Table 5. In Vitro Inhibition of HDACs Isoforms of Representative Compoundsa.
| cpd | IC50 of HDAC1 (nM) | IC50 of HDAC2 (nM) | IC50 of HDAC3 (nM) | IC50 of HDAC6 (nM) | HDAC2/ HDAC3 isoform selectivity | HDAC6/ HDAC3 isoform selectivity | HDAC2/ HDAC1 isoform selectivity | HDAC6/ HDAC1 isoform selectivity |
|---|---|---|---|---|---|---|---|---|
| 11e | 10.3 | 535.5 | 14.1 | 142.2 | 37.9 | 10.1 | 51.7 | 13.7 |
| 11p | 13.2 | 432.1 | 143.0 | 143.7 | 3.0 | 1.0 | 32.6 | 10.8 |
| 11r | 11.8 | 498.1 | 3.9 | 308.2 | 127.7 | 79.0 | 42.2 | 26.1 |
| 11w | 16.7 | 457.0 | 5.5 | 101.7 | 83.1 | 18.5 | 27.2 | 6.01 |
| 11y | 6.0 | 413.6 | 3.2 | 185.6 | 129.2 | 58 | 68.7 | 30.8 |
| 27c | 329.9 | 498.5 | 403.2 | 164.4 | 1.2 | 0.4 | 1.5 | 0.5 |
| 21c | 355.4 | 791.2 | 47.0 | 293.6 | 16.8 | 6.2 | 2.2 | 0.8 |
| SAHA | 34.6 | 184.7 | 90.1 | 63.0 | 2.0 | 0.7 | 5.3 | 1.8 |
a
Assays were performed in replicate (n ≥ 2); the SD values are <20% of the mean.