Figure 9. Characterizing potential TLK2 inhibitors identified from a public kinase profiling data set.

(a) Nominating potential TLK2 inhibitors based on analysis of a public kinase profiling data set⁴¹. Two potential TLK2 inhibitors were selected based on relatively strong TLK2 inhibition (shown in bar chart) and low number of off-targets (shown in line chart). (b) The activity of the potential TLK2 kinase inhibitors Go6983 and GF109203X against TLK2 kinase were measured by in vitro kinase assay using recombinant active TLK2 protein. Myelin Basic Protein (MBP) was used as a substrate. (c) Clonogenic assays following Go6983 or GF109203X treatment of the MCF7 cells inducibly expressing TLK2. Go6983 (4 μM) or GF109203X and 0.2 or 1 μg ml⁻¹ of Dox were administered. Error bars represent the s.d. of two replicate measurements per condition. P values are calculated based on t-test. *P<0.05; ^**P<0.01.