Table 2.
IC50 values for benzhydroxamate-based HADC inhibitors underlying PROTAC development.
| ID | Inhibitor Structure | HDAC1 IC50 (µM) |
HDAC6 IC50 (µM) |
HDAC8 IC50 (µM) |
|---|---|---|---|---|
| 2a |
|
33.6 ± 1.8 | 3.0 ± 0.3 | 0.58 ± 0.05 |
| 2b |
|
2.3 ± 1.2 | 2.5 ± 1.1 | 0.09 ± 0.02 |
| 2c |
|
11.6 ± 3.9 | 0.12 ± 0.02 | 0.12 ± 0.04 |
| 2d |
|
2.3 ± 1.2 | 2.5 ± 1.1 | 0.14 ± 0.01 |
| 2e |
|
21.8 ± 2.1 | 5.1 ± 0.3 | 0.26 ± 0.04 |
| 2f |
|
14.5 ± 1.4 | 5.1 ± 0.8 | 0.07 ± 0.02 |
| 2g |
|
10.4 ± 1.2 | 4.0 ± 0.2 | 0.25 ± 0.04 |
| 2h |
|
>20 | 0.15 ± 0.001 | 0.01 ± 0.001 |
| 2i |
|
>20 | 7.4 ± 0.6 | 0.41 ± 0.05 |