HDAC

HDAC Inhibitors (39)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1047 Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • Nat Biotechnol, 2011, 29(3):255-65
  • Nature, 2011, 471(7337):235-9
S1053 Entinostat (MS-275) Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Phase 3.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • Nat Biotechnol, 2011, 29(3):255-65
  • Nat Immunol, 2014, 15(5):439-48
S1030 Panobinostat (LBH589) Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.
  • Nat Biotechnol, 2011, 29(3):255-65
  • Cell, 2014, 159(5):1110-25
  • Nat Med, 2015, 10.1038/nm.3855
S1045 Trichostatin A (TSA) Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • Cancer Cell, 2014, 26(4):534-48
  • EMBO J, 2014, 34(1):115-29
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Phase 2.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • Nat Struct Mol Biol, 2013, 20(3):317-25
  • Nat Commun, 2013, 4:2735
S1085 Belinostat (PXD101) Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.
  • Nat Biotechnol, 2011, 29(3):255-65
  • Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384
  • Cell Rep, 2013, 5(6):1679-89
S3020 Romidepsin (FK228, Depsipeptide) Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively.
  • Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384
  • Diabetes, 2014, 63(9):2924-34
  • PLoS Pathog, 2014, 10(8):e1004287
S1484 MC1568 MC1568 is a selective HDAC inhibitor for maize HD1-A with IC50 of 100 nM in a cell-free assay. It is 34-fold more selective for HD1-A than HD1-B.
  • Nat Commun, 2013, 4:2735
  • Proc Natl Acad Sci USA, 2012, 109(34):E2284-93
  • Oncogene, 2014, 33(5):653-64
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).
  • J Med Chem, 2015, 58(2):785-800
  • Int J Cancer, 2013, 134(11):2560-71
  • J Biol Chem, 2014, 289(14):9918-25
S2170 Givinostat (ITF2357) Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2.
  • PLoS Pathog, 2014, 10(4):e1004071
  • J Neurosci, 2013, 33(17):7535-47
  • J Antimicrob Chemother, 2014, 69(1):28-33
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1095 LAQ824 (Dacinostat) LAQ824 (Dacinostat) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.
  • Nat Biotechnol, 2011, 29(3):255-65
  • Diabetologia, 2012, 55(9):2421-31
  • Mol Pain, 2010, 6:51
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.
  • J Chem Inf Model, 2014, 54(3):881-93
  • ACS Med Chem Lett, 2013, 4(9):858-62
  • Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066
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.
  • J Clin Oncol, 2016, 10.1200/JCO.2016.66.5547
  • Nat Commun, 2013, 4:2735
  • J Biol Chem, 2014, 289(28):19519-30
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.
  • PLoS Pathog, 2014, 10(4):e1004071
  • Antimicrob Agents Chemother, 2012, 56(7):3849-56
  • Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066
S2012 PCI-34051 PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • BMC Biol, 2014, 12:95
  • J Mol Biol, 2014, 426(20):3442-53
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.
  • Nat Struct Mol Biol, 2013, 20(3):317-25
  • Int J Cancer, 2016, 138(1):125-36
  • Oncogenesis, 2014, 3:e127
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.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • Nat Biotechnol, 2011, 29(3):255-65
  • Diabetologia, 2012, 55(9):2421-31
S2244 AR-42 AR-42 is an HDAC inhibitor with IC50 of 30 nM. Phase 1.
  • Sci Transl Med, 2014, 6(256):256ra135
  • Leuk Res, 2014, 38(11):1320-6
  • Biochem Biophys Res Commun, 2015, 10.1016/j.bbrc.2015.05.078
S7229 RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
  • J Biol Chem, 2016, 291(14):7386-95
S8001 Rocilinostat (ACY-1215) Rocilinostat (ACY-1215) 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. Phase 2.
  • Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0481
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1168 Valproic acid sodium salt (Sodium valproate) Valproic acid sodium salt (Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • J Neurosci, 2013, 33(17):7535-47
  • Cell Death Dis, 2016, 7:e2221
S2818 CI994 (Tacedinaline) CI994 (Tacedinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • J Biomol Screen, 2011, 16(10):1247-53
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.
  • Am J Transl Res, 2014, 6(5):471-493
S2779 M344 M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.
  • Biochem Biophys Res Commun, 2014, 445(2):320-6
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.
  • Nat Biotechnol, 2015, 10.1038/nbt.3130
  • Leukemia, 2014, 28(3):680-9
  • PLoS Biol, 2013, 12(1):e1001758
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.
S7292 RG2833 (RGFP109) RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively.
S8043 Scriptaid Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.
  • J Antimicrob Chemother, 2014, 69(1):28-34
S4125 Sodium Phenylbutyrate Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders.
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).
  • Nat Commun, 2014, 5:3479
  • Oncogene, 2015, 10.1038/onc.2015.293
  • Cell Rep, 2013, 5(6):1679-89
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S7726 BRD73954 BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
S7473 Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
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.
S7617 Tasquinimod Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
S7596 CAY10603 CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
  • Med Oncol, 2016, 33(5):50
S7569 LMK-235 LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
S7278 HPOB HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
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.
S7689 BG45 BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively.
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All HDAC Products

