-IN-15 is applicable for research in the field of Alzheimer's disease.

BACE-1/Mpro-IN-1 is a compound capable of penetrating the blood-brain barrier, acting as a dual inhibitor for BACE-1 (IC50 = 0.26 μM) and SARS-CoV-2 Mpro (IC50 = 0.91 μM). It functions as a mixed inhibitor by binding to aspartic and cysteine proteases and demonstrates optimal docking scores alongside robust interaction characteristics. BACE-1/Mpro-IN-1 is applicable in research focusing on COVID-19-related neuroinflammation and Alzheimer’s disease.

AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active AChE, BACE-1, and BChE inhibitor with IC50 values of 0.069, 0.097, and 0.127 μM against hAChE, hBACE-1, and hBChE, respectively. It exhibits remarkable antioxidant potential, considerable binding capability towards PAS-AChE, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress with excellent brain permeation [1].

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki values of 3.5 nM and 1.2 nM, respectively. It acts as a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 shares these properties, being a complete agonist of CB1 and a competitive inverse agonist of CB2.

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].