Table 1.
IC50 values for synthesized PROTACs.
| ID | Structure | HDAC1 IC50 (µM) or % inhib. at Given conc. |
HDAC6 IC50 (µM) or % inhib. at Given conc. |
HDAC8 IC50 (µM) |
|---|---|---|---|---|
| CRBN-based PROTACs | ||||
| CRBN_1a |
|
4.37 ± 0.65 | 0.22 ± 0.06 | 0.09 ± 0.03 |
| CRBN_1b |
|
>20 | 0.56 ± 0.1 | 0.81 ± 0.17 |
| CRBN_1c |
|
10 µM: 40.1% 1 µM: 22.2% |
0.25 ± 0.02 | 0.15 ± 0.01 |
| CRBN_1d |
|
13.1 ± 0.6 | 6.7 ± 0.6 | 0.37 ± 0.05 |
| CRBN_1e |
|
16.2 ± 0.8 | 17.2 ± 2.4 | 0.25 ± 0.07 |
| CRBN_1f |
|
10.8 ± 0.7 | 1.3 ± 0.3 | 0.25 ± 0.03 |
| CRBN_1g |
|
10 µM: 69% 1µM: 10.1% |
10 µM: 72.6% 1µM: 24.8% |
0.59 ± 0.11 |
| CRBN_1h |
|
3.91 ± 0.48 | 10 µM: 66.8% 1µM: 33.5% |
0.33 ± 0.19 |
| CRBN_1i |
|
10 µM: 67.4% 1µM: 20.7% |
10 µM: 92.3% 1µM: 85.4% |
0.65 ± 0.14 |
| CRBN_1j |
|
10 µM: 60.0% 1µM: 13.9% |
10 µM: 80.9% 1µM: 46.2% |
4.84 ± 1.05 |
| VHL-based PROTACs | ||||
| VHL_1k |
|
>20 | 0.31 ± 0.01 | 0.11 ± 0.01 |
| VHL_1l |
|
10 µM: 45.5% 1µM: 6.0% |
10 µM: 72.4% 1µM: 8.3% |
0.72 ± 0.15 |
| HyT-based PROTACs | ||||
| HyT_1m |
|
10 µM: 81.9% 1µM: 47.7% |
0.25 ± 0.08 | 0.57 ± 0.11 |
| HyT_1n |
|
10 µM: 30.0% 1 µM: 38.6% |
0.82 ± 0.05 | 0.39 ± 0.03 |
| HyT_1o |
|
10 µM: 52.6% 1 µM: 9.8% |
0.37 ± 0.03 | 0.09 ± 0.01 |
| HyT_1p |
|
10 µM: 40.0% 1µM: 2.3% |
10 µM: 72.8% 1µM: 12.4% |
0.75 ± 0.09 |