protac parp1 degrader-4

PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader, demonstrating DC50 values of 180 nM and 240 nM in T47D and MDA-MB-231 cell lines, respectively. It facilitates the ubiquitination and degradation of PARP1 and inhibits its enzymatic activity without causing significant DNA trapping effects. Additionally, PROTAC PARP1 degrader-4 can inhibit tumors with BRCA gene mutations while having minimal impact on the growth of normal cells.

(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that combines the (S,R,S)-AHPC-based VHL ligand with a 4-unit polyethylene glycol (PEG) linker, used in PROteolysis TAgeting Chimera (PROTAC) technology. This compound aids in the formation of vRucaparib-TP4, a potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM[1].

Pomalidomide 4'-PEG3-azide is a chemically synthesized E3 ligase ligand-linker conjugate that incorporates the cereblon ligand derived from Pomalidomide, along with a linker. This compound is utilized in the synthesis of iRucaparib-TP3 (Compound 3), an effective PARP1 degrader developed through the PROTAC strategy and derived from Rucaparib.