Table 2.
Screening results for identified hits from the GSK library, n.i., no inhibition (less than 10% inhibition at 50 µM); n.d., not detectable (assay interference at higher concentrations than the given concentration). Chemical structures are given in figure 7b or electronic supplementary material, figure S7.
| inhibitors | IC50 (µM) or percentual inhibition |
||||||||
|---|---|---|---|---|---|---|---|---|---|
| Sirt1 |
Sirt2 |
Sirt3 |
|||||||
| ZMAL-assay | ZMAL-assay | FA-assay |
FP-assay | T-shift-assay | ZMAL-assay | FA-assay |
|||
| acetyl | myristoyl | acetyl | myristoyl | ||||||
| GSK237700A | n.i. | 4.3 ± 0.4 µM | 40.9 ± 19.5 µM | 16.2% at 50 µM | 23.3 ± 3.5 | 2.3°C | 35.2% at 50 µM | 39.4% at 50 µM | 43.2% at 50 µM |
| GSK300014A | n.i. | 44.5% at 50 µM IC50-value n.d. |
44.6% at 50 µM IC50-value n.d. |
24.5% at 50 µM | n.d. | 2.7°C | n.i. | n.i. | 42.4% at 50 µM |
| GW435821X | 26.5% at 50 µM | 24.6 ± 2.8 µM | 12.9 ± 2.8 µM | 58.8 ± 6.8 | 16.5 ± 3.5 | 2.8°C | 41.7 ± 2.0 | 15.9 ± 2.0 | 37.6% at 50 µM |
| GW654652X | n.i. | 1.1 ± 0.1 µM | 5.6 ± 0.6 µM | 21.9% at 50 µM | 1.6 ± 0.4 | 4.0°C | 19.6% at 50 µM | 12.8% at 50 µM | 32.4% at 50 µM |
| GW799251X | 15.5% at 50 µM | 1.6 ± 0.3 µM | 8.8 ± 2.2 µM | 10.5 ± 1.1 | 53.2% at 4 µM IC50-value n.d. |
0.7°C | n.i. | 16.7 ± 2.1 | 21.7 ± 4.3 |
| GW856804X | n.i. | 2.2 ± 0.2 µM | 2.8 ± 0.3 µM | 24.9% at 50 µM | 2.7 ± 0.8 | 4.6°C | n.i. | n.i. | 30.2% at 50 µM |