| S7596 |
CAY10603 |
CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
|
Selective |
HDAC6, IC50: 2 pM |
| S8495 |
WT161 |
WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis. |
Selective |
HDAC6, IC50: 0.4 nM |
| S8648 |
ACY-738 |
ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs. |
Selective |
HDAC6, IC50: 1.7 nM |
| S9934 |
KA2507 |
KA2507, a potent, orally active and selective HDAC6 inhibitor with IC50 of 2.5 nM, shows antitumor activities and immune modulatory effects in preclinical models. |
Selective |
HDAC6, IC50: 2.5 nM |
| S8464 |
Citarinostat (ACY-241) |
Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3. |
Selective |
HDAC6, IC50: 2.6 nM |
| S2239 |
Tubacin |
Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis. |
Selective |
HDAC6, IC50: 4 nM |
| S8001 |
Ricolinostat (ACY-1215) |
Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. 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. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2. |
Selective |
HDAC6, IC50: 4.7 nM |
| S7473 |
Nexturastat A |
Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs. |
Selective |
HDAC6, IC50: 5 nM |
| S0864 |
ACY-775 |
ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5 nM. |
Selective |
HDAC6, IC50: 7.5 nM |
| S2627 |
Tubastatin A HCl |
Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). |
Selective |
HDAC6, IC50: 15 nM |
| S0709 |
Tubastatin A TFA |
Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
Selective |
HDAC6, IC50: 15 nM |
| S8049 |
Tubastatin A |
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
Selective |
HDAC6, IC50: 15 nM |
| S7278 |
HPOB |
HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
|
Selective |
HDAC6, IC50: 56 nM |
| S8743 |
SKLB-23bb |
SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.
|
Selective |
HDAC6, IC50: <100 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 |
HDAC6, IC50: 5.1 nM |
| S8769 |
Tinostamustine(EDO-S101) |
Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs). |
Pan |
HDAC6, IC50: 6 nM |
| S5810 |
UF010 |
UF010 is a class I HDAC-selective inhibitor with IC50 values of 0.5 nM, 0.1 nM, 0.06 nM, 1.5 nM, 9.1 nM and 15.3 nM for HDAC1, HDAC2, HDAC3, HDAC8, HDAC6 and HDAC10, respectively. |
Pan |
HDAC6, IC50: 9.1 nM |
| S1090 |
Abexinostat (PCI-24781) |
Abexinostat (PCI-24781, CRA-024781) 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 |
HDAC6, Ki: 17 nM |
| S2759 |
Fimepinostat (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. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
Pan |
HDAC6, IC50: 27 nM |
| S7726 |
BRD73954 |
BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
|
Pan |
HDAC6, IC50: 36 nM |
| S2693 |
Resminostat |
Resminostat (RAS2410) 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 |
HDAC6, IC50: 71.8 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 |
HDAC6, IC50: 1.008 μM |
| S1422 |
Droxinostat |
Droxinostat (NS 41080) 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 |
HDAC6, IC50: 2.47 μM |
| S2132 |
SR-4370 |
SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth. |
Pan |
HDAC6, IC50: 3.7 μM |
| S8773 |
TH34 |
TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM). |
Pan |
HDAC6, IC50: 4.6 μM |
| S9275 |
Isoguanosine |
Isoguanosine (Crotonoside) inhibits FLT3 and HDAC3/6 for the treatment of AML.Isoguanosine is a naturally occurring active isomer of guanosine that is found in the seeds of Croton tiglium. |
Pan |
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