HDAC Inhibitor Drug Screening Kit (Fluorometric)

Inhibition of histone deacetylase (HDAC) has been implicated to modulate transcription and to induce apoptosis or differentiation in cancer cells. However, screening of compounds for HDAC inhibition has been difficult due to the lack of convenient tools for analyzing HDAC activity. The new HDAC Inhibitor Drug Screening Kit provides a fast, fluorescence-based method that eliminates radioactivity, extractions, or chromatography, as used in traditional assays. The new procedure requires only two easy steps, both performed on the same microtiter plate. First, your inhibitor candidates are mixed with HeLa Nuclear Extract and HDAC fluorometric substrate, which comprises an acetylated lysine side chain. Deacetylation of the substrate sensitizes the substrate, so that, in the second step, treatment with the Lysine Developer produces a fluorophore. The fluorophore can be easily analyzed using a fluorescence plate reader or a fluorometer. The assay is well suited for high throughput screening applications.

• Detection method: Fluorescence (Ex/Em 350:380/440:460 nm) • Species reactivity: Mammalian • Applications: Screening of compounds for HDAC inhibition by analyzing HDAC activity

• Simple two-step procedure • Fast fluorescence-based method that eliminates radioactivity, extractions, or chromatography • The assay is well suited for high throughput screening applications.

HDAC

none

• HDAC Substrate [Boc-Lys(Ac)-AMC, 4 mM] • 10X HDAC Assay Buffer • Lysine Developer • HDAC Inhibitor (Trichostatin A, 1 mM) • HeLa Nuclear Extract (5 mg/ml)

-20°C

gel pack

12 months

see datasheet

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Cell and tissue lysates, culture media, urine, plasma and serum, as well as many other biological fluids

Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.