HDAC

HDAC Products

  • All (82)
  • HDAC Inhibitors (81)
  • HDAC Activator (1)
  • New HDAC Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1047 Vorinostat (SAHA) Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Cell Rep, 2024, 43(1):113575
NPJ Precis Oncol, 2024, 8(1):52
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-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. Entinostat induces autophagy and apoptosis. Phase 3.
Nat Commun, 2024, 15(1):4739
Nat Commun, 2024, 15(1):8044
J Clin Invest, 2024, 134(6)e171063
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Nat Commun, 2024, 15(1):5209
Nat Commun, 2024, 15(1):4450
Emerg Microbes Infect, 2024, 13(1):2327371
S1045 TSA (Trichostatin A) TSA (Trichostatin A) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Nat Commun, 2024, 15(1):1190
Nat Commun, 2024, 15(1):5209
Nat Commun, 2024, 15(1):9463
S3020 Romidepsin Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.
Nat Commun, 2024, 15(1):2989
Nucleic Acids Res, 2024, 52(1):141-153
Cell Rep, 2024, 43(2):113778
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) 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. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Dev Cell, 2024, S1534-5807(24)00326-5
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Clin Epigenetics, 2024, 16(1):13
S7229 RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Sci Immunol, 2024, 9(99):eadk7387
Nat Commun, 2024, 15(1):8044
Acta Pharm Sin B, 2024, 14(2):712-728
S1085 Belinostat Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
Nat Commun, 2024, 15(1):4739
J Immunother Cancer, 2024, 12(10)e009590
Cell Rep, 2024, 43(1):113575
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.
Theranostics, 2024, 14(6):2345-2366
Biomedicines, 2024, 12(6)1203
Life Sci Alliance, 2024, 7(7)e202302384
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.
Cancer Immunol Immunother, 2024, 73(1):7
Cancer Immunol Immunother, 2024, 73(1):7
Cancer Res Commun, 2024, 4(2):349-364
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.
iScience, 2024, 27(4):109366
iScience, 2024, 27(9):110775
Int J Mol Sci, 2024, 25(3):1411.
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.
iScience, 2024, 27(9):110775
Front Med (Lausanne), 2022, 9:848938
Hepatology, 2021, 10.1002/hep.32245
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).
Nat Metab, 2022, 4(1):44-59
Cancer Lett, 2022, 549:215911
Elife, 2022, 11e67368
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. PCI-34051 induces caspase-dependent apoptosis.
J Cell Mol Med, 2024, 28(18):e70114
The University of Auckland, 2023,
Reprod Med Biol, 2023, 22(1):e12527
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Cancer Cell Int, 2024, 24(1):303
Front Pharmacol, 2024, 15:1418902
PLoS Negl Trop Dis, 2024, 18(8):e0012428
S2818 Tacedinaline (CI994) Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) 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.
Adv Sci (Weinh), 2024, 11(24):e2308945
Biomedicines, 2024, 12(6)1203
J Transl Med, 2023, 21(1):604
S7569 LMK-235 LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
Dev Cell, 2024, S1534-5807(24)00326-5
Environ Pollut, 2024, 355:124194
Shock, 2023, 60(1):75-83
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.
Viruses, 2024, 16(5)775
JCI Insight, 2023, 8(7)e162907
Cell Biosci, 2022, 12(1):135
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.
Dev Cell, 2024, S1534-5807(24)00326-5
Br J Cancer, 2023, 10.1038/s41416-023-02195-0
Int J Mol Sci, 2023, 24(5)4720
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.
J Leukoc Biol, 2024, qiae006
Sci Transl Med, 2022, 14(657):eabg3277
J Exp Clin Cancer Res, 2022, 41(1):325
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
J Exp Clin Cancer Res, 2024, 43(1):152
J Immunother Cancer, 2024, 12(11)e009805
Sci Total Environ, 2022, 838(Pt 2):155825
S3944 VPA (Valproic acid) VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
Nat Commun, 2024, 15(1):668
Dev Cell, 2024, S1534-5807(24)00326-5
S2244 AR-42 AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1.
Nat Commun, 2024, 15(1):4739
EBioMedicine, 2024, 105:105211
Int J Mol Sci, 2024, 25(14)7866
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.
