Figure 8. Mebendazole binds directly to VEGFR2 kinase assay and also inhibits angiogenesis.
(A) Mebendazole binds directly to VEGFR2 and affects VEGFR2 kinase activity with an IC50 value of 3.6 μM. IC50 curves were generated using GraphPad 5 and a standard 4-parameter non-linear regression model (log [inhibitor] vs response – variable slope). Data points correspond to the averages of duplicate wells, and error bars represent the mean ± replicate % activity. The graphical representation shows dashed lines at the IC50 values, where the vertical line is at (log x) = −5.4437. Solving the equation (log x) = −5.4437 results in the IC50 value of 3.6 μM. (B) Control: Staurosporine binds to VEGFR2 and affects kinase activity with a IC50 value of 8 nM. (C). Mebendazole, predicted to act as a VEGFR2 inhibitor by TMFS, inhibits angiogenesis in a HUVEC cell based assay. Mebendazole significantly inhibited network formation with an IC50 value of 8.8 μM, which is implicated by the lack of cellular migration, alignment and branching.