HDAC

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HDAC Signaling Pathway Map

HDAC Signaling Pathways

HDAC Products

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  • New HDAC Products
Catalog No. Product Name Information Product Use Citations Product Validations
E1194New HDAC10-IN-1 HDAC10-IN-1 (10c), a nanomolar inhibitors of HDAC10 with high specificity, inhibits HDAC10 with high specificity over HDAC6 and with no significant impact on class I HDACs, with a IC50 of 20 nM on danio rerio HDAC10 (drHDAC10).
E1195New HDAC10-IN-2 HDAC10-IN-1 (13b), a nanomolar inhibitors of HDAC10 with high specificity, inhibits HDAC10 with high specificity over HDAC6 and with no significant impact on class I HDACs, with a IC50 of 58 nM on danio rerio HDAC10 (drHDAC10).
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.
Drug Dev Res, 2022, 10.1002/ddr.21927
S0864 ACY-775 ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5  nM.
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.
Signal Transduct Target Ther, 2022, 7(1):98
Blood, 2022, blood.2022016241
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
S1045 Trichostatin A (TSA) Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Cell Stem Cell, 2022, S1934-5909(22)00010-8
Cell Res, 2022, 10.1038/s41422-022-00668-0
Nat Neurosci, 2022, 25(5):596-606
S1047 Vorinostat (SAHA) Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683, Zolinza) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Nature, 2022, 605(7908):160-165
Nat Commun, 2022, 13(1):107
Clin Transl Med, 2022, 12(5):e798
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.
Nature, 2022, 602(7895):112-116
Cell Res, 2022, 10.1038/s41422-022-00668-0
J Clin Invest, 2022, e147908
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.
S1085 Belinostat (PXD101) Belinostat (PXD101, NSC726630, PX-105684) 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.
Clin Transl Med, 2022, 12(5):e798
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
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 Commun, 2022, 13(1):2666
Clin Transl Med, 2022, 12(5):e798
Nucleic Acids Res, 2021, 49(4):2390-2399
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.
Clin Transl Med, 2022, 12(5):e798
ACS Omega, 2019, 4(22):19895-19904
Cancer Res, 2018, 78(20):5731-5740
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.
NPJ Precis Oncol, 2022, 6(1):5
Nat Commun, 2021, 12(1):5404
Nucleic Acids Res, 2021, 49(4):2390-2399
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.
Cell Res, 2022, 10.1038/s41422-022-00668-0
J Clin Invest, 2022, e147908
Cancer Cell, 2021, S1535-6108(20)30662-0
S1168 Valproic Acid (NSC 93819) sodium salt Valproic Acid sodium salt (NSC 93819, 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. 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.
Sci Total Environ, 2022, 838(Pt 2):155825
Transl Psychiatry, 2022, 12(1):130
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13014
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.
Cancer Sci, 2020, 112(1):133-143
Anticancer Drugs, 2020, 31(2):158-168
NPJ Breast Cancer, 2020, 6:30
S1313 GSK3117391 GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor.
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.
Exp Ther Med, 2021, 21(5):515
Cancer Sci, 2020, 111(7):2374-2384
Cancer Res, 2018, 78(20):5731-5740
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.
Front Med (Lausanne), 2022, 9:848938
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
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.
Nat Commun, 2022, 13(1):2666
Mol Biol Rep, 2022, 10.1007/s11033-022-07559-y
Cancer Lett, 2021, 521:268-280
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
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.
Phytother Res, 2022, 36(3):1326-1337
Dis Markers, 2022, 2022:3129781
Adv Sci (Weinh), 2021, e2103360
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.
J Exp Clin Cancer Res, 2022, 41(1):111
Int J Mol Sci, 2022, 23(8)4213
Cell Mol Life Sci, 2021, 10.1007/s00018-021-03883-x
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.
