-
Description
High-throughput compatible, quick and easy screening for HDAC6 ligands; Includes human recombinant HDAC6
-
Summary
• Detection method - Fluorescence (Ex/Em 380/490 nm) • Species reactivity - Human • Applications - • Screening of drugs and novel ligands for interaction with human recombinant HDAC6
-
Detection Method
Fluorescence (Ex/Em 380/490 nm)
-
Species Reactivity
Human
-
Applications
• Rapid, high-throughput screening of drugs and novel ligands. • Development of structure-activity relationship (SAR) models to predict HDAC6 interaction liability of novel compounds.
-
Sample Type
Samples containing drugs, inhibitors or ligands (compounds that can interact and affect HDAC6 activity)
-
Features Benefits
• Simple, highly sensitive, high-throughput compatible • Rapid screening of HDAC6 inhibitors • Kit includes Tubacin, an HDAC6 inhibitor, and a stable, recombinant human HDAC6
-
Storage Conditions
-80°C
-
Shipping Conditions
dry ice
-
Shelf life
12 months
-
Background
Histone Deacetylase 6 (HDAC6, EC 3.5.1.98), is a class IIb HDAC enzyme that deacetylates an ε-N-acetyl lysine of histone and non-histone protein substrates. It is a unique member of HDAC family as it contains two deacetylase domains that are proposed to function independently of each other. HDAC6 can shuttle between the nucleus and cytoplasm, suggesting potential extra-nuclear functions by regulating the acetylation status of non-histone substrates. HDAC6 also affects transcription and translation by regulating the heat-shock protein 90 (Hsp90) and stress granules. Elevated HDAC6 activity is associated with cell motility and catalyzes increases α-tubulin deacetylation, thus influencing cancer cell metastasis. In addition, mutations in HDAC6 gene have been associated with Alzheimer's disease. HDAC6-selective inhibitors are considered as promising targets against autoimmune, inflammatory and oncology diseases such as breast and ovarian cancer. BioVision’s HDAC6 Inhibitor Screening Kit utilizes deacetylase activity of HDAC6 towards a synthetic acetylated-peptide substrate resulting in the release of an AFC fluorophore, which can be easily quantified using a conventional microplate reader. In the presence of an HDAC6-selective inhibitor (Tubacin), the deacetylase activity of HDAC6 is reduced/abolished resulting in decrease or total loss of the fluorescence. This simple and high-throughput adaptable assay kit can be used to screen/study/characterize potential inhibitors of HDAC6.
-
-
Additional description
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.
