iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) that functions as a potent inhibitor of PARP1 and PARP2. It demonstrates DC50 values for PARP1 and PARP2 degradation at 36 nM and 63 nM, respectively, with IC50 values of 69 nM and 21 nM. The compound contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder, utilizing Thalidomide to recruit CRBN E3 ubiquitin ligase, thereby facilitating effective degradation of PARP2. This innovative mechanism positions iVeliparib-AP6 as a valuable tool for studying PARP-related pathways and therapeutic strategies in cancer research.
iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) that functions as a potent inhibitor of PARP1 and PARP2. It demonstrates DC50 values for PARP1 and PARP2 degradation at 36 nM and 63 nM, respectively, with IC50 values of 69 nM and 21 nM. The compound contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder, utilizing Thalidomide to recruit CRBN E3 ubiquitin ligase, thereby facilitating effective degradation of PARP2. This innovative mechanism positions iVeliparib-AP6 as a valuable tool for studying PARP-related pathways and therapeutic strategies in cancer research.
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