PROTAC PARP1 degrader

PROTAC PARP1 degrader is a PROTAC PARP1 degrader. PROTAC PARP1 degrader mediates the interaction between PARP1 and MDM2 E3 ubiquitin ligase, thereby inducing ubiquitination of PARP1 and subsequent proteasome-mediated degradation. PROTAC PARP1 degrader selectively inhibits the growth of breast cancer cells. PROTAC PARP1 degrader induces cell apoptosis by activating caspase-3 and phosphatidylserine externalization. PROTAC PARP1 degrader can be used in the research of triple-negative breast cancer^[1]. IC50 & Target:IC50: 6.12 μM (MDA-MB-231 cell)^[1] In Vitro:PROTAC PARP1 degrader (compound 3) (4-10 μM; 24 h) induces concentration-dependent cleavage of PARP1 in MDA-MB-231 cells, and this effect depends on specific binding to PARP1 and MDM2 as well as proteasome function^[1].
PROTAC PARP1 degrader (10 μM; 24 h) induces apoptosis in MDA-MB-231 cells, which is evidenced by increased phosphatidylserine externalization and production of cleaved caspase-3 after treatment with 10 μM for 24 h^[1].
PROTAC PARP1 degrader (10 μM; 24-48 h) potently inhibits the viability of MDA-MB-231 cells, with an IC₅₀ of 8.45 μM at 24 h and 6.12 μM at 48 h. Its potency in this cell line is 5-fold higher than that of the PARP1 inhibitors niraparib, olaparib and veliparib^[1].
PROTAC PARP1 degrader (100 μM; 48 h) shows high selectivity toward MDA-MB-231 cells; even after treatment at 100 μM for 48 h, it exhibits only extremely low or no cytotoxicity, with no PARP1 degradation, in MCF10A, BEAS-2B, HeLa and HepG2 cells^[1].