Table 1.
Inhibitor | HDAC Isoform | Selectivity |
---|---|---|
Class I-selective inhibitors | ||
Trapoxin A and derivatives | HDAC1 | 640–570 000-fold vs. HDAC6 |
Apicidin | HDAC2–3 | 5–83-fold vs. HDAC1, 4–9 |
Romidepsin | HDAC1–2 | 10-fold vs. HDAC4 |
Azumamide E | HDAC1–3 | 37–500-fold vs. HDAC4–9 |
2 | HDAC1–3 | 10-fold vs. HDAC6 |
65-fold vs. HDAC4,5,7 | ||
3 | HDAC3,6 | 4–135-fold vs. |
HDAC1,2,4,5,7,8 | ||
4 | HDAC1,4 | 3–8-fold vs. HDAC6 |
MS-275 | HDAC1,3 | 135-fold vs. HDAC6,8 |
CI-994 | HDAC1,3 | 133-fold vs. HDAC6,8 |
MGCD0103 | HDAC1,3 | 40-fold vs. HDAC6,8 |
13–15 | HDAC1,2 | 100-fold vs. HDAC3,8 |
SK-7041 | HDAC1,2 | HDAC3–6 |
SK-7068 | HDAC1,2 | HDAC3–6 |
VPA | HDAC1–5,7 | >20-fold vs. HDAC6, 10 |
Isoform-selective inhibitors within class I | ||
1 | HDAC1 | 4-fold vs. HDAC8 |
5 | HDAC1 | 10-fold vs. HDAC2 |
20-fold vs. HDAC3 | ||
6 | HDAC1 | 4-fold vs. HDAC2 |
13-fold vs. HDAC3 | ||
12 | HDAC1 | 5–32-fold vs. HDAC2 |
>145-fold vs. HDAC3,8 | ||
16–23 | HDAC1 | 6–19-fold vs. HDAC2 |
SB-429201 | HDAC1 | 20-fold vs. HDAC3,8 |
27 | HDAC1 | 370-fold vs. HDAC4 |
10-fold vs. HDAC2,3 | ||
25 | HDAC8 | 140-fold vs. HDAC1 |
115-fold vs. HDAC6 | ||
26 | HDAC8 | 330-fold vs. HDAC1 |
180-fold vs. HDAC6 | ||
PCI-34051 | HDAC8 | >290-fold vs. |
HDAC1–3,6,10 | ||
SB-379278A | HDAC8 | 60-fold vs. HDAC1,3 |
Class II-selective inhibitors | ||
10 | HD1-A | 78-fold vs. HD1-B |
11 | HD1-A | 176-fold vs. HD1-B |
Tubacin | HDAC6 | 4-fold vs. HDAC1 |
9 | HDAC6 | 14-fold vs. HDAC1 |
28 | HDAC4 | 3-fold vs. HDAC1,2,3 |
Isoform-selective inhibitors within class II | ||
8d | HDAC6 | 46-fold vs. HDAC1 |
51-fold vs. HDAC4 | ||
24 | HDAC4 | 4-fold vs. HDAC1 |
15-fold vs. HDAC6 |