HDAC8-IN-20a is a potent, selective HDAC8 inhibitor with IC50 of 27 nM.

ZSNI-21 is a dual inhibitor of ADAM17 and HDAC2. ZSNI-21 effectively inhibits the proliferation of Bel-7402 cells and demonstrates significant anti-metastatic capabilities against HCC-LM3 cells. ZSNI-21 is promising for research of hepatocellular carcinoma (HCC).

S234984 (Compound 13) is a molecular glue enhancer can specifically bind to KBTBD4 and HDAC2 to form a stable ternary complex. S234984 can be used for anti-cancer study.

LSQ-28 is an orally active HDAC3 inhibitor with an IC50 of 42 nM, and exhibits potent anticancer, antiproliferative, antimigratory, anti-invasive, and antiwound healing activities. LSQ-28 can be utilized in cancer research.

KT32 (10c) is a potent dual inhibitor of HDAC and Topo II α. KT32 induces cell death through apoptosis.

HDSI-18 is an orally active HDAC6 selective inhibitor (IC50: 1.6 nM). HDSI-18 is cytotoxic to K562, MV4-11, MOLM-13, THP-1, and Jurkat cells (IC50: 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively). HDSI-18 activates Caspase-3, induces mitochondrial depolarization and apoptosis, and has antitumor activity.

Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by inhibiting HDAC6 activity, with an IC50 value of 63 nM. It also exhibits good selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat significantly downregulates fibrotic markers (fibronectin and collagen 1) in fibroblasts. Additionally, Fibrostat demonstrated no toxicity in rat-perfused heart and zebrafish larvae models. Fibrostat shows potential for research into fibrosis-related diseases.

FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively.

DS-103 is an inhibitor for HDAC that inhibits HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8 with IC50s of 0.029, 0.123, 0.022, 0.367 and 9.26 μM, respectively. DS-103 inhibits Plasmodium falciparum 3D7 with IC50 of 5.08 μM. DS-103 exhibits cytotoxicity in cells A2780 and Cal27 with IC50 of 1.48 μM and 1.47 μM, reverses Cisplatin resistance in A2780 and Cal27 with IC50 of 4.62 μM and 2.23 μM. DS-103 exhibits synergistic effect with Cisplatin, enhances Cisplatin-induced apoptosis.

CS4 is a selective HDAC inhibitor with the IC50 values of 38 nM, 12 nM, 5.8 μM, 19 μM and 61 μM against of HDAC1, HDAC6, HDAC8, HDAC4 and HDAC11, respectively. CS4 promotes α-tubulin and histone 3 acetylation. CS4 activates PPARγ and blocks glycolysis. CS4 induces cell cycle arrest at G2 phase and apoptosis, and shows anticancer effect both in vivo and in vitro.

CHDI-00484077 (Compound 12) is a CNS-penetrant class IIa HDAC inhibitor, with IC50s of 0.01 μM (HDAC4), 0.02 μM(HDAC5), 0.02 μM (HDAC7), 0.03 μM (HDAC9) respectively. CHDI-00484077 can be used for research of huntington’s disease.

C1A is a class I/II HDACs and sirtuin inhibitor with an IC50 of 479 nM for HDAC6. C1A induces sustained acetylation of HDAC6 substrates, α-tubulin and HSP90. C1A shows srtong anticancer effcts, and induces apoptosis in cancer cells.

Butyrylhydroxamic acid (N-Hydroxybutanamide) is a potent inhibitor of histone deacetylase (HDAC). Butyrylhydroxamic acid enhances memory in behavioral models of rodents and can be used as memory enhancers, mood stabilizers, and β-chain hemoglobin disease studies.

Bavarostat (EKZ-001) is a BBB-penetrable and selective HDAC6 inhibitor (IC50: 0.06 μM). Bavarostat modulates tubulin acetylation selectively over histone acetylation. Bavarostat can be used for research of cancers and central nervous system (CNS) disorders.

(Rac)-Nanatinostat ((Rac)-CHR-3996, example 44) is a potent HDAC inhibitor with an IC50 of <330 nM. (Rac)-Nanatinostat has anticancer effects and can effectively inhibit the cell growth of HeLa, U937 and HUT cells.

