hdac5

SS-208 is a selective inhibitor of HDAC6 (IC50 = 12 nM) with anti-tumor activity. SS-208 shows selectivity over other HDAC subtypes.

BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitor of HDAC5 and HDAC9 with IC50 values of 0.85 μM and 1.88 μM, respectively.

BRD 4354 is an inhibitor of HDAC5 and HDAC9. For HDAC5 and HDAC9, the IC50s values are 0.85 and 1.88 μM, respectively.

CHDI-390576 is a CNS-permeable, selective and potent dibenzoyl isohydroxamic acid class IIa histone deacetylase (HDAC) inhibitor that inhibits class IIa HDAC 4, HDAC 5, HDAC 7, HDAC 9, and can be used in cancer research.

SW-100 is a selective histone deacetylase 6 inhibitor (IC50: 2.3 nM). It also shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays an obviously improved ability to cross the blood-brain-barrier.

TMP269 is an effective, specific class IIa HDAC inhibitor for HDAC4 (IC50: 157 nM), HDAC5 (IC50: 97 nM), HDAC7 (IC50: 43 nM), and HDAC9 (IC50: 23 nM), respectively.

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.

TMP195 (TFMO 2) is a selective class IIa histone deacetylase (HDAC) inhibitor.

Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor targeting HDAC1/2/3 with IC50 values of 1.20/1.12/0.57 μM, respectively, and also inhibits Lysine-specific demethylase 1 (LSD1).

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.

LMK-235 is a potent HDAC inhibitor, and is used in cancer research.

Givinostat hydrochloride (ITF2357 hydrochloride) is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.

Domatinostat (4SC202) 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.

ACY-1083 is a small molecule inhibitor, a highly selective HDAC6 inhibitor (IC50=3 nM), with 260-fold higher selectivity over other classes of HDAC isoforms. It is brain-penetrant and used for research on chemotherapy-induced peripheral neuropathy.

BRD 9757 (N-Hydroxy-1-cyclopentene-1-carboxamide) is a selective inhibitor of HDAC6 (IC50 = 30 nM).

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.

CHDI 00484077 is a highly selective, central nervous system (CNS) permeable Class IIa HDAC inhibitor with inhibitory effects on HDAC4, HDAC5, HDAC7, and HDAC9, which improves neuronal function, and can be used to study Huntington's disease.

Nanatinostat (CHR-3996) is an HDAC inhibitor with selectivity and oral bioavailability, with IC50 values of 3-7 nM for HDAC1/2/3 and >200 nM for other subtypes. Nanatinostat also inhibits tumour cell proliferation and induces apoptosis, for studying neurodegenerative diseases and cancer.

Nexturastat A is an effective and specific HDAC6 inhibitor (IC50: 5 nM). Its selectivity is >190-fold than other HDACs.

Fimepinostat (CUDC 907) is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan-histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types.

XSJ-10 is an HDAC inhibitor containing a RAS/RAF protein interference unit, with IC50 values of 0.05 μM in PANC-1 cells and 0.04 μM in HT-29 cells. It effectively induces cancer cell apoptosis and tumor inhibition by strongly suppressing the RAS-RAF-MEK-ERK signaling pathway and HDAC3 acetylation levels.

CM-444 is an inhibitor of HDAC (IC50 ranging from 6 nM to 0.6 μM) and DNA methyltransferase (DNMT, IC50 ranging from 1.8 to 2.3 μM). This compound induces differentiation in acute myeloid leukemia cells, exhibits anti-leukemia activity, and enhances survival rates in mouse models.

ZG-126 is an agonist of the vitamin D receptor (VDR) and an inhibitor of histone deacetylase (HDAC) with an IC50 range of 0.63-67.6 μM. It demonstrates cytotoxicity in cancer cell lines MDA-MB-231 and 4T1. In mouse models, ZG-126 exhibits antitumor and antimetastatic effects against melanoma and triple-negative breast cancer (TNBC). Additionally, it shows anti-inflammatory activity by reducing macrophage infiltration and polarization to the immunosuppressive M2 subtype.