Histone Deacetylase (HDAC) Inhibitor Set II

General Description

A convenient set of seven individual HDAC (Histone Deacetylase) inhibitors.

• CI-994

• Panobinostat (LBH589)

• SAHA

• SBHA

• Scriptaid

• Trichostatin A

• Tubacin

Biochem/physiol Actions

CI-994 - Cell-permeable. A histone deacetylase (HDAC) inhibitor: Ki values are 0.41, 0.75, >100 and >100 μM for HDAC1, HDAC3, HDAC6 and HDAC8, respectively. Displays significant antitumor activity in vitro and in vivo against a broad spectrum of murine and human tumor models.Panobinostat (LBH589) - Highly potent inhibitor of both histone deacetylase 1 (HDAC1) activity and tumour cell proliferation in vitro. The IC50 values of HDAC isozymes HDAC1-IP Ac-H4, HDAC8, MALunselective, B61HDAC1 and B12HDAC6 are 0.23±0.06, 283±29, 75±4, 47±5 and 89±12 nM, respectively. And to A2780 proliferation, IC50 value is 4.6±1.8 nM.SAHA - Potent, reversible inhibitor of histone deacetylase 1 (HDAC1) and 3 (HDAC3). Induces cell growth arrest at both G1 and G2 phases. Induces apoptosis.SBHA - Competitive histone deacetylase (HDAC) inhibitor that has been shown to inhibit HDAC1 (IC50 = 0.25 μM) and HDAC3 (IC50 = 0.30 μM). SBHA causes cell differentiation, cell cycle arrest, or apoptosis. SBHA also enhances cytotoxicity induced by Oxaliplatin in the colorectal cancer cell lines.Scriptaid - A relatively non-toxic Inhibitor of histone deacetylase (HDAC). Facilitates transcriptional activation (TGF-?/Smad4) in both stable and transient receptor assays in a concentration-dependent manner. At ~2 μg/ml (6-8 μM) concentrations, results in a greater than 100-fold increase in histone acetylation in PANC-1 cells.Trichostatin A - Potent, reversible inhibitor of histone deacetylase. Mediates the activation of O6-methylguanine-DNA methyltransferase (MGMT). May be involved in cell cycle progression of several cell types, induces cell growth arrest at both G1 and G2/M phases. In some cases induces apoptosis.Tubacin - Tubacin (Tubulin acetylation inducer) is a highly potent, selective, reversible, and cell-permeable inhibitor of histone deacetylase 6 (HDAC6, IC50 = 4 nM). Displays 1000-fold more selectivity for HDAC6 over other HDACs. It inhibits α-tubulin deacetylation in mammalian cells. Unlike trichostatin A (TSA), which is a broad spectrum HDAC inhibitor, tubacin is specific for the tubulin deacetylase activity of HDAC6. Tubacin causes increased acetylation of α-tubulin, accumulation of polyubiquitinated proteins, and apoptosis. It does not affect global histone deacetylation, gene-expression profiling, or cell cycle progression mediated α-tubulin deacetylation in mammalian cells.