Biomedicines, 2024, 12(6)1203
Cell Syst, 2023, 14(6):482-500.e8
Elife, 2022, 11e73718
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
Nat Commun, 2024, 15(1):4764
Nat Commun, 2024, 15(1):5209
Cell Rep, 2024, 43(2):113778
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.
EBioMedicine, 2024, 105:105211
Nat Commun, 2023, 14(1):5051
Nat Commun, 2023, 14(1):5051
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.
Nat Commun, 2023, 14(1):2095
Nat Commun, 2023, 14(1):2095
J Transl Med, 2023, 21(1):604
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.
Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
Cancers (Basel), 2024, 16(21)3606
Nat Commun, 2022, 13(1):2666
S7595 Santacruzamate A (CAY10683) Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.
J Exp Clin Cancer Res, 2024, 43(1):152
Cell Death Dis, 2024, 15(8):593
Nat Commun, 2023, 14(1):5051
S2341 (-)-Parthenolide (-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.
Genes Environ, 2024, 46(1):10
Transl Oncol, 2023, 35:101712
PLoS Genet, 2021, 17(11):e1009890
S1095 Dacinostat (LAQ824) Dacinostat (LAQ824, NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.
Int J Mol Sci, 2023, 24(17)13660
Clin Transl Med, 2022, 12(5):e798
Cancers (Basel), 2022, 14(19)4708
S7596 CAY10603 CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
EBioMedicine, 2024, 105:105211
iScience, 2024, 27(9):110775
Respir Res, 2024, 25(1):66
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.
Cell Stress Chaperones, 2024, 29(3):359-380
Cancer Res Commun, 2024, 4(2):349-364
Cell Death Dis, 2023, 14(2):142
S7617 Tasquinimod Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
Signal Transduct Target Ther, 2023, 8(1):11
Nat Commun, 2022, 13(1):1481
Int J Biol Sci, 2022, 18(15):5724-5739
S4125 4-PBA (Sodium Phenylbutyrate) 4-PBA (Sodium Phenylbutyrate) is a salt of 4-phenylbutyrate (4-PBA) or 4-phenylbutyric acid.Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders.
J Clin Invest, 2024, e175310
Aging Cell, 2023, 22(6):e13840
Inflammopharmacology, 2023, 31(3):1319-1327
S8567 Tucidinostat (Chidamide) Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
Cell Death Dis, 2024, 15(1):95
Clin Immunol, 2024, 260:109915
Mol Cancer Ther, 2024, 23(4):520-531
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.
Dev Cell, 2024, S1534-5807(24)00326-5
Nat Commun, 2023, 14(1):2095
Nat Commun, 2023, 14(1):2095
S7473 Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
Biomedicines, 2024, 12(6)1203
Cancer Res Commun, 2024, 4(2):349-364
Int J Mol Sci, 2023, 24(5)4720
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.
PLoS One, 2024, 19(6):e0304914
Exp Ther Med, 2021, 21(5):515
Cancer Sci, 2020, 111(7):2374-2384
S7555 Domatinostat (4SC-202) Domatinostat (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.
Nat Commun, 2023, 14(1):5051
Nat Commun, 2023, 14(1):5051
Cell Rep Med, 2023, 4(7):101101
S8043 Scriptaid Scriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.
Cell Res, 2022, 10.1038/s41422-022-00668-0
J Appl Physiol (1985), 2020, 128(2):276-285
Nat Biotechnol, 2019, 10.1038/s41587-019-0372-z
S3592 4-PBA (4-Phenylbutyric acid) 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
Int J Biol Sci, 2024, 20(4):1279-1296
Phytomedicine, 2024, 135:156088
J Transl Med, 2024, 22(1):248
S2779 M344 M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.
Nat Commun, 2020, 29;11(1):2086
Cell Syst, 2019, 8(2):97-108
Front Cell Neurosci, 2019, 13:468
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.
J Cancer, 2020, 6;11(14):4059-4072
Oncol Lett, 2020, 20(1):533-540
Biochemistry, 2019, 58(49):4912-4924
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.
Int J Mol Sci, 2021, 22(5)2592
Endocrinology, 2021, 162(5)bqab036
Oncogene, 2020, 39(13):2786-2796
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.
iScience, 2024, 27(9):110775
Cancer Res Commun, 2024, 4(2):349-364
Int J Mol Sci, 2023, 24(5)4805
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.
