Figure 4. Novel TNK2 inhibitors.
(A) Structures of TNK2 inhibitors XMD8-87, XMD16-5 and AIM-100. (B) Selectivity of XMD8-87 and XMD16-5 were analyzed by KiNativ. Percent inhibitions were represented by bar height. Brown bar indicates >90% inhibition; red bar, 75%–90% inhibition; orange highlight, 50%–75% inhibition; and yellow bar, 35-50%. (C) ELISA of TNK2 inhibition by XMD8-87 and XMD16-5. Assay was performed as described in the methods with drug concentrations between 0 and 10 uM. (D) Inhibition of TNK2 phosphorylation was measured by western blot analysis. Cells were then treated with XMD8-87 or XMD16-5 at 5 μM and with 9 1:1 serial dilutions down to ≈10 nM. Two additional samples were treated with DMSO only. GAPDH is used as a loading control.