Table 1

Effects of FK228 and its derivatives on HDAC enzymes

HDAC-inhibitory activity was evaluated by using HDACs prepared from 293T cells, and the (IC50s) were determined as the means ± SD of the concentrations calculated from at least three independent dose-response curves. Each data point of the dose-response curves was the mean of duplicate assays. NT, not tested.

CompoundIC50 ± SD (nm)
Class IClass IIHDAC1 (C151S)
HDAC1HDAC2HDAC4HDAC6
FK22836 ± 1647 ± 18510 ± 34014,000 ± 3,100280 ± 75
FK228 + DTT1.0 ± 0.1NTNTNTNT
FK228 + H2O22,000 ± 370NTNTNTNT
redFK1.6 ± 0.93.9 ± 2.725 ± 7.3790 ± 11057 ± 12
redFK + DTT1.1 ± 0.7NTNTNTNT
Dimethyl FK2286,300 ± 1,9003,300 ± 1,00011,0000 ± 53,000>100,000>100,000
TSA19 ± 0.957 ± 2150 ± 1814 ± 4.312 ± 2.2