NHEJ Inhibitor SCR7
SCR7 is a potent and
selective inhibitor of non-homologous end joining (NHEJ). It inhibits joining
of DSBs in cell-free DNA repair system, blocks Ligase IV-mediated joining by
interfering with its DNA binding but not that of T4 DNA Ligase or Ligase I, thereby
leading to accumulation of DSBs within the cells, culminating into
cytotoxicity. SCR7 inhibits NHEJ in a Ligase IV-dependent manner within cells,
and activates the intrinsic apoptotic pathway. More importantly, SCR7 impedes
tumor progression in mouse models, and when co-administered with DSB-inducing
therapeutic modalities it enhances their sensitivity significantly. SCR7 to
target NHEJ offers a novel strategy toward the treatment of cancer and
improvement of existing regimens.