FIGURE 10

FIGURE 10

IC₅₀-determination of G2-2 and G2-3 with GST-humCK1δ^TV1, His-DrCK1δA and His-DrCK1δB. The IWP-derived inhibitors G2-2 and G2-3 were further assessed and IC₅₀-values were determined. The transfer of radioactively labelled γ-phosphate to the substrate α-casein was measured by Cherenkov counting. The inhibitors were applied in different concentrations ranging from 13 to 26667 nM. The standardized kinase- and ATP-concentration as well as reaction time can be found in Supplementary Table S5. The kinase activity of the inhibitor-treated samples was normalized to the DMSO-controls. The results are shown as the mean value ± standard deviation. The experiments were conducted in technical triplicates. (A) IC₅₀-determination of G2-2 with GST-humCK1δ^TV1. (B) IC₅₀-determination of G2-2 with His-DrCK1δA. (C) IC₅₀-determination of G2-2 with His-DrCK1δB. IC₅₀: 50% inhibitory concentration. (D) IC₅₀-determination of G2-3 with GST-humCK1δ^TV1. (E) IC₅₀-determination of G2-3 with His-DrCK1δA. (F) IC₅₀-determination of G2-3 with His-DrCK1δB. IC₅₀: 50% inhibitory concentration.