Biomedicines, 2024, 12(6)1203
Nat Commun, 2023, 14(1):5051
Nat Commun, 2023, 14(1):5051
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.
Nat Cell Biol, 2022, 24(4):483-496
Sci Rep, 2022, 12(1):22550
bioRxiv, 2020, 10.1101/2020.12.20.423672
S7278 HPOB HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
Tuberculosis (Edinb), 2021, 127:102062
Molecules, 2018, 23(5)
Neurochem Int, 2016, 99:239-51
S8323 ITSA-1 (ITSA1) ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors.
Front Pharmacol, 2024, 15:1333235
Clin Transl Med, 2022, 12(2):e747
Alzheimers Res Ther, 2021, 13(1):7
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.
Cell Mol Life Sci, 2023, 80(11):333
Cell Mol Life Sci, 2023, 80(11):333
Drug Dev Res, 2022, 10.1002/ddr.21927
S6738 TC-H 106 TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively.
Cell Rep, 2023, 42(11):113322
Cell Mol Life Sci, 2023, 80(11):333
Cell Mol Life Sci, 2023, 80(11):333
S6687 SIS17 SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
Cell Signal, 2023, 104:110555
BioRxiv, 2023, 10.1101/2023.06.01.543360
Clin Epigenetics, 2022, 14(1):147
S1703 Divalproex Sodium Divalproex Sodium, consisting of a compound of sodium valproate and valproic acid in a 1:1 molar relationship in an enteric coated form, is a HDAC inhibitor, used in the treatment for epilepsy.
CNS Neurosci Ther, 2018, 24(5):404-411
S0864 ACY-775 ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5  nM.
J Exp Clin Cancer Res, 2024, 43(1):152
Int J Mol Sci, 2023, 24(5)4720
S1073 BML-210 (CAY10433) BML-210 (CAY10433) is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM.
Cell Biochem Funct, 2022, 40(6):589-599
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).
Dev Cell, 2024, S1534-5807(24)00326-5
J Virol, 2022, e0044222
S9262 Raddeanin A Raddeanin A (Raddeanin R3, NSC382873), a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity.
Cell Mol Biol (Noisy-le-grand), 2020, 66(7):174-179
S3981 Sinapinic Acid Sinapinic acid (Sinapic acid) is a small naturally occurring hydroxycinnamic acid which belongs to phenylpropanoid family and commonly used as matrix in MALDI mass spectrometry. Sinapinic acid (Sinapic acid) acts as an inhibitor of HDAC, with IC50 of 2.27 mM, and also inhibits ACE-I activity.
ROYAL SOCIETY OF CHEMISTRY, 2023, 7, 2953-2973
E1086 KT-531 KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms.
E1912New B102(PARP/HDAC-IN-1) B102(PARP/HDAC-IN-1) is a dual inhibitor of PARP and HDAC, with IC50 of 19.01 nM, 2.13 nM, 1.69 μM, > 10 μM for PARP1, PARP2, HDAC1, HDAC6, respectively, in an enzymatic assay. It exhibits anti-proliferative and anti-tumor effects. It also induces DNA damage and apoptosis in vitro.
E1686New SW-100 SW-100 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 2.3 nM. It displays 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes.
E1580New TNG260 TNG260 is an inhibitor of CoREST-selective deacetylase (CoreDAC) that inhibits HDAC1 with 10-fold selectivity over HDAC3. It decreases intratumoral neutrophil infiltration and exhibits immune-mediated cell killing.
E1469 ITF3756 ITF3756 is a selective histone deacetylase 6 (HDAC6) inhibitor bearing a pentaheterocyclic scaffold. It can be used in research of autoimmune disorders, neurodegenerative diseases, and cancer.
E1554New Tefinostat(CHR-2845) Tefinostat(CHR-2845) is a monocyte/macrophage-targeted inhibitor of pan-histone deacetylase (HDAC). Tefinostat undergoes cleavage mediated by the intracellular esterase human carboxylesterase-1 (hCE-1) to yield the active acid CHR-2847. In vitro studies reveal a specific heightened sensitivity of monocytoid leukemias to tefinostat.