​​RBC1HI​​ represents a breakthrough in epigenetic modulation for opioid withdrawal management, demonstrating dual pharmacological activity as a selective HDAC1/HDAC2 inhibitor with neuroprotective properties.

Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling.

Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis.

KA2507 (KA-2507, KA 2507) is a potent and selective inhibitor of HDAC6 with IC50 of 2.5 nM, >300-fold selectivity over other HDACs.KA2507 demonstrated cellular potency (IC50=150 nM) in a cellular assay measuring induction of acetylated α-tubulin, a marker of HDAC6 inhibition.KA2507 displays antiproliferative effects against a set of 93 human cancer cells with IC50 of 2-30 uM.KA2507 inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model.

Inhibitor of histone deacetylase (HDAC); potently inhibits affinity purified HDAC1. Also inhibits the growth of tumor cells in vitro and in vivo. Induces p21/WAF1 expression in tumor cells.

Tucidinostat (Chidamide, HBI-8000, CS055) is a novel histone deacetylase (HDAC) inhibitor with IC50 of 95/160/67/733/78/432 nM for HDAC1/2/3/8/10/11, respectively; shows no activity against Class IIa HDAC4/4/7/9 and HDAC6; demonstrates significant and broad spectrum in vitro and in vivo antitumor activity, induces G1 arrest, ROS-dependent apoptosis and differentiation in human leukaemia cells.

TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs).

HDAC3 inhibitor PT3 is a novel potent, selective, BBB-permeable HDAC3 inhibitor.PT3 exhibited higher selectivity for HDAC3 over HDAC1, HDAC6, and HDAC8 compared to the reference compound CI994.PT3 upregulated H3K9 acetylation, CREB 1, BDNF, TRKB, Nr4a2, c-fos, PKA, GAP 43 and MMP9 expression in mouse neuronal (N2A) cells.PT3 significantly improved the discrimination index in C57/BL6 mice in the novel object recognition (NOR) model, significant increased in H3K9 acetylation in hippocampus.PT3 upregulated CREB 1, BDNF, TRKB, Nr4a2, c-fos, PKA, GAP 43, PSD 95 and MMP9 expression in mice treated with PT3.

BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.

FT234 (FT-234) is a selective HDAC11 inhibitor.FT234 demonstrated significant reduction in self-renewal stem-like SP cells with 2 uM FT234 or FT895, as well as the formation of vascular networks by SP cells at 5 uM compound treatment.FT234 significantly decreased the mRNA of Sox2 as well as its target genes like HK2 and PDK2 in SPAdh cells.FT234 compound inhibited the growth and viability by 60–80% in both A549 and H1650 cells at 5-10 uM, inhibited the viability of cancer cell lines A549 and H1650 ranged from 4.663–6.594 uM, reduced the viability of chemo-resistant cancer cells as well as chemo-insensitive CSCs.FT234 selectively prevent growth of cancer cells in presence of cancer associated fibroblasts (CAFs).

YSR734 is a first-in-class covalent HDACs inhibitor with IC50 of 0.109 uM, 0.154 uM and 0.143 uM for HDAC1, HDAC2, and HDAC3, sparing other deacetylases (HDAC4-HDAC10, IC50>10 uM).

YSL-109 (YSL109) is a potent, highly selective small molecule inhibitor of HDAC6 with IC50 of 0.537 nM, >4000-fold selectivity over HDAC1 and HDAC8.

Yanostat (KH16) is a novel potent HDAC inhibitor with low nanomolar in vitro activity against class I HDACs (HDAC1/2/3 IC50=13/34/6 nM).

YAK540 is a potent, highly selective class IIa HDAC inhibitor with IC50 of 114 nM (HDAC4), displays excellent selectivity against HDAC2 (265-fold), HDAC6 (100-fold), and HDAC8 (82-fold).

TTA03-107 is a potent, selective HDAC1 inhibitor with Ki of 3.22 and 17.6 nM for HDAC1/2, respectively.