| S7617 |
Tasquinimod |
Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
|
Selective |
|
| S1096 |
Quisinostat (JNJ-26481585) 2HCl |
Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, 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 |
HDAC4, IC50: 0.64 nM |
| S7569 |
LMK-235 |
LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
|
Pan |
HDAC4, IC50: 11.9 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 |
HDAC4, IC50: 13.2 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. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2. |
Pan |
HDAC4, IC50: 56 nM |
| S8502 |
TMP195 |
TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with Ki of 59, 60, 26 and 15nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
Pan |
HDAC4, Ki: 59 nM |
| S7324 |
TMP269 |
TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
Pan |
HDAC4, IC50: 157 nM |