S2190New Pyroxamide (NSC 696085) Pyroxamide(NSC 696085) is a potent inhibitor of affinity-purified HDAC1 with ID50 of 100 nM. It also induces growth suppression and cell death in human rhabdomyosarcoma in vitro.
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.
Biomedicines, 2024, 12(6)1203
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.
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.
S6548 NKL 22 NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM.
E0391New BRD-6929 BRD-6929 is an inhibitor of histone deacetylase 1 (HDAC1) and HDAC2 with an IC50s of 0.04 µM and 0.1 µM, respectively. It exhibits antiproliferative activities against a human cancer cell line (HCT116) and in human mammary epithelial cells (HMEC).
S5771 Sulforaphane Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis.,
Nucleic Acids Res, 2024, gkae761
Redox Biol, 2024, 72:103137
J Adv Res, 2024, S2090-1232(24)00422-3
S7726 BRD73954 BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
E0812 CXD101 CXD101 (HDAC-IN-4) is a potent, selective and orally active class I histone deacetylase (HDAC) inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively.
S5905 Suberohydroxamic acid Suberohydroxamic acid (suberic bishydroxamic acid) is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively.
S8962 BRD3308 BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release.
S7593 Splitomicin Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.
S5438 Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
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.
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.
S1313 GSK3117391 GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor.
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).
S1047 Vorinostat (SAHA) Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Cell Rep, 2024, 43(1):113575
NPJ Precis Oncol, 2024, 8(1):52
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-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. Entinostat induces autophagy and apoptosis. Phase 3.
Nat Commun, 2024, 15(1):4739
Nat Commun, 2024, 15(1):8044
J Clin Invest, 2024, 134(6)e171063
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Nat Commun, 2024, 15(1):5209
Nat Commun, 2024, 15(1):4450
Emerg Microbes Infect, 2024, 13(1):2327371
S1045 TSA (Trichostatin A) TSA (Trichostatin A) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Nat Commun, 2024, 15(1):1190
Nat Commun, 2024, 15(1):5209
Nat Commun, 2024, 15(1):9463
S3020 Romidepsin Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.
Nat Commun, 2024, 15(1):2989
Nucleic Acids Res, 2024, 52(1):141-153
Cell Rep, 2024, 43(2):113778
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) 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. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Dev Cell, 2024, S1534-5807(24)00326-5
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Clin Epigenetics, 2024, 16(1):13
S7229 RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Sci Immunol, 2024, 9(99):eadk7387
Nat Commun, 2024, 15(1):8044
Acta Pharm Sin B, 2024, 14(2):712-728
S1085 Belinostat Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
Nat Commun, 2024, 15(1):4739
J Immunother Cancer, 2024, 12(10)e009590
Cell Rep, 2024, 43(1):113575
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.
Theranostics, 2024, 14(6):2345-2366
Biomedicines, 2024, 12(6)1203
Life Sci Alliance, 2024, 7(7)e202302384
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.
Cancer Immunol Immunother, 2024, 73(1):7
Cancer Immunol Immunother, 2024, 73(1):7
Cancer Res Commun, 2024, 4(2):349-364
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.
iScience, 2024, 27(4):109366
iScience, 2024, 27(9):110775
Int J Mol Sci, 2024, 25(3):1411.
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.
iScience, 2024, 27(9):110775
Front Med (Lausanne), 2022, 9:848938
Hepatology, 2021, 10.1002/hep.32245
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).
Nat Metab, 2022, 4(1):44-59
Cancer Lett, 2022, 549:215911
Elife, 2022, 11e67368
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. PCI-34051 induces caspase-dependent apoptosis.
J Cell Mol Med, 2024, 28(18):e70114
The University of Auckland, 2023,
Reprod Med Biol, 2023, 22(1):e12527
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Cancer Cell Int, 2024, 24(1):303
Front Pharmacol, 2024, 15:1418902
PLoS Negl Trop Dis, 2024, 18(8):e0012428
S2818 Tacedinaline (CI994) Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) 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.
Adv Sci (Weinh), 2024, 11(24):e2308945
Biomedicines, 2024, 12(6)1203
J Transl Med, 2023, 21(1):604
S7569 LMK-235 LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
Dev Cell, 2024, S1534-5807(24)00326-5
Environ Pollut, 2024, 355:124194
Shock, 2023, 60(1):75-83
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.
