Vorinostat (SAHA): Selectivity & Specificity
Vorinostat (SAHA) is a potent inhibitor of HDAC1 (0.08 µg/mL, 89 nM), HDAC6 (0.09 µg/mL, 98 nM), HDAC2 (10.16 ± 2.75 nM, 91 nM), HDAC3 (0.024 ± 0.006 µM, 77 nM), HDAC4 (25 ± 13 µM), HDACs (from SiHa cell nuclear extracts) (0.18 µM), Total HDAC (from K562 nuclear extracts) (23 nM), HDAC8 (1155 nM, 0.42 ± 0.08 µM), HDAC10 (122 nM), HDAC11 (41 nM), HeLa nuclear extracts (0.048 ± 0.035 µmol/L), HDACs (HeLa cell extract) (0.630 ± 0.011 µM), Pan-HDAC (HeLa cell nuclear extracts) (20 nM), HDAC7 (>5000 nM), HDAC9 (>5000 nM), cdHDAC4 wt (40 ± 2 µM), Class I and II HDACs (< 86 nM), HDAC1 and HDAC2 (from HeLa cell nucleus extracts) (10.0±1.0 nM), Recombinant HDAC1 (45.97 ±5.62 nM), Recombinant HDAC2 (96.90 ±8.43 nM), Recombinant HDAC3 (33.87 ±2.38 nM), Recombinant HDAC8 (542.83 ±32.73 nM), Recombinant HDAC4 (>10^4 nM), Recombinant HDAC6 (15.50 ±1.38 nM). Vorinostat (SAHA) exhibits the greatest inhibitory potency toward HDAC1 and HDAC2 (from HeLa cell nucleus extracts) (IC50 = 10.0±1.0 nM).