Table 2. Dual Sirt2/HDAC6 Inhibitors Tested by Means of a Biochemical in Vitro Demyristoylation Assay.47a.
| compd | Sirt2 (demyristoylation) |
|---|---|
| 21 | nib |
| 22 | nib |
| 31 | 29 ± 1 |
| 32 | 1.7 ± 0.2 |
| 33 | 9.7 ± 1.3 |
| 44 | 34 ± 2 |
| 45 | 2.8 ± 0.6 |
| 46 | 13.2 ± 1.9 |
| 4 | 1.4 ± 0.3 |
| 5 | 2.5 ± 0.2c |
| 55 | nib |
| 56 | nib |
| 57 | <15% @ 5 μM |
| SAHA | 18% @ 10 μM |
IC50 values [μΜ, mean ± SD] or percentual inhibition at a given concentration of the dual Sirt2/HDAC6 inhibitors, as well as reference compounds for selective Sirt2 inhibition (4,5), HDAC6 inhibition (55–57), and SAHA as an nonselective inhibitor of Zn2+-dependent HDACs.
ni = no inhibition (inhibition <15% @ 20 μM).
Values for 5 taken from Vogelmann et al.47