Biochem/physiol Actions

CI-994 - Cell-permeable. A histone deacetylase (HDAC) inhibitor: K_i 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-ß/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.

General description

A convenient set of seven individual HDAC (Histone Deacetylase) inhibitors. CI-994 CAS Number: 112522-64-2 Molecular Formula: C₁₅H₁₅N₃O₂ Molecular Weight: 269.3 Panobinostat (LBH589) CAS Number: 404950-80-7 Molecular Formula: C₂₁H₂₃N₃O₂ Molecular Weight: 349.43 SAHA CAS Number: 149647-78-9 Molecular Formula: C₁₄H₂₀N₂O₃ Molecular Weight: 264.3 SBHA CAS Number: 38937-66-5 Molecular Formula: C₈H₁₆N₂O₄ Molecular Weight: 204.22 Scriptaid CAS Number: 287383-59-9 Molecular Formula: C₁₈H₁₈N₂O₄ Molecular Weight: 326.35 Trichostatin A CAS Number: 58880-19-6 Molecular Formula: C₁₇H₂₂N₂O₃ Molecular Weight: 302.4 Tubacin CAS Number: 537049-40-4 Molecular Formula: C₄₁H₄₃N₃O₇S Molecular Weight: 721.86