PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 µM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma[1].
Molecular Weight:
1005.25
Formula:
C55H69FN8O7S
Target:
DNA/RNA Synthesis,PARP,PD-1/PD-L1,PROTACs
Application Notes:
MCE Product type: Reference compound
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