aβ/tau aggregation in 1

Tau/Aβ40 aggregation-IN-1 (Compound 20) functions as an inhibitor for tau and Aβ 40 aggregation, exhibiting IC50 values of 1.8 μM and 1.3 μM, respectively [1].

Aβ tau aggregation-IN-1 is a potent inhibitor of Aβ 1-42 β-sheet formation and tau aggregation, exhibiting K D values of 160 μM and 337 μM with Aβ 1-42 and tau, respectively. Additionally, Aβ tau aggregation-IN-1 efficiently penetrates the blood-brain barrier.

Tau Protein Aggregation-IN-1 (Compound 0c) serves as an inhibitor of Tau protein aggregation, applicable in research related to protein folding disorders including Alzheimer's disease, dementia, Parkinson's disease, Huntington's disease, and prion-based spongiform encephalopathies [1].

Tau-aggregation-IN-1 is a dopamine D2 and D3 receptor agonist and an inhibitor of tau441 protein aggregation (IC50: 21 μM).

Aβ tau aggregation-IN-3 is a potent inhibitor of amyloid protein aggregation, with an IC50 value of 0.85 µM in an Aβ-Thioflavin T (Aβ-ThT) functional aggregation assay, demonstrating anti-amyloid activity [1].

Tau-aggregation-IN-3 (compound 9), a Tau protein aggregation inhibitor (TAI), demonstrates effectiveness in cell-based aggregation inhibition experiments with an EC50 of 4.816 μM. It is applicable in Alzheimer's disease research [1].

Aβ1-42 aggregation inhibitor 1 effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values of 2.64 μM and 1.29 μM, respectively. At 25 μM, it also reduces self-mediated Aβ1-42 aggregation by 51.29%, showcasing its potential for Alzheimer's disease research [1].

Tau protein/α-synuclein-IN-1 is a dual inhibitor that not only impedes tau protein and α-synuclein but also reduces the development of α-syn inclusions in M17D neuroblastoma cells, making it a useful agent in the study of Alzheimer's disease [1].

Tau tracer 1 is a radiopharmaceutical agent designed specifically for visualizing Tau protein aggregates, commonly associated with neurodegenerative diseases. Its primary application lies in the diagnosis of these conditions.

Tau-aggregation and neuroinflammation-IN-1 is a potent inhibitor of tau protein aggregates, showing significant inhibitory activity against AcPHF6 and full-length tau protein aggregates. It has anti-inflammatory activity, reduces NO release, exhibits low cytotoxicity against LSP-stimulated BV2 cells, and reverses okadaic acid-induced memory impairment in rats.

BuChE-IN-5 (compound 25b) is a highly potent BuChE inhibitor with an IC50 value of 1.94 μM, effectively inhibiting Aβ and tau protein aggregation in Escherichia coli, and demonstrating significant free radical scavenging and antioxidant activity, making it a valuable tool for Alzheimer's disease research [1].

hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), showing IC50 values of 0.17 μM for both enzymes. It also potently inhibits glycogen synthase kinase 3 beta (GSK3β) with an IC50 of 0.21 μM. Furthermore, it effectively inhibits tau protein and Aβ1-42 peptide self-aggregation, and can bind the peripheral anionic site (PAS) to prevent amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) supports its potential in developing multitargeted anti-Alzheimer's agents [1].

hBChE-IN-1 (compound 4), a quinolizidinyl derivative, effectively inhibits human Butyrylcholinesterase (hBChE) with an IC50 value of 7 nM, demonstrating high selectivity against human Acetylcholinesterase (hAChE). It also inhibits tau and Aβ 40 protein aggregation, with IC50 values of 20 and 4.3 μM, respectively, making it valuable for Alzheimer's disease research [1].