Table 1. In Vitro Potency of Compounds Used in This Study.
IC50 (nM) |
|||||||
---|---|---|---|---|---|---|---|
HDAC | 7 | 8 | 9 | 10 | 4 | 5 | 6 |
HDAC1 | >20,000a | >20,000 | NT | NT | >20,000 | 9166 | >20,000 |
HDAC2 | 17,410 ± 2814 | >20,000 | NT | NT | >20,000 | >20,000 | NT |
HDAC3 | >20,000 | >20,000 | NT | NT | >20,000 | NT | NT |
HDAC4 | >20,000 | >20,000 | NT | NT | >20,000 | >20,000 | >20,000 |
HDAC5 | >20,000 | >20,000 | NT | NT | >20,000 | NT | NT |
HDAC6 | 14.6 ± 8.0 | 2.06 ± 0.39 | 85 ± 2.8 | >100,000 | 2160 ± 392 | 10,800 ± 3259 | 14,450 ± 1131 |
HDAC7 | >20,000 | >20,000 | NT | NT | >20,000 | NT | NT |
HDAC8 | >20,000 | >20,000 | NT | NT | >20,000 | >20,000 | >20,000 |
HDAC9 | >20,000 | >20,000 | NT | NT | >20,000 | NT | NT |
HDAC10 | >20,000 | >20,000 | NT | NT | NT | NT | NT |
HDAC11 | >20,000 | >20,000 | NT | NT | >20,000 | NT | NT |
zHDAC6 (WT) | NT | NT | NT | NT | 3866 ± 1644 | NT | 41,736 ± 13,638 |
zHDAC6 (Y745F) | 311 ± 150 | 75 ± 26 | >20,000 | NT | >50,000 | >20,000 | >50,000 |
IC50 values were determined using purified human proteins as described in the Materials and Methods section. NT, not tested; zHDAC6, zebrafish HDAC6, catalytic DD2 domain.