hdac-8

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1 2 3 6 7 11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

HDAC8-IN-20a (HDAC8 inhibitor-20a) is a potent and selective HDAC8 inhibitor with an IC50 of 27 nM. HDAC8-IN-20a blocks activation of growth receptor survival signals.

Quisinostat (JNJ-26481585) (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, 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.

HDAC-IN-7, an analogue of Tucidinostat (Chidamide), is a HDAC inhibitor. HDAC-IN-7 inhibits acetylation of histone protein H3 and induces apoptosis in human colon cancer cell lines[1].

Ricolinostat (Rocilinostat) is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity.

Tubastatin A Hydrochloride (TSA HCl) is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (>1000-fold) against all other isozymes except HDAC8 (>57-fold).

Droxinostat (NS 41080) is a selective HDAC inhibitor, primarily targeting HDACs 6 and 8 with IC50 values of 2.47 μM and 1.46 μM, respectively. It is over 8-fold more selective against HDAC3 and shows no inhibition for HDAC1, 2, 4, 5, 7, 9, and 10.

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

PCI-34051 is an effective and selective HDAC8 inhibitor (IC50: 10 nM).

Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.

CRA-026440(PCI-34051) is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.

ACY-241, also known as Citarinostat (ACY241), is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis.

BRD73954, an effective and specific HDAC inhibitor, which is with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs.

ACY-957 (HDAC Inhibitor C001) is an orally active and selective inhibitor of HDAC1 and HDAC2 (IC50s: 7 nM, 18 nM, and 1300 nM against HDAC1 2 3) and shows no inhibition on HDAC4 5 6 7 8 9.

CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor. CRA-026440 hydrochloride exhibits 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 exhibits antitumor and antiangiogenic activities.

MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.

UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively.

Nanatinostat is an effective and class I selective inhibitor of histone deacetylase (IC50: 8 nM).

Tubulin HDAC-IN-3 (compound 12a) is a potent dual inhibitor of tubulin polymerization and HDAC1 8, with IC50 values of 5.4 μM for tubulin polymerization, and 0.155 and 0.177 μM for HDAC1 and HDAC8, respectively. It obstructs the cell cycle, triggers apoptosis, and suppresses colony formation [1].

HDAC-IN-38 is a potent inhibitor of HDAC. HDAC-IN-38 has similar micromolar inhibitory effects on HDAC1, 2, 3, 5, 6 and 8, and also increases histone acetylation levels (H3K14 or H4K5). HDAC-IN-38 increases cerebral blood flow (CBF), reduces cognitive impairment and improves hippocampal atrophy.

Pimelic diphenylamide 106 (RGFA-8) is a slow, tight-binding inhibitor of class I HDAC (with IC50 values of 150 nM , 760 nM and 370 nM for HDAC 1, 2, and 3, respectively), showing no activity against class II HDACs.

Givinostat (ITF-2357) is an HDAC inhibitor with IC50 values of 198 nM for HDAC1 and 157 nM for HDAC3.