Biological Activity
Aβ/tau aggregation-IN-1 is a potent Aβ1-42 β-sheets formation and tau aggregation inhibitor. The KD values of Aβ/tau aggregation-IN-1 with Aβ1-42 and tau are 160 μM and 337 μM, respectively. Aβ/tau aggregation-IN-1 can permeate the blood-brain barrier[1].
Aβ/tau aggregation-IN-1 (1 μM; 24 hours; HEK-293 T cells) significantly declines the tau aggregation foci[1].Aβ/tau aggregation-IN-1 with N-methylation of the quinolone ring effectively inhibits Aβ1-42 aggregation by 84.7%-99.5% and tau aggregation by 71.2%-101.8%. Aβ/tau aggregation-IN-1 inhibits self-induced Aβ1-42 aggregation by inhibiting the formation of β-sheets. Aβ/tau aggregation-IN-1 shows certain binding abilities with Aβ1-42 and tau. The KD value of Aβ/tau aggregation-IN-1 with Aβ1-42 is 160 μM. The KD value of Aβ/tau aggregation-IN-1 with tau is 337 μM. Aβ/tau aggregation-IN-1 interacts with Aβ1-42 and tau through noncovalent interactions[1].
References
[1]. Lv P, et al. Synthesis and evaluation of 1,2,3,4-tetrahydro-1-acridone analogues as potential dual inhibitors for amyloid-beta and tau aggregation. Bioorg Med Chem. 2018;26(16):4693-4705.
