hdac5

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

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.

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.

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 selective, brain-penetrating HDAC6 inhibitor (IC50: 3 nM) that effectively reverses chemotherapy-induced peripheral neuropathy.

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

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.

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

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.

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.

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.

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.

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

Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by hindering HDAC6 activity, with an IC50 value of 63 nM for HDAC6. It exhibits superior selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat effectively reduces the expression of fibrosis markers, fibronectin and collagen 1, in fibroblasts. It shows no toxicity in rat perfused heart and zebrafish larvae studies. Fibrostat holds promise for research on fibrosis-related diseases.

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.

Ebselen oxide (EB-2), a novel variant of HER2 inhibitor for HER2-positive cancers, is an EB-1 analog with antibacterial and antifungal activity, and has shown cytoprotective effects in vitro in addition to cytoprotective effects against HN2.Ebselen oxide inhibits alginate production by Pseudomonas aeruginosa and inhibits HDAC1, HDAC3, HDAC3, and HDAC3. Ebselen oxide inhibits alginate production by Pseudomonas aeruginosa, inhibits HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9, and can be used in the study of fungal infections.