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CAS No. | 902128-92-1 | Cat. No. | BCP46932 |
Name | E7016 | ||
Synonyms | E-7016; E 7016; GPI21016; GPI 21016; GPI-21016; | ||
SMILES | C1CN(CCC1O)CC2=CC3=C(C=C2)OC4=CC=CC5=C4C3=NNC5=O | ||
Chemical Name | |||
Formula | C20H19N3O3 | M. Wt | 349.38 |
Purity | 98% | Storage | Store at 4-8°C |
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. |
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