Remodelin is an inhibitor of acetyl-transferase NAT10.

R306465, also known as JNJ-16241199, is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models.

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.

Pracinostat(SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6; has no activity against the class III isoenzyme SIRT I.

Panobinostat(LBH-589) is a broad-spectrum HDAC inhibitor; low nanomolar concentrations (IC50=5-20 nM) of LBH589 induced cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation in MOLT-4 and Reh cell.

Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.

MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively.

MC1568 is a class II (IIa) HDAC inhibitor selective for HDAC4 and HDAC6

LMK-235 is a selective histone deacetylase (HDAC) 4 and HDAC5 inhibitor (IC50 values are 4.22, 11.9, 55.7, 320, 852, 881, and 1278 nM for HDAC 5, 4, 6, 1, 11, 2, and 8, respectively).

HPOB is a novel selective inhibitor of HDAC6 catalytic activity in vivo and in vitro.

GSK3117391 (CHR5154) is a HDAC inhibitor.

Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM. Phase 1/2.

Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10. Phase 1/2.

Droxinostat is a selective HDAC3, HDAC6 and HDAC8 inhibitor.

CUDC-907 (PI3K/HDAC Inhibitor I) is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.

Dacinostat (NVP-LAQ824, LAQ824) is a highly potent HDAC inhibitor with IC50 of 32 nM.

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.

CI994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM.

Chidamide is a class I HDAC inhibitor with IC50s of 95/160/67/733 nM for HDAC1/2/3/8; also inhibits HDAC10/11(IC50=78/432 nM); no inhibition on HDAC4/5/7/9/6(IC50>30 uM).

CAY10683 is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.

CAY10603 is a potent and selective inhibitor of HDAC6 with IC50 of 2 pM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively.

BML-210 is the novel HDAC inhibitor, and its mechanism of action has not been characterized.

Belinostat (PXD101) is a novel pan-HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors.

CRA-026440 hydrochloride is a potent, broad-spectrum HDAC (HDAC) inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities.

SAHA-OH is a selective HDAC6 inhibitor (IC50=23 nM), shows a 10- to 47-fold selectivity for HDAC6 compared to HDAC 1, 2, 3, and 8. SAHA-OH shows anti-inflammatory activity, and attenuates macrophage apoptosis.

DKFZ-748 is a selective HDAC10 inhibitor (pIC50=7.66), and shows anti-tumor activity.

Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia.

TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity.

HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM. HC-Toxin induces tumor cell apoptosis and has anticancer effects.

PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM.