iVeliparib-AP6 is a proteolysis-targeting chimera ( PROTAC ) molecule designed based on Veliparib ( HY-10129 ), which targets PARP1/2 . The DC 50 s of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC 50 s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib -based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide ( HY-14658 ) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism. (Pink: PARP-2 and PARP-1 ligand ( HY-10129 ); Blue: Cereblon ligand ( HY-41547 ); Black: linker ( HY-120918 )).
Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Epigenetics | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > PARP
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