||Selective / Pan
||IC50 / Ki
||PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10.
||HDAC8, IC50: 10 nM
||Quisinostat (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.
||HDAC8, IC50: 4.26 nM
||CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
||HDAC8, IC50: 79.8 nM
||Rocilinostat (ACY-1215) is a selective HDAC6 inhibitor with IC50 of 5 nM. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Phase 2.
||HDAC8, IC50: 100 nM
||Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.
||HDAC8, IC50: 140 nM
||CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. Phase 1.
||HDAC8, IC50: 191 nM
||PCI-24781 (Abexinostat) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.
||HDAC8, IC50: 280 nM
||Tubastatin A HCl
||Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
||HDAC8, IC50: 854 nM
||Droxinostat is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.
||HDAC8, IC50: 1.46 μM
||HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
||HDAC8, IC50: 2.8 μM