Histone Deacetylase (HDAC) Inhibitor Set I

General Description

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

• Apicidin

• M344

• Sodium 4-phenylbutuyrate

• Splitomycin

• Trichostatin A

• Valproic Acid, Sodium Salt

Biochem/physiol Actions

Apicidin - A potent, cell permeable inhibitor of histone deacetylase (IC50 = 700 pM for parasitic histone deacetylase). Inhibits HeLa cell proliferation (IC50 = 50-100 nM) and induces the transcriptional activation of p21 (WAF1) in a reversible manner. Also prevents H-ras-induced invasive phenotype of MCF-10A cells possibly by down regulating MMP-2 in a reversible manner. M344 - An amide analog of Trichostatin A that potently Inhibits histone deacetylases (IC50 = 40 nM for rat liver HDAC and IC50 = 100 nM for maize HDAC). Induces differentiation and inhibits proliferation (~2 μM) of murine erythroleukemia cells. Sodium 4-phenylbutuyrate - Inhibitor of histone deacetylase (HDAC). Anti-neoplastic agent and transcriptional regulator. Also acts as an inducer of tumor cytostasis and differentiation.Splitomycin - Potent inhibitor of yeast NAD+ dependent histone deacetylase Sir2p (IC50= 60 μM). Sensitizes mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. Acts by either altering or blocking access to the acetylated histone binding pocket.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.Valproic acid sodium salt - A cell-permeable histone deacetylase 1 (HDAC1) inhibitor (IC50 = 400 μM) that exhibits anticancer, anti-inflammatory and neuroprotective properties. Recently it has been reported that Valproic acid enables reprogramming of primary human fibroblasts with only two factors, Oct4 and Sox2, without the need for the oncogenes c-Myc or Klf4.