Discovery and Characterization of a Potent and Selective Inhibitor of Aedes aegypti Inward Rectifier Potassium Channels
Figure 1
Tl+ flux assay of AeKir1 channel activity for high-throughput screening.
(A) Representative Tl+-induced changes in Thallos fluorescence in T-Rex-HEK293-AeKir1 cells cultured overnight with (+Tet) or without (-Tet) tetracycline. The shaded box indicates the cell exposure to Tl+. (B) DMSO concentrations up to 1.3% v/v DMSO have no effect on Tl+ flux through AeKir1. Data are means ±SEM (n = 3). One-way ANOVA P<0.0001, and asterisks (**, ***) indicate P<0.01 or P<0.001 respectively, when compared to 0% DMSO (Tukey's test). (C) Representative checkerboard analysis using 100 µM VU573 or 0.1% v/v DMSO as the vehicle control. The mean peak fluorescence amplitude of each sample population is indicated with a solid line and alternating samples for DMSO (top) and VU573 (bottom) are graphed as individual points. The mean ±SD Z′ calculated over 6 plates on 3 separate days was 0.69±0.05.