Table 2.
IC50 values for SIRT2 using different substrates and SIRT2 inhibitors. The structures of all substrates are shown in Figure S12, and the structures of the inhibitors used are shown in Figure S13. Mcm1_T denotes a buffer containing 0.1% Tween20 (w/v) instead of BSA. SD values denote the standard deviations of at least two independent replicates.
| cmp | IC50 Value ± SD in µM or Inhibition in % at a Given Concentration | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| [S] | K (µM) |
[E] (nM) | NAM | S2iL5 | cmp12 | SMyr | KK-22 | SirReal2 | AGK2 |
| F4 (1 µM) | 0.033 | 10 | 100 ± 5 | 0.34 ± 0.02 | 0.32 ± 0.04 | 0.015 ± 0.001 | 16 ± 1.2 | 0% @20 µM |
0% @20 µM |
| F4 (40 nM) | 0.033 | 1 | 211 ± 7 | 0.034 ± 0.004 | 0.015 ± 0.002 | 0.00078 ± 0.00005 | 1.5 ± 1 | 25 ± 2% @20 µM |
42 ± 4% @20 µM |
| S2 (1 µM) | 0.0053 | 10 | 340 ± 7 | 1.3 ± 0.3 | 0.93 ± 0.2 | 0.028 ± 0.005 | 30 ± 2 | 18 ± 2% @20 µM |
0% @20 µM |
| S2 (10 nM) | 0.0053 | 0.5 | 600 ± 70 | 0.028 ± 0.015 | 0.019 ± 0.006 | 0.00058 ± 0.00013 | 2.1 ± 0.1 | 1.1 ± 0.1 | 32 ± 2% @20 µM |
| Mcm1 (1 µM) | 0.017 | 10 | 43 ± 6 | 2.4 ± 0.5 | 1.7 ± 0.2 | 0.093 ± 0.002 | 7 ± 3% @20 µM |
0% @20 µM |
0% @20 µM |
| Mcm1_T (1 µM) | 0.017 | 10 | 45 ± 3 | 1.9 ± 0.1 | 14 ± 3 | 0.058 ± 0.025 | 0% @20 µM |
0% @20 µM |
0 % @20 µM |
| S1 (1 µM) | 0.15 | 10 | 120 ± 10 | 0.56 ± 0.02 | 0.41 ± 0.04 | 0.0099 ± 0.003 | 12 ± 0.5 | 5.5 ± 0.8 | 33 ± 5 % @20 µM |
| C1 (20 µM) | - | 100 | 12 ± 1 | 0.21 ± 0.01 | 0.048 ± 0.005 | 0.056 ± 0.011 | 0.41 ± 0.03 | 0.089 ± 0.009 | 12 ± 1 |
| C2 (1 µM) | - | 100 | 42 ± 6 | 0.42 ± 0.02 | 0.24 ± 0.03 | 0.33 ± 0.01 | 24 ± 1% | 22 ± 3% @20 µM |
6 ± 6% @ 6 µM |