rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader . ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
References:
[1]. Zhao Q, et al. Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule. Chem Commun (Camb). 2019 Jan 2;55(3):369-372.