HDAC Inhibitor Screening

1. HDAC Inhibitor Screening

2. Histone deacetylases (HDACs) are enzymes removing acetyl groups from lysine residues on histone tails, restoring the positive charge of the histone tail lysine residue. HDACs are involved in important biological procedures, including cell differentiation, proliferation, apoptosis, and senescence. Site-specific histone deacetylation could result in a more tightly compacted, heterochromatin conformation, thus repressing eukaryotic gene transcription. Class I, II, and IV belong to the classic HDAC enzymes, whereas class III comprises sirtuin (SIRT) enzymes that require the cofactor NAD+ for their activity. Aberrant HDAC enzyme expression is observed in various diseases and therefore HDAC has been proved to be novel epigenetic targets for the treatment of cancer. It has become one of the most important research fields to find small molecules that function as HDAC enzyme inhibitors with promising anti-tumor efficacy in vitro and in vivo, especially during the coming area of epigenetics. Quite a few HDAC inhibitors have come into the market as anti-cancer drugs, and dozens more are in the process of clinical trials.

3. Intelligent screening workflows that combine different assay formats and multiplex various readouts at Creative BioMart allow efficient screening of large compound libraries to provide a holistic view of compound effects. A comprehensive series of HDACs screening and profiling assays could be performed, including HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9, HDAC10, HDAC11, SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, SIRT7, and so on. All HDAC assays are fluorescent based and a detailed report is attached to each order. Most of our HDACs and SIRTs are produced in house and are also available for purchase. Moreover, substrates, assay kits, and inhibitors/activators for HDAC screening and profiling services are also accessible to give researchers the tools necessary to deepen the understanding of this important target. Procedure of Histone Deacetylase/SIRT Screening at Creative BioMart HDAC/SIRT assay method at Creative BioMart precludes radioactivity, extraction, and chromatography aspects of other assays. There only needs two simple steps on a microtiter plate to evaluate HDAC activity. An HDAC fluorometric substrate is first incubated with purified HDAC enzyme. Subsequently, the deacetylation catalyzed by HDAC make the resulting product become sensitive to subsequent treatment with the developer, releasing a fluorophore that can be easily measured on a fluorescence reader.

4. Benefits of Histone Deacetylase/SIRT Screening Services at Creative BioMart • Screen inhibitors or targets with our wide range panels of HDACs and SIRTs • IC50 (half maximal inhibitory concentration) determination and single point concentration determination • Get project guidance in a time-efficient manner • Available for profiling and low cost high-throughput screening • High sensitivity and reproducibility • Fast turnaround time

5. Creative BioMart offers unbeatable services in HDAC screening with the most competitive price and is dedicating to identifying your inhibitors or activators against HDACs targets with the great chance to success. Our highly professional team in state-of-the-art labs will customize the most adequate assay campaign to ensure your project advances quickly and promise a successful progression in epigenetic drug research with high quality, reliability and efficiency. If you have any special requirements in HDACs or SIRTs assay services, please feel free to contact us. Reference1. Wu, D. F.; et al. Screening of selective histone deacetylase inhibitors by proteochemometric modeling. BMC Bioinformatics. 2012, 13: e212.

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