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HDAC Targeted Libraries

GPCR focused librariesClassical histone deacetylases (HDACs classes I, II, and IV) are a promising novel class of epigenetic anti-cancer drug targets. Inhibition of histone deacetylases results in hyperacetylation of histones and modulates gene expression by creating an open chromatin state that leads to expression of previously silenced genes.

 
Although the mechanism of action is not fully understood, inhibiting HDACs has been observed to result in cell cycle arrest and apoptosis of cancer cells. First HDAC inhibitors have been evaluated in clinical trials and show activity against several cancer diseases. The majority of HDAC inhibitors in and out of clinical trials inhibit all HDAC isoforms nonspecifically (so called pan-inhibitors). Efforts to create selective HDAC inhibitors have seen increased attention over the past several years, leading to several class-selective and some isoform-selective inhibitors.
 
We offer two receptor-based HDAC Targeted Libraries which are specifically targeted towards class I and class II HDAC isoforms in such a way to minimize cross-reactivity between these two classes.
 
  • HDAC Class I Focused Library - 599 compounds
  • HDAC Class II Focused Library - 204 compounds
 
The selective targeting has been achieved by inspection of HDAC active site’s critical structural determinants for ligand recognition (including essential interaction with Zn2+), docking validation of reference set of about 1,000 known HDAC inhibitors with the IC50 at least 1.1 uM and exclusion of predicted cross-binders from the final set of compounds. Each compound in the library contains a metal-binding moiety that coordinates to the catalytic metal atom (Zn2+) within the HDAC active site.
 
The library comprises drug-like compounds only.

 

 

All the compounds are in stock, cherry-picking is available.

 

The libraries (DB, SD, XLS, PDF format) as well as the price-list are available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain this library or if you need more information.

 


 

 

 

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