Hover Mouse over '+' to display IC50

Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1047 Vorinostat (SAHA, MK0683) <1 mg/mL 53 mg/mL 3 mg/mL
S1053 Entinostat (MS-275) <1 mg/mL 75 mg/mL <1 mg/mL
S1030 Panobinostat (LBH589) <1 mg/mL 69 mg/mL <1 mg/mL
S1045 Trichostatin A (TSA) <1 mg/mL 23 mg/mL <1 mg/mL
S1122 Mocetinostat (MGCD0103) <1 mg/mL 13 mg/mL <1 mg/mL
S1085 Belinostat (PXD101) <1 mg/mL 64 mg/mL <1 mg/mL
S3020 Romidepsin (FK228, Depsipeptide) <1 mg/mL 10 mg/mL <1 mg/mL
S1484 MC1568 <1 mg/mL 13 mg/mL <1 mg/mL
S2627 Tubastatin A HCl <1 mg/mL 74 mg/mL <1 mg/mL
S2170 Givinostat (ITF2357) <1 mg/mL 95 mg/mL 3 mg/mL
S1095 LAQ824 (Dacinostat) <1 mg/mL 76 mg/mL <1 mg/mL
S1194 CUDC-101 <1 mg/mL 20 mg/mL <1 mg/mL
S1096 Quisinostat (JNJ-26481585) 2HCl <1 mg/mL 79 mg/mL <1 mg/mL
S1515 Pracinostat (SB939) <1 mg/mL 72 mg/mL 27 mg/mL
S2012 PCI-34051 <1 mg/mL 59 mg/mL <1 mg/mL
S1422 Droxinostat <1 mg/mL 49 mg/mL 49 mg/mL
S1090 PCI-24781 (Abexinostat) <1 mg/mL 80 mg/mL <1 mg/mL
S2244 AR-42 <1 mg/mL 63 mg/mL 63 mg/mL
S7229 RGFP966 <1 mg/mL 72 mg/mL <1 mg/mL
S8001 Rocilinostat (ACY-1215) <1 mg/mL 86 mg/mL <1 mg/mL
S1168 Valproic acid sodium salt (Sodium valproate) 33 mg/mL 33 mg/mL 33 mg/mL
S2818 CI994 (Tacedinaline) <1 mg/mL 54 mg/mL <1 mg/mL
S2759 CUDC-907 <1 mg/mL 102 mg/mL <1 mg/mL
S2779 M344 <1 mg/mL 62 mg/mL 4 mg/mL
S2239 Tubacin <1 mg/mL 100 mg/mL <1 mg/mL
S2693 Resminostat <1 mg/mL 70 mg/mL 70 mg/mL
S7292 RG2833 (RGFP109) <1 mg/mL 68 mg/mL 10 mg/mL
S8043 Scriptaid <1 mg/mL 65 mg/mL <1 mg/mL
S4125 Sodium Phenylbutyrate 30 mg/mL 8 mg/mL <1 mg/mL
S8049 Tubastatin A <1 mg/mL 9 mg/mL <1 mg/mL
S7726 BRD73954 <1 mg/mL 56 mg/mL 9 mg/mL
S7473 Nexturastat A <1 mg/mL 68 mg/mL 2 mg/mL
S7324 TMP269 <1 mg/mL 100 mg/mL 2 mg/mL
S7617 Tasquinimod <1 mg/mL 81 mg/mL 11 mg/mL
S7596 CAY10603 <1 mg/mL 89 mg/mL 5 mg/mL
S7569 LMK-235 <1 mg/mL 58 mg/mL 58 mg/mL
S7278 HPOB <1 mg/mL 62 mg/mL 38 mg/mL
S7555 4SC-202 <1 mg/mL 89 mg/mL <1 mg/mL
S7689 BG45 <1 mg/mL 42 mg/mL 2 mg/mL
Tags: HDAC inhibition | HDAC cancer | HDAC assay | histone deacetylase activity | HDAC inhibitors cancer | HDAC activity assay | HDAC activation | HDAC inhibitor mechanism | selective HDAC inhibitors | HDAC phosphorylation | HDAC inhibitor drugs | HDAC inhibitors in clinical trials | HDAC inhibitors list | HDAC inhibitor review
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