Table 1. Testing Various Selective HDAC Inhibitors as Activators of FXN Gene Transcription.
Target/Class | Compound Structure | Ki or IC50 | FXN transcription |
---|---|---|---|
HDAC1/2 |
Ki = 7 nM HDAC1 Ki = 2.5 μM HDAC3 |
Weakly active | |
HDAC3 |
Ki = 14 nM HDAC3 Ki = 148 nM HDAC1 |
Highly active | |
Class II | IC50 ∼ 1 μM class II HDACs | Inactive | |
Sirtuins | IC50 = 100 nM Sirt1 IC50 = 20 μM Sirt2 IC50 = 50 μM Sirt3 |
Inactive |