Lack of correlation between the level of HDAC inhibition (IC50 values) and the degree of γ promoter induction by HDAC inhibitors
Compound . | IC50, μM* . | Compound concentration, μM . | Change in γF/γF + βR luciferase ratio . |
|---|---|---|---|
| M344 | 0.11 | 5 | 5.91 |
| M360 | 0.26 | 5 | 2.31 |
| M355 | 0.10 | 20 | 0.83 |
| MD85 | 0.22 | 10 | 0.68 |
| SW68 | 0.26 | 25 | 5.41 |
| SW70 | 0.64 | 25 | 6.00 |
| SW99 | 0.80 | 50 | 2.85 |
| SW86 | 0.41 | 10 | 1.69 |
| SW183 | 0.53 | 4 | 0.56 |
| SW187 | 0.70 | 4 | 0.39 |
| SW188 | 0.41 | 4 | 1.08 |
| SW189 | 0.44 | 4 | 0.89 |
| M232 | 0.80 | 10 | 2.53 |
| HR13 | 0.06 | 2 | 2.60 |
| HR11 | 0.12 | 10 | 1.65 |
| HR10 | 0.72 | 10 | 1.00 |
| Propionate | < 10% @ 1 mM | — | — |
| Butyrate | < 10% @ 1 mM | — | — |
| Propionate-hydroxamate | 384 | — | — |
| Butyrate-hydroxamate | 47.2 | — | — |
Compound . | IC50, μM* . | Compound concentration, μM . | Change in γF/γF + βR luciferase ratio . |
|---|---|---|---|
| M344 | 0.11 | 5 | 5.91 |
| M360 | 0.26 | 5 | 2.31 |
| M355 | 0.10 | 20 | 0.83 |
| MD85 | 0.22 | 10 | 0.68 |
| SW68 | 0.26 | 25 | 5.41 |
| SW70 | 0.64 | 25 | 6.00 |
| SW99 | 0.80 | 50 | 2.85 |
| SW86 | 0.41 | 10 | 1.69 |
| SW183 | 0.53 | 4 | 0.56 |
| SW187 | 0.70 | 4 | 0.39 |
| SW188 | 0.41 | 4 | 1.08 |
| SW189 | 0.44 | 4 | 0.89 |
| M232 | 0.80 | 10 | 2.53 |
| HR13 | 0.06 | 2 | 2.60 |
| HR11 | 0.12 | 10 | 1.65 |
| HR10 | 0.72 | 10 | 1.00 |
| Propionate | < 10% @ 1 mM | — | — |
| Butyrate | < 10% @ 1 mM | — | — |
| Propionate-hydroxamate | 384 | — | — |
| Butyrate-hydroxamate | 47.2 | — | — |
Data from Wittich et al,10 Wittich,54 and Heltweg and Jung.12 — indicates not done.