HDAC (Histone Deacetylase) histone deacetylase activity determination and drug screening program

Histone deacetylase (HDAC) is a type of protease, which plays an important role in the modification of chromosome structure and the regulation of gene expression. In general, acetylation of histones is conducive to the dissociation of DNA and histone octamers, and the structure of nucleosomes is relaxed, so that various transcription factors and cooperative transcription factors can specifically bind to DNA binding sites and activate genes. Of transcription. In the nucleus, the process of histone acetylation and histone deacetylation is in a dynamic balance and is transferred by histone acetylation The enzyme (histone acetyltransferase, HAT) and histone deacetylase (HDAC) are jointly regulated. HAT transfers the acetyl group of acetyl-CoA to a specific lysine residue at the amino terminus of histones. HDAC deacetylates histones, tightly binds to negatively charged DNA, densely curls chromatin, and inhibits gene transcription .

In cancer cells, the overexpression of HDAC leads to the enhancement of acetylation. By restoring the positive charge of histone, thereby increasing the attraction between DNA and histone, the relaxed nucleosome becomes very compact, which is not conducive to the specific gene Expression, including some tumor suppressor genes. Histone deacetylase inhibitors (HDACi) can increase the acetylation of histones in specific regions of chromatin, thereby regulating the expression and stability of apoptosis-related and differentiation-related proteins, and inducing apoptosis and differentiation. Become a new class of anti-tumor drugs. HDACi not only has a good therapeutic effect on various hematological tumors and solid tumors, but also has the advantages of relatively high selectivity and low toxicity of tumor cells. Several HDACi have entered clinical trials. However, due to the lack of convenient tools for analyzing HDAC activity, it is difficult to screen HDACi complexes. Imagine recommends to you the full range of HDAC (Histone Deacetylase) histone deacetylase activity determination and drug screening programs of the famous American brand BioVison:

Chinese and English brand name article number specification details HDAC histone deacetylase activity fluorescence analysis kit-HDAC Fluorometric Assay Kit Biovision K330-100 100 analysis details HDAC histone deacetylase activity colorimetric analysis kit-HDAC Colorimetric Assay Kit Biovision K331-100 100 analysis details HDAC Histone Deacetylase Inhibitor Drug Screening Kit-HDAC Inhibitor Drug Screening Kit Biovision K340-100 100 analysis details

Among them, the recommended HDAC histone deacetylase activity fluorescence analysis kit-HDAC Fluorometric Assay Kit (Cat. No. K330-100) and HDAC histone deacetylase activity colorimetric analysis kit-HDAC Colorimetric Assay Kit (HDAC Colorimetric Assay Kit) K331-100) is mainly used to detect the activity of HDAC in biological sample solutions such as crude extracts of mammalian tissue cells, cell culture supernatant, urine, plasma, serum, purified protein solution, etc. The former uses the fluorescence method, the latter The author uses the substrate color method. The fluorophore or chromophore-labeled substrates are provided in the kit, respectively, and are activated after deacetylation by the HDAC enzyme in the sample. Subsequently, the lysine imaging agent produces a fluorophore or luminophore. The final luminophore can be read and analyzed by ELISA plate reader or microplate reader, and the fluorophore can be analyzed by fluorescence plate reader or fluorometer. The kit also provides Hela Nuclear Extract (HeLa Nuclear Extract) as a positive control, and Trichostatin A as a negative control. This analysis is very suitable for high-throughput screening.

The HDACi (Histone Deacetylase Inhibitor) Drug Screening Kit-HDAC Inhibitor Drug Screening Kit (K340-100) uses a similar principle to the HDAC Fluorometric Assay Kit (Cat. No. K330-100), which is provided in the kit Hela cell nuclear extract is used as a routine detection environment. By adding a sample to be tested and labeling the substrate with a fluorophore, the content of the HDAC inhibitor in the sample to be tested is analyzed by measuring the enzyme activity of HDAC. The HDAC activity inhibitor drug screening kit can be used for screening of HDAC inhibitor drugs in biological sample solutions such as crude extracts of mammalian tissue cells, cell culture supernatant, urine, plasma, serum, purified protein solution, etc., which is very suitable for use For high-throughput drug screening.

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