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. Author manuscript; available in PMC: 2017 Jan 1.
Published in final edited form as: Cancer Res. 2015 Dec 17;76(1):127–138. doi: 10.1158/0008-5472.CAN-15-0817

Figure 4. Novel TNK2 inhibitors.

Figure 4

(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.