Cell Rep, 2021, 37(12):110129
Thyroid, 2021, 10.1089/thy.2020.0948
Tuberculosis (Edinb), 2021, 127:102062
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.
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.
Elife, 2021, 10e68714
PLoS One, 2021, 16(11):e0260633
Cancers (Basel), 2020, 12(11)E3161
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.
Oncogene, 2022, 10.1038/s41388-022-02236-7
Signal Transduct Target Ther, 2021, 6(1):333
STAR Protoc, 2021, 2(3):100674
S2244 AR-42 AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1.
Nat Commun, 2021, 12(1):256
Cancer Cell, 2020, 13;37(4):599-617 e7
J Mater Chem B, 2020, 8(37):8558-8572
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.
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
S2627 Tubastatin A HCl Tubastatin A HCl (TSA) 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).
Elife, 2022, 11e67368
Drug Dev Res, 2022, 10.1002/ddr.21927
Sci Adv, 2021, 7(49):eabk0490
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
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.
Transl Oncol, 2022, 18:101362
Blood Cancer J, 2021, 11(6):111
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
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
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.
Nat Commun, 2022, 13(1):205
J Virol, 2022, e0044222
Front Oncol, 2021, 11:648023
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.
J Clin Invest, 2022, e147908
Mol Psychiatry, 2022, 10.1038/s41380-022-01566-y
Theranostics, 2022, 12(4):1715-1729
S3592 4-Phenylbutyric acid (4-PBA) 4-Phenylbutyric acid (4-PBA, Benzenebutyric 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.
Toxicol In Vitro, 2021, 77:105249
Nan Fang Yi Ke Da Xue Xue Bao, 2021, 41(5):702-709
Part Fibre Toxicol, 2020, 17(1):50
S3944 Valproic acid (VPA) Valproic acid (VPA, 2-Propylvaleric Acid, Valproate) 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.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Int J Mol Sci, 2022, 23(8)4213
Front Immunol, 2021, 12:771453
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.
S4125 Sodium Phenylbutyrate Sodium phenylbutyrate (4-PBA, 4-Phenylbutyric acid, NaPB) 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.
Cell Death Dis, 2021, 12(11):1016
Am J Cancer Res, 2021, 11(3):691-711
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00700-w
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.
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.
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.
S6548 NKL 22 NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM.
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.
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.
J Virol, 2022, e0044222
S7229 RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Cell Rep, 2022, 38(4):110302
Cytokine, 2022, 153:155842
Thyroid, 2021, 10.1089/thy.2020.0948
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
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.
Front Mol Neurosci, 2021, 14:616886
Nat Metab, 2021, 3(1):75-89
Theranostics, 2020, 10(21):9644-9662
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.
Endocrinology, 2022, bqac038
Cell Death Dis, 2021, 12(6):501
Signal Transduct Target Ther, 2021, 6(1):333
S7473 Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
Cancer Res Treat, 2022, 54(2):458-468
Cell Prolif, 2021, 54(6):e13054
Cancer Discov, 2019, 9(4):526-545
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.
Cancers (Basel), 2022, 14(7)1753
Oral Dis, 2021, 10.1111/odi.13860
Cancers (Basel), 2020, 23;12(3) pii: E756
S7569 LMK-235 LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
Int J Biol Macromol, 2022, 211:556-567
Biochem Biophys Res Commun, 2022, 615:136-142
Thyroid, 2021, 10.1089/thy.2020.0948
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.
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.
Thyroid, 2021, 10.1089/thy.2020.0948
Brain Res Bull, 2021, 175:213-223
Nat Cell Biol, 2020,
S7596 CAY10603 CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
Oncogene, 2022, 10.1038/s41388-022-02236-7
Neuro Oncol, 2021, 23(3):376-386
Cancer Res, 2021, canres.0955.2021
S7617 Tasquinimod Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
Nat Commun, 2022, 13(1):1481
Thyroid, 2021, 10.1089/thy.2020.0948
Int J Mol Sci, 2021, 22(3)E1011
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.
