E7016
| CAS号 | 902128-92-1 | 货号 | BCP46932 |
| 中文名 | E7016 | ||
| 英文名 | E7016 | ||
| 中文别名 | |||
| 英文别名 | E-7016; E 7016; GPI21016; GPI 21016; GPI-21016; | ||
| 分子式 | C20H19N3O3 | 分子量 | 349.38 |
| 生物活性 | 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. | ||
| 信号通路 | Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | PARP | ||
结构式
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