SIRT Inhibitor Screening, Slides of Biology

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SIRT Inhibitor Screening

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.

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.

Benefits of Histone Deacetylase/SIRT Screening Services at Creative BioMart

Screen inhibitors or targets with our wide range panels of HDACs and SIRTs

IC

50

(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

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.

Thank you!

Excerpt from:

https://www.creativebiomart.net/epigenetics/services/

epigenetic-drug-discovery/biochemical-assays/hat-hdac-

screening/histone-deacetylase-sirt-screening/