Nucleic Acids Res, 2020, 6;48(6):2912-2923
Front Aging Neurosci, 2020, 12:619866
Anticancer Drugs, 2018, 29(1):61-74
S7726 BRD73954 BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
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.
Int J Oncol, 2022, 60(5)54
Cancer Chemother Pharmacol, 2022, 89(5):643-653
Cancer Res, 2021, 81(20):5325-5335
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
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.
Drug Dev Res, 2022, 10.1002/ddr.21927
Sci Adv, 2021, 7(49):eabk0490
Sci Adv, 2021, 7(49):eabk0490
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
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.
Front Pharmacol, 2022, 13:780179
Nat Metab, 2021, 3(1):75-89
S8502 TMP195 TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
Clin Epigenetics, 2021, 13(1):187
Cell, 2020, S0092-8674(20)31394-5
Front Immunol, 2020, 3;11:36
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.
Clin Transl Med, 2022, 12(5):e798
iScience, 2022, 25(4):104153
Signal Transduct Target Ther, 2021, 6(1):333
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.
bioRxiv, 2020, 10.1101/2020.12.20.423672
J Biomed Sci, 2019, 26(1):27
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.
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).
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).
J Virol, 2022, e0044222
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.
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
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.
S9934New 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.
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.
Elife, 2022, 11e67368
Cell Death Discov, 2021, 7(1):375
Cell Commun Signal, 2021, 19(1):35
S8323 ITSA-1 (ITSA1) ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors.
Clin Transl Med, 2022, 12(2):e747
Alzheimers Res Ther, 2021, 13(1):7
Cancer Res, 2018, 78(20):5731-5740
E1194New HDAC10-IN-1 HDAC10-IN-1 (10c), a nanomolar inhibitors of HDAC10 with high specificity, inhibits HDAC10 with high specificity over HDAC6 and with no significant impact on class I HDACs, with a IC50 of 20 nM on danio rerio HDAC10 (drHDAC10).
E1195New HDAC10-IN-2 HDAC10-IN-1 (13b), a nanomolar inhibitors of HDAC10 with high specificity, inhibits HDAC10 with high specificity over HDAC6 and with no significant impact on class I HDACs, with a IC50 of 58 nM on danio rerio HDAC10 (drHDAC10).
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.
Drug Dev Res, 2022, 10.1002/ddr.21927
S0864 ACY-775 ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5  nM.
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.
Signal Transduct Target Ther, 2022, 7(1):98
Blood, 2022, blood.2022016241
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
S1045 Trichostatin A (TSA) Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Cell Stem Cell, 2022, S1934-5909(22)00010-8
Cell Res, 2022, 10.1038/s41422-022-00668-0
Nat Neurosci, 2022, 25(5):596-606
S1047 Vorinostat (SAHA) Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683, Zolinza) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Nature, 2022, 605(7908):160-165
Nat Commun, 2022, 13(1):107
Clin Transl Med, 2022, 12(5):e798
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.
Nature, 2022, 602(7895):112-116
Cell Res, 2022, 10.1038/s41422-022-00668-0
J Clin Invest, 2022, e147908
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.
S1085 Belinostat (PXD101) Belinostat (PXD101, NSC726630, PX-105684) 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.
Clin Transl Med, 2022, 12(5):e798
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
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 Commun, 2022, 13(1):2666
Clin Transl Med, 2022, 12(5):e798
Nucleic Acids Res, 2021, 49(4):2390-2399
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.
Clin Transl Med, 2022, 12(5):e798
ACS Omega, 2019, 4(22):19895-19904
Cancer Res, 2018, 78(20):5731-5740
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.
NPJ Precis Oncol, 2022, 6(1):5
Nat Commun, 2021, 12(1):5404
Nucleic Acids Res, 2021, 49(4):2390-2399
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.
