Table 2. Activity of MPT0E028 and SAHA against HDACs.
Compound | HDAC1 | HDAC2 | HDAC8 | HDAC4 | HDAC6 |
Class I | Class IIa | Class IIb | |||
IC50 (nM±SE) | |||||
MPT0E028 | 53.0±12.0 | 106.2±23.0 | 2532.6±314.7 | >10000 | 29.5±6.4 |
SAHA | 102.2±22.1 | 336.2±91.2 | 2898.9±128.7 | >10000 | 19.5±3.1 |
HDAC activity was determined indirectly by measuring the fluorescence generated by a deacetylated fluorogenic peptide product (Materials and Methods). Data represent triplicate determinations from three independent experiments (mean±SE). HDAC Class I isoforms: HDAC1, HDAC2, and HDAC8, HDAC Class II isoforms: HDAC4 and HDAC6.