Viruses, 2024, 16(5)775
JCI Insight, 2023, 8(7)e162907
Cell Biosci, 2022, 12(1):135
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.
Dev Cell, 2024, S1534-5807(24)00326-5
Br J Cancer, 2023, 10.1038/s41416-023-02195-0
Int J Mol Sci, 2023, 24(5)4720
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.
J Leukoc Biol, 2024, qiae006
Sci Transl Med, 2022, 14(657):eabg3277
J Exp Clin Cancer Res, 2022, 41(1):325
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
J Exp Clin Cancer Res, 2024, 43(1):152
J Immunother Cancer, 2024, 12(11)e009805
Sci Total Environ, 2022, 838(Pt 2):155825
S3944 VPA (Valproic acid) VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
Nat Commun, 2024, 15(1):668
Dev Cell, 2024, S1534-5807(24)00326-5
S2244 AR-42 AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1.
Nat Commun, 2024, 15(1):4739
EBioMedicine, 2024, 105:105211
Int J Mol Sci, 2024, 25(14)7866
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.
Biomedicines, 2024, 12(6)1203
Cell Syst, 2023, 14(6):482-500.e8
Elife, 2022, 11e73718
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
Nat Commun, 2024, 15(1):4764
Nat Commun, 2024, 15(1):5209
Cell Rep, 2024, 43(2):113778
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.
EBioMedicine, 2024, 105:105211
Nat Commun, 2023, 14(1):5051
Nat Commun, 2023, 14(1):5051
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.
Nat Commun, 2023, 14(1):2095
Nat Commun, 2023, 14(1):2095
J Transl Med, 2023, 21(1):604
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.
Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
Cancers (Basel), 2024, 16(21)3606
Nat Commun, 2022, 13(1):2666
S7595 Santacruzamate A (CAY10683) Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.
J Exp Clin Cancer Res, 2024, 43(1):152
Cell Death Dis, 2024, 15(8):593
Nat Commun, 2023, 14(1):5051
S2341 (-)-Parthenolide (-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.
Genes Environ, 2024, 46(1):10
Transl Oncol, 2023, 35:101712
PLoS Genet, 2021, 17(11):e1009890
S1095 Dacinostat (LAQ824) Dacinostat (LAQ824, NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.
Int J Mol Sci, 2023, 24(17)13660
Clin Transl Med, 2022, 12(5):e798
Cancers (Basel), 2022, 14(19)4708
S7596 CAY10603 CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
EBioMedicine, 2024, 105:105211
iScience, 2024, 27(9):110775
Respir Res, 2024, 25(1):66
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.
Cell Stress Chaperones, 2024, 29(3):359-380
Cancer Res Commun, 2024, 4(2):349-364
Cell Death Dis, 2023, 14(2):142
S7617 Tasquinimod Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
Signal Transduct Target Ther, 2023, 8(1):11
Nat Commun, 2022, 13(1):1481
Int J Biol Sci, 2022, 18(15):5724-5739
S4125 4-PBA (Sodium Phenylbutyrate) 4-PBA (Sodium Phenylbutyrate) is a salt of 4-phenylbutyrate (4-PBA) or 4-phenylbutyric acid.Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders.
J Clin Invest, 2024, e175310
Aging Cell, 2023, 22(6):e13840
Inflammopharmacology, 2023, 31(3):1319-1327
S8567 Tucidinostat (Chidamide) Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
Cell Death Dis, 2024, 15(1):95
Clin Immunol, 2024, 260:109915
Mol Cancer Ther, 2024, 23(4):520-531
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.
Dev Cell, 2024, S1534-5807(24)00326-5
Nat Commun, 2023, 14(1):2095
Nat Commun, 2023, 14(1):2095
S7473 Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
Biomedicines, 2024, 12(6)1203
Cancer Res Commun, 2024, 4(2):349-364
Int J Mol Sci, 2023, 24(5)4720
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.
PLoS One, 2024, 19(6):e0304914
Exp Ther Med, 2021, 21(5):515
Cancer Sci, 2020, 111(7):2374-2384
S7555 Domatinostat (4SC-202) Domatinostat (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.