Cell Res, 2022, 10.1038/s41422-022-00668-0
J Clin Invest, 2022, e147908
Cancer Cell, 2021, S1535-6108(20)30662-0
S1168 Valproic Acid (NSC 93819) sodium salt Valproic Acid sodium salt (NSC 93819, 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. 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.
Sci Total Environ, 2022, 838(Pt 2):155825
Transl Psychiatry, 2022, 12(1):130
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13014
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.
Cancer Sci, 2020, 112(1):133-143
Anticancer Drugs, 2020, 31(2):158-168
NPJ Breast Cancer, 2020, 6:30
S1313 GSK3117391 GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor.
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.
Exp Ther Med, 2021, 21(5):515
Cancer Sci, 2020, 111(7):2374-2384
Cancer Res, 2018, 78(20):5731-5740
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.
Front Med (Lausanne), 2022, 9:848938
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
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.
Nat Commun, 2022, 13(1):2666
Mol Biol Rep, 2022, 10.1007/s11033-022-07559-y
Cancer Lett, 2021, 521:268-280
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
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.
Phytother Res, 2022, 36(3):1326-1337
Dis Markers, 2022, 2022:3129781
Adv Sci (Weinh), 2021, e2103360
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.
J Exp Clin Cancer Res, 2022, 41(1):111
Int J Mol Sci, 2022, 23(8)4213
Cell Mol Life Sci, 2021, 10.1007/s00018-021-03883-x
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.
Cell Rep, 2021, 37(12):110129
Thyroid, 2021, 10.1089/thy.2020.0948
Tuberculosis (Edinb), 2021, 127:102062
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.
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.
Elife, 2021, 10e68714
PLoS One, 2021, 16(11):e0260633
Cancers (Basel), 2020, 12(11)E3161
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.
Oncogene, 2022, 10.1038/s41388-022-02236-7
Signal Transduct Target Ther, 2021, 6(1):333
STAR Protoc, 2021, 2(3):100674
S2244 AR-42 AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1.
Nat Commun, 2021, 12(1):256
Cancer Cell, 2020, 13;37(4):599-617 e7
J Mater Chem B, 2020, 8(37):8558-8572
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.
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
S2627 Tubastatin A HCl Tubastatin A HCl (TSA) 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).
Elife, 2022, 11e67368
Drug Dev Res, 2022, 10.1002/ddr.21927
Sci Adv, 2021, 7(49):eabk0490
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
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.
Transl Oncol, 2022, 18:101362
Blood Cancer J, 2021, 11(6):111
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
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
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.
Nat Commun, 2022, 13(1):205
J Virol, 2022, e0044222
Front Oncol, 2021, 11:648023
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.
J Clin Invest, 2022, e147908
Mol Psychiatry, 2022, 10.1038/s41380-022-01566-y
Theranostics, 2022, 12(4):1715-1729
S3592 4-Phenylbutyric acid (4-PBA) 4-Phenylbutyric acid (4-PBA, Benzenebutyric 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.
Toxicol In Vitro, 2021, 77:105249
Nan Fang Yi Ke Da Xue Xue Bao, 2021, 41(5):702-709
Part Fibre Toxicol, 2020, 17(1):50
S3944 Valproic acid (VPA) Valproic acid (VPA, 2-Propylvaleric Acid, Valproate) 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.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Int J Mol Sci, 2022, 23(8)4213
Front Immunol, 2021, 12:771453
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.
S4125 Sodium Phenylbutyrate Sodium phenylbutyrate (4-PBA, 4-Phenylbutyric acid, NaPB) 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.
Cell Death Dis, 2021, 12(11):1016
Am J Cancer Res, 2021, 11(3):691-711
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00700-w
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.
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.
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.
S6548 NKL 22 NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM.
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.
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.
