E7016

E7016 (also known as GPI-21016) is an orally available small molecule inhibitor of poly(ADP-ribose) polymerase (PARP), a nuclear enzyme involved in DNA repair. By selectively binding to PARP and inhibiting its activity, E7016 prevents the repair of single-strand DNA breaks via the base-excision repair pathway. This leads to accumulation of DNA damage, genomic instability, and ultimately apoptosis in tumor cells. E7016 has demonstrated potential as a chemo- and radiosensitizer by enhancing the cytotoxicity of DNA-damaging agents such as temozolomide and radiation therapy. Preclinical studies have shown that it can increase tumor cell radiosensitivity both *in vitro* and *in vivo*, with particular interest for use in glioblastoma multiforme treatment[1][2][3][4][5][7].

Other names

902128-92-1UNII-M8926C7ILXUNII-M-8926C7ILXUNII-M 8926C7ILX