| S7229 |
RGFP966 |
RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC. |
Selective |
HDAC3, IC50: 80 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 |
HDAC3, IC50: 1.8 nM |
| 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 |
HDAC3, IC50: 4.86 nM |
| S7292 |
RG2833 (RGFP109) |
RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. |
Pan |
HDAC3, Ki: 5 nM; HDAC3, IC50: 50 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 |
HDAC3/SMRT, Ki: 8.2 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 |
HDAC3, IC50: 9.1 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 |
HDAC3, IC50: 43 nM |
| S2693 |
Resminostat |
Resminostat dose-dependently and selectively inhibits HDAC1/3/6 with IC50 of 42.5 nM/50.1 nM/71.8 nM, less potent to HDAC8 with IC50 of 877 nM. |
Pan |
HDAC3, IC50: 50.1 nM |
| S8001 |
Rocilinostat (ACY-1215) |
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. |
Pan |
HDAC3, IC50: 51 nM |
| S7555 |
4SC-202 |
4SC-202 is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
|
Pan |
HDAC3, IC50: 0.57 μM |
| S1122 |
Mocetinostat (MGCD0103) |
Mocetinostat (MGCD0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Phase 2. |
Pan |
HDAC3, IC50: 1.66 μM |
| S7278 |
HPOB |
HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
|
Pan |
HDAC3, IC50: 1.7 μM |
| S1053 |
Entinostat (MS-275) |
Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10. Phase 3. |
Pan |
HDAC3, IC50: 1.7 μM |
| S1422 |
Droxinostat |
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. |
Pan |
HDAC3, IC50: 16.9 μM |
