HDAC

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HDAC Inhibitors (33)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
S1047 Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM.
  • Nature, 2011, 471(7337):235-9
  • Nat Biotechnol, 2011, 29(3):255-65
  • Cell, 2014, 158(5):989-99
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.
  • Nat Biotechnol, 2011, 29(3):255-65
  • Nat Immunol, 2014, 15(5):439-48
  • Sci Transl Med, 2014, 6(256):256ra135
S1030 Panobinostat (LBH589) Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM. Phase 3.
  • Nat Biotechnol, 2011, 29(3):255-65
  • Nat Commun, 2013, 4:2735
  • Acta Neuropathol, 2011, 122(5):637-50
S1045 Trichostatin A (TSA) Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM – HDAC8 is the only known member of the HDAC-family that is not affected by TSA.
  • PLoS Biol, 2014, 12(1):e1001758
  • EMBO J, 2014, 10.15252/embj. 201489559
  • Proc Natl Acad Sci U S A, 2014, 111(3):E364-73
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.
  • Nat Struct Mol Biol, 2013, 20(3):317-25
  • Circ Res, 2012, 110(5):739-48
  • Nat Commun, 2013, 4:2735
S7617 Tasquinimod Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
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.
S7473 Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
S7292 RG2833 (RGFP109) RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
S1085 Belinostat (PXD101) Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM, 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, respectively.
  • Diabetes, 2014, 63(9):2924-34
  • Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384
  • PLoS Pathog, 2014, 10(8):e1004287
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.
S7229 RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC.
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
S8049 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
  • Nat Commun, 2014, 5:3479
  • Cell Rep, 2013, 5(6):1679-89
  • Int J Cancer, 2014, 134(11):2560-71
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.
  • Antimicrob Agents Chemother, 2012, 56(7):3849-56
  • J Thromb Thrombolysis, 2013, 35(2):185-92
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
  • Theriogenology, 2014, 81(4):572-8
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
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.
  • J Mol Biol, 2014, 10.1016/j.jmb.2014.03.007
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
S2627 Tubastatin A HCl Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
  • J Biol Chem, 2013, 288(20):14400-7
  • J Biol Chem, 2014, 289(14):9918-25
  • Int J Cancer, 2013, 134(11):2560-71
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, 2011, 29(3):255-65
  • Diabetologia, 2012, 55(9):2421-31
  • Pharm Res, 2013, 10.1007/s11095-013-1231-0
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
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, 10.1016/j.leukres.2014.08.014
S4125 Sodium Phenylbutyrate Sodium Phenylbutyrate is a transcriptional regulators that act by altering chromatin structure via the modulation of HDAC activity.
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.
S2239 Tubacin Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.
  • PLoS Biol, 2013, 12(1):e1001758
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.
  • Nat Commun, 2013, 4:2735
  • J Biol Chem, 2014, 289(28):19519-30
  • J Thromb Thrombolysis, 2013, 35(2):185-92
S1484 MC1568 MC1568 is a selective HDAC inhibitor for maize HD1-A with IC50 of 100 nM. It is 34-fold more selective for HD1-A than HD1-B.
  • Nat Commun, 2013, 4:2735
  • Proc Natl Acad Sci U S A, 2012, 109(34):E2284-93
  • Oncogene, 2014, 33(5):653-64
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. Phase 2.
  • PLoS Pathog, 2014, 10(4):e1004071
  • J Neurosci, 2013, 33(17):7535-47
  • J Antimicrob Chemother, 2014, 69(1):28-33
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
  • PLoS One, 2014, 9(8):e102684
S1168 Valproic acid sodium salt (Sodium valproate) Valproic acid is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • J Neurosci, 2013, 33(17):7535-47
S2818 CI994 (Tacedinaline) CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest. Phase 3.
  • J Biomol Screen, 2011, 16(10):1247-53
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