Research Paper Volume 3, Issue 9 pp 852—872
Structure-based development of novel sirtuin inhibitors
Figure 2. Effects of docking hits on the in vitro activity of Sirt2, 3, 5 and 6. (a) Shown is the relative activity compared to a control containing DMSO, which was used as solvent for all compounds. Green bars show Sirt2 activity, red Sirt3, yellow Sirt5, and blue Sirt6. CSC5 and 40 were not compatible with the assay used. (b) Concentration-dependent inhibition of Sirt2 activity by compound 3. (c) Concentration-dependent inhibition of Sirt2 activity by compound 4. (d) Effects of 100 mM compound 3 or 4, respectively, on the in vitro activity of Sirt1. Inhibition of Sirt1 by 2 mM nicotinamide is shown as a control.