Table 4.
Selectivity over histone deacetylases and deubiquitinases compared to pan-DUB inhibitor PR-619.
Compound | % inhibition @ 100 μM | Qualitative pan-DUB inhibition | ||
---|---|---|---|---|
HDAC1 | HDAC6 | @ 10 μM | @ 50 μM | |
S1th 10 | n.i.* | 29% | n.i. | n.i. |
S1th 11 | n.i. | n.i. | n.i. | n.i. |
S1th 12 | n.i. | 36% | n.i. | n.i. |
S1th 13 | n.i. | 19% | n.i. | n.i. |
PR-619 | 54% | 49% | + | +++ |
n.i., no inhibition (<10%), + low inhibition, +++ full inhibition.