Nat Commun, 2023, 14(1):5051
Nat Commun, 2023, 14(1):5051
Cell Rep Med, 2023, 4(7):101101
S8043 Scriptaid Scriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.
Cell Res, 2022, 10.1038/s41422-022-00668-0
J Appl Physiol (1985), 2020, 128(2):276-285
Nat Biotechnol, 2019, 10.1038/s41587-019-0372-z
S3592 4-PBA (4-Phenylbutyric acid) 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
Int J Biol Sci, 2024, 20(4):1279-1296
Phytomedicine, 2024, 135:156088
J Transl Med, 2024, 22(1):248
S2779 M344 M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.
Nat Commun, 2020, 29;11(1):2086
Cell Syst, 2019, 8(2):97-108
Front Cell Neurosci, 2019, 13:468
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.
J Cancer, 2020, 6;11(14):4059-4072
Oncol Lett, 2020, 20(1):533-540
Biochemistry, 2019, 58(49):4912-4924
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.
Int J Mol Sci, 2021, 22(5)2592
Endocrinology, 2021, 162(5)bqab036
Oncogene, 2020, 39(13):2786-2796
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.
iScience, 2024, 27(9):110775
Cancer Res Commun, 2024, 4(2):349-364
Int J Mol Sci, 2023, 24(5)4805
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.
Biomedicines, 2024, 12(6)1203
Nat Commun, 2023, 14(1):5051
Nat Commun, 2023, 14(1):5051
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.
Nat Cell Biol, 2022, 24(4):483-496
Sci Rep, 2022, 12(1):22550
bioRxiv, 2020, 10.1101/2020.12.20.423672
S7278 HPOB HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
Tuberculosis (Edinb), 2021, 127:102062
Molecules, 2018, 23(5)
Neurochem Int, 2016, 99:239-51
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.
Cell Mol Life Sci, 2023, 80(11):333
Cell Mol Life Sci, 2023, 80(11):333
Drug Dev Res, 2022, 10.1002/ddr.21927
S6738 TC-H 106 TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively.
Cell Rep, 2023, 42(11):113322
Cell Mol Life Sci, 2023, 80(11):333
Cell Mol Life Sci, 2023, 80(11):333
S6687 SIS17 SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
Cell Signal, 2023, 104:110555
BioRxiv, 2023, 10.1101/2023.06.01.543360
Clin Epigenetics, 2022, 14(1):147
S1703 Divalproex Sodium Divalproex Sodium, consisting of a compound of sodium valproate and valproic acid in a 1:1 molar relationship in an enteric coated form, is a HDAC inhibitor, used in the treatment for epilepsy.
CNS Neurosci Ther, 2018, 24(5):404-411
S0864 ACY-775 ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5  nM.
J Exp Clin Cancer Res, 2024, 43(1):152
Int J Mol Sci, 2023, 24(5)4720
S1073 BML-210 (CAY10433) BML-210 (CAY10433) is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM.
Cell Biochem Funct, 2022, 40(6):589-599
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).
Dev Cell, 2024, S1534-5807(24)00326-5
J Virol, 2022, e0044222
S9262 Raddeanin A Raddeanin A (Raddeanin R3, NSC382873), a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity.
Cell Mol Biol (Noisy-le-grand), 2020, 66(7):174-179
S3981 Sinapinic Acid Sinapinic acid (Sinapic acid) is a small naturally occurring hydroxycinnamic acid which belongs to phenylpropanoid family and commonly used as matrix in MALDI mass spectrometry. Sinapinic acid (Sinapic acid) acts as an inhibitor of HDAC, with IC50 of 2.27 mM, and also inhibits ACE-I activity.
ROYAL SOCIETY OF CHEMISTRY, 2023, 7, 2953-2973
E1086 KT-531 KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms.
E1912New B102(PARP/HDAC-IN-1) B102(PARP/HDAC-IN-1) is a dual inhibitor of PARP and HDAC, with IC50 of 19.01 nM, 2.13 nM, 1.69 μM, > 10 μM for PARP1, PARP2, HDAC1, HDAC6, respectively, in an enzymatic assay. It exhibits anti-proliferative and anti-tumor effects. It also induces DNA damage and apoptosis in vitro.
E1686New SW-100 SW-100 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 2.3 nM. It displays 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes.
