Table 1.
HDAC6 inhibitors and selectivity over HDAC 1, 2, and 3. The half maximal inhibitory concentration (IC50) is indicated for each HDAC6 inhibitor. The selectivity over HDAC 1, 2, and 3 is indicated for each drug. The selectivity index is the ratio of each HDAC IC50 vs. HDAC6 IC50.
| HDAC6i | IC50 HDAC6 | HDAC1/6 | HDAC2/6 | HDAC3/6 |
|---|---|---|---|---|
| ACY-738 | 1.7 nM | 55-fold | 75-fold | 128-fold |
| ACY-1215 | 4.7 nM | 12-fold | 10-fold | 11-fold |
| Tubacin | 4.0 nM | 350-fold | >1000-fold | 318-fold |
| Tubastatin A | 4.4 nM | >1000-fold | >1000-fold | >1000-fold |
| SW-100 | 2.3 nM | >1000-fold | >1000-fold | >1000-fold |
| ACY-775 | 7.5 nM | 283-fold | 347-fold | >1000-fold |
| ACY-1083 | 3.0 nM | >260-fold | >260-fold | >260-fold |
| MPTOG211 | 0.29 nM | >1000-fold | >1000-fold | >1000-fold |
| W-2 | 21 nM | 153-fold | 60-fold | 63-fold |
| 5-Aroylindole 6 | 3.92 nM | 559-fold | 145-fold | >1000-fold |