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An Advanced Tool To Interrogate BRD9.

Rezaul M Karim1,2, Ernst Schönbrunn1,2

  • 1Drug Discovery Department, Moffitt Cancer Center , Tampa, Florida 33612, United States.

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|April 28, 2016
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Summary
This summary is machine-generated.

Selective inhibitors of bromodomain-containing protein 9 (BRD9) show therapeutic promise for cancer and inflammatory diseases. BI-9564 is a new tool compound for studying BRD9

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Bromodomain-containing protein 9 (BRD9) is implicated in human malignancies and inflammatory diseases.
  • Targeting BRD9 offers potential therapeutic strategies.
  • A well-characterized small molecule inhibitor is needed to investigate BRD9's biological functions and therapeutic utility.

Purpose of the Study:

  • To develop and characterize a selective small molecule inhibitor of BRD9.
  • To provide a tool compound for exploring BRD9 biology in disease contexts.
  • To assess the potential of BRD9 as a drug target.

Main Methods:

  • Synthesis and characterization of BI-9564.
  • Assessment of cell permeability and cytotoxicity.
  • Evaluation of BRD9 inhibitory activity (details not provided in abstract).

Main Results:

  • BI-9564 was synthesized and identified as a selective BRD9 inhibitor.
  • The compound is cell-permeable and noncytotoxic.
  • BI-9564 is suitable for in vitro and potentially in vivo studies.

Conclusions:

  • BI-9564 serves as a valuable chemical probe for the scientific community.
  • This inhibitor facilitates further research into BRD9's role in disease.
  • BI-9564 supports the investigation of BRD9 as a viable drug target.