E7016

  • Chemical Properties
CAS No. 902128-92-1 Cat. No. BCP46932
Name E7016
Synonyms E-7016; E 7016; GPI21016; GPI 21016; GPI-21016;
Formula C20H19N3O3 M. Wt 349.38
  • Biological Activity
Description E7016, also known as GPI21016, is an inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with potential chemo- and/or radiosensitizing activity. PARP inhibitor E7016 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks and promotes genomic instability and eventually leads to apoptosis. In addition, this agent may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and is activated by single-strand DNA breaks.
Pathways Cell Cycle/DNA Damage Epigenetics 
Targets PARP 

Structure

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