Figure 4
From: Alterations to the broad-spectrum formin inhibitor SMIFH2 modulate potency but not specificity
Structure activity data for SMIFH2 and 17 analogs tested against five human formins. Each individual data point indicates an IC50 value from a titration of inhibitor in the pyrene-actin assembly assay. The average and standard deviation for each formin/analog pair is reported in Table 1. Conditions: 2 µM actin (5% pyrene-labeled), 4 µM S. pombe profilin, formin (5 nM DIAPH1-FFC, 5 nM DIAPH2-FFC, 5 nM INF2-FFC, 20–37.5 nM FMN2-FFC, 20 nM FMNL3-FFC), inhibitor with a fixed volume of DMSO. Due to low solubility, compound 9 was dissolved in DMF. Because we cannot reliably measure IC50 values above 40 µM, those points are indicated at the > 40 µM line. Individual IC50 values are listed in Table S1.
