Skip to main content
. 2019 Sep 6;10(10):1430–1435. doi: 10.1021/acsmedchemlett.9b00213

Figure 3.

Figure 3

PD-173955 analogues reduce Aβ production potently by affecting BACE1 cleavage of APP and do not inhibit Abl and Src kinases. (A) Compound 3a, 3m, 5b, 5c, and 5f reduced production of Aβ40 and Aβ42 peptides from N2a695 cells. Aβ40 and Aβ42 levels in cell supernatants post treatment with compounds were measured using human Aβ ELISA kits. (B) Compounds 3m, 5b, 5c and 5f did not inhibit or weakly inhibited Abl and Src kinase activity at 10 μM compound concentration (kinase activity assays were performed by Luceome Biotechnologies, Tucson, Arizona). Compound 3a is known to not inhibit Abl and Src kinase (ref (5)). (C, D) Effects of 3a analogues on Aβ production in N2a cells transfected with human (C) APP-FL or (D) APP-C99, measured by ELISA. DAPT is used as a positive control, and MK8931 is used as positive control in (C) and a negative control in (D). All experiments were performed in duplicate, and results shown here are the representative of two independent experiments. Statistical significance: *P < 0.05%; **P < 0.01%.