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. Author manuscript; available in PMC: 2013 Aug 9.
Published in final edited form as: J Med Chem. 2012 Jul 25;55(15):6832–6848. doi: 10.1021/jm300576q

Figure 8. Mebendazole binds directly to VEGFR2 kinase assay and also inhibits angiogenesis.

Figure 8

(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.