Table 1. HDAC panel assay.
The selectivity of T-3796106 and T-3793168 was analyzed based on HDAC enzyme inhibition. [a] The compound activity against 11 HDACs represented with the IC50 value. The IC50 values shown are the mean values of duplicate measurements; the numbers in parentheses represent each data. [b] No inhibition or compound activity that could not be fit to an IC50 curve.
| Target | Compounds IC50 (nM)a | ||
|---|---|---|---|
| T-3796106 | T-3793168 | Tubastatin A | |
| HDAC1 | 6200 (5820-6660) | b | >10000 |
| HDAC2 | >10000 | b | >10000 |
| HDAC3 | 4000 (3480-4470) | b | >10000 |
| HDAC8 | >1000 | 5600 (4170-7080) | >1000 |
| HDAC4 | 6200 (5970-6380) | >10000 | 6200 (6030-6330) |
| HDAC5 | 1700 (1610-1800) | 2300 (1550-3060) | 1900 (1580-2310) |
| HDAC7 | 1100 (1050-1130) | 5800 (4000-7660) | 590 (530-641) |
| HDAC9 | 2700 (2540-2840) | 5000 (4950-4960) | 1100 (913-1380) |
| HDAC6 | 12 (12.3-12.4) | 86 (67.4-104) | 15 (14.3-15.2) |
| HDAC10 | >10000 | b | >10000 |
| HDAC11 | >10000 | b | >10000 |