NCIt definition : An orally bioavailable inhibitor of DNA-dependent protein kinase (DNA-PK) with potential
antineoplastic activity, and potential sensitizing and enhancing activities for both
chemo- and radiotherapies. Upon administration, peposertib binds to and inhibits the
activity of DNA-PK, thereby interfering with the non-homologous end joining (NHEJ)
process and preventing repair of DNA double strand breaks (DSBs) caused by ionizing
radiation or chemotherapeutic treatment. This increases chemo- and radiotherapy cytotoxicity
and leads to enhanced tumor cell death. The enhanced ability of tumor cells to repair
DSBs plays a major role in the resistance of tumor cells to chemo- and radiotherapy;
DNA-PK plays a key role in the NHEJ pathway and DSB repair.;
UNII : GN429E725A;
InChIKey : MOWXJLUYGFNTAL-DEOSSOPVSA-N;
CAS number : 1637542-33-6;
Molecule name : MSC-2490484A; MSC 2490484A; M-3814; M 3814;