bace1in1

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

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.

hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE that can cross the blood-brain barrier. It effectively inhibits hAChE and hBACE-1, with IC50 values of 0.076 and 0.23 μM, respectively. Additionally, hAChE/hBACE-1-IN-1 prevents Aβ1-42 aggregation and enhances learning and memory in mice. This compound is useful in Alzheimer's disease research.

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.

AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor that targets acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), with IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM against hAChE, hBChE, and hBACE-1, respectively. It exhibits significant binding affinity with PAS-AChE, excellent blood-brain barrier permeability, potential disassembly of amyloid-beta (Aβ) aggregates, neuroprotective properties against Aβ-induced stress, and remarkable antioxidant capabilities [1].

BACE1-IN-12 is a potent BACE1 inhibitor (IC50: 8.9 μM) that can cross the blood-brain barrier. BACE1-IN-12 selectively inhibits BuChE (butylcholinesterase) activity (IC50: 3.2 μM). BACE1-IN-12 has potential for anti-Alzheimer's disease studies.

BACE1-IN-10 is a potent inhibitor of BACE1, demonstrating sub-micromolar activity against recombinant BACE1 (rBACE1) [1].

BACE1-IN-13 (Compound 36), an orally active inhibitor of BACE1, exhibits high potency with an IC50 of 2.9 nM and demonstrates greater efficacy in hAβ42 cells (IC50 = 1.3 nM). It is considered safe for the cardiovascular system and induces a sustained reduction of Aβ42 in both mouse and dog animal models [1].