​​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.

SP-2-225 is a potent, selective HDAC6 inhibitor, improves antitumor immune responses and prevent tumor relapse after radiotherapy.

SBI-46 (SBI 46) is an antiandrogen-equipped histone deacetylase (HDAC) inhibitor, strongly binds to androgen receptor (AR, IC50=8.4 nM) and potently inhibited HDACs and the proliferation of AR+ CRPC.

RGFP963 (RGFP 963) is a potent, selective class I HDAC inhibitor with IC50 of 1.51 uM, 0.75 and 0.096 uM for HDAC1, HDAC2, and HDAC3, respectively.

Purinostat is a potent, highly selective class I and IIb HDAC inhibitor with IC50 of 0.81, 1.4, 1.7, and 3.8 nM for class I HDAC1, 2, 3, and 8, and 11.5, 1.1 nM for class IIb HDAC 6 and 10, respectively.

PB118 is a potent, selective HDAC6 inhibitor with IC50 of 5.6 nM, shows >1000 times selectively towards HDAC1, reduces alzheimer's disease neuropathology.

NT160 is a high affinity, selective class-IIa histone deacetylase (HDAC) inhibitor with IC50 of 80 nM (HDAC4), 600-fold selectivity over HDAC2 and 27-fold selectivity over HDAC8.

NN-429 (NN429) is a potent, selective second-generation inhibitor of HDAC6 with IC50 of 3.2 nM, >312-fold selectivityt over all HDAC isoforms.

NBM-T-L-BMX-OS01 (BMX, HDAC8 inhibitor) is a potent, selective and BB penetrant HDAC8 inhibitor with IC50 of 831 nM.

Mz325 is a potent, selective, dual inhibitor of Sirt2/HDAC6 with IC50 of 320/43 nM, respectively.

KPZ560 is a potent, HDAC1/2-selective inhibitor with IC50 of 12/68 nM, respectively.

KH-259 is a potent, isozyme-selective and CNS-penetrant HDAC6 inhibitor with IC50 of 260 nM, shows weak activity against HDAC1 and HDAC4 (IC50>6 uM).

HR488B is a potent, selective HDAC1 inhibitor with IC50 of 1.24 uM, effectively inhibits the proliferation of CRC cells.

HO53 is a small moecule inducer of cathelicidin antimicrobial peptide gene (CAMP) expression in bronchial epithelium cells, HO53 is a histone deacetylase (HDAC) inhibitor, interacts directly with HDAC3.

GH8HA01 is a highly potent, selective HDAC8 inhibitor with Ki of 0.67 nM, highly selective against HDAC8 compared to other HDACs.

CM-1758 is a novel histone deacetylase (HDAC) inhibitor with IC50 of 5 nM and 126 nM for HDAC1 and HDAC6, respectively.