Table 1.
Compound | Binding assay HDAC4-F + CD | Histone assay HDAC4-F* | Biomol assay HDAC4-F* | Biomol assay mHDAC4-F† | Biomol assay mHDAC4-CD† |
---|---|---|---|---|---|
MS-275 | − | 510 (±62) | 3,017 (±422) | NA up to 10,000 | NA up to 10,000 |
Apicidin | − | 2.4 (±0.5) | 1.2 (±0.3) | NA up to 10,000 | NA up to 10,000 |
Open Apicidin | − | 152 (±24) | 88 (±11) | NA up to10,000 | NA up to 10,000 |
LAQ824 | + | 4 (±1.3) | 1 (±0.5) | 3 (±0.8) | 2.5 (±0.7) |
IC50 values (nM) are the means of at least two independent experiments. NA, not active.
*[HDAC4-F] was 15 nM; in these assays endogenous class I HDAC activity is measured.
†[mHDAC4] was 1 nM.