| S1096 |
Quisinostat (JNJ-26481585) |
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. |
Pan |
HDAC10, IC50: 0.46 nM |
| S2759 |
CUDC-907 |
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. |
Pan |
HDAC10, IC50: 2.8 nM |
| S1090 |
PCI-24781 (Abexinostat) |
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. |
Pan |
HDAC10, IC50: 24 nM |
| S1194 |
CUDC-101 |
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. |
Pan |
HDAC10, IC50: 26.1 nM |
| S1515 |
Pracinostat (SB939) |
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. |
Pan |
HDAC10, IC50: 40 nM |
| S7278 |
HPOB |
HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
|
Pan |
HDAC10, IC50: 3.0 μM |
| S2012 |
PCI-34051 |
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. |
Pan |
HDAC10, IC50: 13 μM |