aβ-in-10

Aβ-IN-10 (Compound Alz-5) is a bifunctional copper chelator and an inhibitor of beta-amyloid (Aβ), interacting with Aβ aggregates to reduce their neurotoxicity. This compound also displays antioxidative properties and exhibits moderate cytotoxicity in SH-SY5Y and HepG2 cells in the presence of CuCl2, with IC50 values of 65.5 and 31.2 μM, respectively. Additionally, Aβ-IN-10 reduces the increase in cell rigidity caused by Aβ.

BuChE-IN-TM-10 (TM-10) is a potent inhibitor of butyrylcholinesterase (BuChE) with an IC50 of 8.9 nM. It effectively inhibits and disaggregates self-induced Aβ aggregation, exhibits significant antioxidant activity, and demonstrates substantial penetration through the blood-brain barrier (BBB), holding promise as a potential treatment for Alzheimer's disease.

hAChE-IN-8 (Compound S-12) is an orally active and selective inhibitor of hAChE, with an IC50 of 0.486 μM. It also inhibits BACE-1 with an IC50 of 0.542 μM, but shows negligible inhibition of Dyrk1A (IC50>10 μM). This compound reduces Aβ aggregation, exhibits good blood-brain barrier penetration, and is primarily used in Alzheimer's disease research.

GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC50= 0.90 μM) that demonstrates good blood-brain barrier permeability (Pe= 10.7 x 10^-6 cm/s). It effectively reduces tau protein phosphorylation in the BR5706 strain and decreases Aβ aggregate deposition in the CL2006 strain, indicating its potential as a candidate for Alzheimer's disease (AD) research.

MAO-B-IN-10 (compound 4f) is a highly potent and selective MAO-B (monoamine oxidase-B) inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 of 5.3 μM. It demonstrates the ability to inhibit self-mediated Aβ (amyloid β) aggregation by 58.2% and disaggregate it by 43.3%, holding promise for Alzheimer's disease research [1].

AChE/BChE-IN-10 is a potent dual inhibitor of AChE and BChE with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 exhibits good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation.

AChE-IN-63 (Compound 5AD) serves as a selective inhibitor of hAChE, exhibiting an IC 50 value of 0.103 μM. Moreover, it inhibits hBChE and hBACE-1 with IC 50 values of 10 μM and 1.342 μM, respectively. AChE-IN-63 is effective in inhibiting Aβ aggregation and preventing the formation and deposition of Aβ1-42. It can effectively penetrate the blood-brain barrier and is orally bioavailable. This compound is primarily utilized in research related to Alzheimer's disease [1].

β-Amyloid (10-35), amide, is a chemical compound comprising 26 amino acids, specifically residues 10-35 of the Aβ peptide, and serves as the primary constituent of amyloid plaques in Alzheimer's disease.