Table 1.
Selectivity of HDAC6is determined in vitro using purified human HDACs.
| Inhibitor | IC50 [nM] | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| HDAC6 GAK |
HDAC6 Literature * | HDAC1 GAK |
HDAC1 RHKK |
HDAC1 Literature * |
SI (HD6/HD1) | SI (HD6/HD1) | HDAC10 | SI (HD6/HD10) | |
| GAK | RHKK | ||||||||
| Next A | 3.8 | 5.02 | 362 | 4959 | 3020 | 95.3 | 1305 | 11 | 2.9 |
| ACY-775 | 1.11 | 7.5 | 1194 | 21,700 | 2123 | 1076 | 19,550 | 34 | 30.6 |
| ACY-1215 | 2.37 | 4.7 | 106 | 625 | 58 | 44.7 | 263.6 | 18.2 | 7.7 |
| TSA | 0.41 | 8.6 | 0.71 | 8.13 | 6 | 1.73 | 19.84 | 4.3 | 10.5 |
| Tub A | 4.65 | 15 | 2288 | 24,680 | 16,400 | 492 | 5308 | 3.8 | 0.82 |
| Tubacin | 35.9 | 4 | 102 | 15,070 | 1400 | 2.84 | 420 | 678 | 18.9 |
| 6 | 0.35 | NA | 49.2 | 281 | NA | 141 | 803 | 68.3 | 195 |
| 7 | 2.06 | NA | >50,000 | >50,000 | NA | >25,000 | >25,000 | >50,000 | >25,000 |
IC50 values were determined using purified human proteins, as described in the Materials and Methods section. Substantial variability exists between the IC50 values determined in this study and those reported in the literature that likely results from differences in reaction conditions used, including two different substrates for HDAC1. Selectivity indices (SI) were calculated as the ratio of IC50 values for HDAC1/10 divided by IC50s for HDAC6. * data were taken from references [10,24,37,38,39].