HDAC8 Inhibitor Screening Kit (Fluorometric)

Histone deacetylases (HDACs) represent a large family of enzymes identified as key regulators of nucleosomal histone acetylation, a major event that controls eukaryotic gene transcription and are classified into three groups. They are believed to be involved in important biological activities, such as cell differentiation, proliferation, apoptosis, and senescence. In BioVision’s HDAC-8 Inhibitor screening Kit, HDAC-8 deacetylates the substrate (R-H-K(Ac)-K(Ac)-AFC) followed by an enzymatic cleavage to release the quenched fluorescent group (AFC), which can be detected at Em/Ex = 380/500 nm. In the presence of an HDAC-8 inhibitor, the deacetylation will be impeded which prevents the cleavage of the substrate to release AFC. The kit provides a rapid, simple, sensitive, and reliable test, which is also suitable for high throughput screening of HDAC-8 inhibitors. Trichostatin A is included as a control inhibitor to compare the efficacy of the test inhibitors.

• Detection method: Fluorescence (Em/Ex = 380/500 nm) • Applications: Suitable for high throughput screening of HDAC:8 inhibitors

• Simple procedure; takes ~ 60 min • Fast and convenient • Kit contains the necessary reagents for testing putative HDAC-8 inhibitors

HDAC

none

•HDAC-8 Assay Buffer •HDAC-8 Substrate •HDAC-8 Enzyme •Developer •Trichostatin A (20 µM in DMSO)

-20°C

gel pack

12 months

see datasheet

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Testing candidate HDAC8 inhibitors

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.