J Virol, 2022, e0044222
S7229 RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Cell Rep, 2022, 38(4):110302
Cytokine, 2022, 153:155842
Thyroid, 2021, 10.1089/thy.2020.0948
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
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.
Front Mol Neurosci, 2021, 14:616886
Nat Metab, 2021, 3(1):75-89
Theranostics, 2020, 10(21):9644-9662
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.
Endocrinology, 2022, bqac038
Cell Death Dis, 2021, 12(6):501
Signal Transduct Target Ther, 2021, 6(1):333
S7473 Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
Cancer Res Treat, 2022, 54(2):458-468
Cell Prolif, 2021, 54(6):e13054
Cancer Discov, 2019, 9(4):526-545
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.
Cancers (Basel), 2022, 14(7)1753
Oral Dis, 2021, 10.1111/odi.13860
Cancers (Basel), 2020, 23;12(3) pii: E756
S7569 LMK-235 LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
Int J Biol Macromol, 2022, 211:556-567
Biochem Biophys Res Commun, 2022, 615:136-142
Thyroid, 2021, 10.1089/thy.2020.0948
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.
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.
Thyroid, 2021, 10.1089/thy.2020.0948
Brain Res Bull, 2021, 175:213-223
Nat Cell Biol, 2020,
S7596 CAY10603 CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
Oncogene, 2022, 10.1038/s41388-022-02236-7
Neuro Oncol, 2021, 23(3):376-386
Cancer Res, 2021, canres.0955.2021
S7617 Tasquinimod Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
Nat Commun, 2022, 13(1):1481
Thyroid, 2021, 10.1089/thy.2020.0948
Int J Mol Sci, 2021, 22(3)E1011
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.
Nucleic Acids Res, 2020, 6;48(6):2912-2923
Front Aging Neurosci, 2020, 12:619866
Anticancer Drugs, 2018, 29(1):61-74
S7726 BRD73954 BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
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.
Int J Oncol, 2022, 60(5)54
Cancer Chemother Pharmacol, 2022, 89(5):643-653
Cancer Res, 2021, 81(20):5325-5335
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
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.
Drug Dev Res, 2022, 10.1002/ddr.21927
Sci Adv, 2021, 7(49):eabk0490
Sci Adv, 2021, 7(49):eabk0490
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
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.
Front Pharmacol, 2022, 13:780179
Nat Metab, 2021, 3(1):75-89
S8502 TMP195 TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
Clin Epigenetics, 2021, 13(1):187
Cell, 2020, S0092-8674(20)31394-5
Front Immunol, 2020, 3;11:36
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.
Clin Transl Med, 2022, 12(5):e798
iScience, 2022, 25(4):104153
Signal Transduct Target Ther, 2021, 6(1):333
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.
bioRxiv, 2020, 10.1101/2020.12.20.423672
J Biomed Sci, 2019, 26(1):27
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.
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).
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).
J Virol, 2022, e0044222
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.
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
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.
S9934New 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.
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.
Elife, 2022, 11e67368
Cell Death Discov, 2021, 7(1):375
Cell Commun Signal, 2021, 19(1):35
S8323 ITSA-1 (ITSA1) ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors.
Clin Transl Med, 2022, 12(2):e747
Alzheimers Res Ther, 2021, 13(1):7
Cancer Res, 2018, 78(20):5731-5740
E1194New HDAC10-IN-1 HDAC10-IN-1 (10c), a nanomolar inhibitors of HDAC10 with high specificity, inhibits HDAC10 with high specificity over HDAC6 and with no significant impact on class I HDACs, with a IC50 of 20 nM on danio rerio HDAC10 (drHDAC10).
E1195New HDAC10-IN-2 HDAC10-IN-1 (13b), a nanomolar inhibitors of HDAC10 with high specificity, inhibits HDAC10 with high specificity over HDAC6 and with no significant impact on class I HDACs, with a IC50 of 58 nM on danio rerio HDAC10 (drHDAC10).
S9934New 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.
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