Table 6.
HDACs inhibitory activity and isoform selectivity for selected HDAC inhibitors.
Compd | IC50 of HDAC1 (μM)a | IC50 of HDAC2 (μM)a | IC50 of HDAC3 (μM)a | HDAC2/HDAC1 isoform selectivity | HDAC3/HDAC1 isoform selectivity |
---|---|---|---|---|---|
9d | 0.046 | 0.128 | 0.667 | 2.8 | 14.5 |
9h | 0.137 | 0.223 | 0.096 | 1.6 | 0.7 |
9m | 0.012 | 0.026 | 0.019 | 2.2 | 1.6 |
9n | 0.032 | 0.256 | 0.311 | 8.0 | 9.7 |
23a | 0.023 | 0.179 | 151.8 | 7.8 | 6600 |
MS-275 | 0.163 | 0.396 | 0.605 | 2.3 | 3.7 |
Assays were performed in replicate (n ≥ 2), the SD values are <20% of the mean.