E1580New TNG260 TNG260 is an inhibitor of CoREST-selective deacetylase (CoreDAC) that inhibits HDAC1 with 10-fold selectivity over HDAC3. It decreases intratumoral neutrophil infiltration and exhibits immune-mediated cell killing.
E1469 ITF3756 ITF3756 is a selective histone deacetylase 6 (HDAC6) inhibitor bearing a pentaheterocyclic scaffold. It can be used in research of autoimmune disorders, neurodegenerative diseases, and cancer.
E1554New Tefinostat(CHR-2845) Tefinostat(CHR-2845) is a monocyte/macrophage-targeted inhibitor of pan-histone deacetylase (HDAC). Tefinostat undergoes cleavage mediated by the intracellular esterase human carboxylesterase-1 (hCE-1) to yield the active acid CHR-2847. In vitro studies reveal a specific heightened sensitivity of monocytoid leukemias to tefinostat.
S2190New Pyroxamide (NSC 696085) Pyroxamide(NSC 696085) is a potent inhibitor of affinity-purified HDAC1 with ID50 of 100 nM. It also induces growth suppression and cell death in human rhabdomyosarcoma in vitro.
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.
Biomedicines, 2024, 12(6)1203
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.
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.
S6548 NKL 22 NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM.
E0391New BRD-6929 BRD-6929 is an inhibitor of histone deacetylase 1 (HDAC1) and HDAC2 with an IC50s of 0.04 µM and 0.1 µM, respectively. It exhibits antiproliferative activities against a human cancer cell line (HCT116) and in human mammary epithelial cells (HMEC).
S5771 Sulforaphane Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis.,
Nucleic Acids Res, 2024, gkae761
Redox Biol, 2024, 72:103137
J Adv Res, 2024, S2090-1232(24)00422-3
S7726 BRD73954 BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
E0812 CXD101 CXD101 (HDAC-IN-4) is a potent, selective and orally active class I histone deacetylase (HDAC) inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively.
S5905 Suberohydroxamic acid Suberohydroxamic acid (suberic bishydroxamic acid) is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively.
S8962 BRD3308 BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release.
S7593 Splitomicin Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.
S5438 Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
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.
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.
S1313 GSK3117391 GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor.
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).
S8323 ITSA-1 (ITSA1) ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors.
Front Pharmacol, 2024, 15:1333235
Clin Transl Med, 2022, 12(2):e747
Alzheimers Res Ther, 2021, 13(1):7
E1912New B102(PARP/HDAC-IN-1) B102(PARP/HDAC-IN-1) is a dual inhibitor of PARP and HDAC, with IC50 of 19.01 nM, 2.13 nM, 1.69 μM, > 10 μM for PARP1, PARP2, HDAC1, HDAC6, respectively, in an enzymatic assay. It exhibits anti-proliferative and anti-tumor effects. It also induces DNA damage and apoptosis in vitro.
E1686New SW-100 SW-100 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 2.3 nM. It displays 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes.
E1580New TNG260 TNG260 is an inhibitor of CoREST-selective deacetylase (CoreDAC) that inhibits HDAC1 with 10-fold selectivity over HDAC3. It decreases intratumoral neutrophil infiltration and exhibits immune-mediated cell killing.
E1554New Tefinostat(CHR-2845) Tefinostat(CHR-2845) is a monocyte/macrophage-targeted inhibitor of pan-histone deacetylase (HDAC). Tefinostat undergoes cleavage mediated by the intracellular esterase human carboxylesterase-1 (hCE-1) to yield the active acid CHR-2847. In vitro studies reveal a specific heightened sensitivity of monocytoid leukemias to tefinostat.
S2190New Pyroxamide (NSC 696085) Pyroxamide(NSC 696085) is a potent inhibitor of affinity-purified HDAC1 with ID50 of 100 nM. It also induces growth suppression and cell death in human rhabdomyosarcoma in vitro.
E0391New BRD-6929 BRD-6929 is an inhibitor of histone deacetylase 1 (HDAC1) and HDAC2 with an IC50s of 0.04 µM and 0.1 µM, respectively. It exhibits antiproliferative activities against a human cancer cell line (HCT116) and in human mammary epithelial cells (HMEC).

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