Table 1. Effects of Compounds 1, 4, and 8–12 on GSK-3β, HDAC1, and HDAC6 Activity.
| compd | n | GSK-3β IC50 (μM)a | HDAC1 IC50 (μM)a | HDAC6 IC50 (μM)a |
|---|---|---|---|---|
| 1 | n.a.b | 0.6 (0.31–3.22)c,d | 5.6 (5.31–7.45)c,d | |
| 4 | 0.05 ± 0.01 | n.d.e | n.d.e | |
| 8 | 1 | 19.96 ± 1.76 | 3.75 ± 0.58 | 18.13 ± 0.17 |
| 9 | 2 | 9.85 ± 1.00 | 2.24 ± 1.17 | 12.58 ± 0.96 |
| 10 | 3 | 4.11 ± 0.01 | 5.02 ± 1.2 | 14.71 ± 0.19 |
| 11 | 4 | 2.69 ± 0.01 | 12.78 ± 0.11 | 3.19 ± 0.08 |
| 12 | 20.22 ± 0.40 | n.a.f | n.a.f |
a
IC50 values are defined as the drug concentration that reduces by 50% the target activity and are reported as a mean value of three or more determinations.
b
n.a.: not active up to 50 μM.
c
Data from ref (25).
d
95% confidence interval.
e
Not determined.
f
Not active up to 30 μM.