PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.IC50 & Target: pKD: 9.02 (EED)
pIC50: 8.17 (PRC2)In Vitro: PROTAC EED degrader-1 (Compound PROTAC 2) binds to EED with a pKD of 9.02±0.09 and inhibits PRC2 function with a pIC50 of 8.17±0.24.
PROTAC EED degrader-1 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422.
PROTAC EED degrader-1 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells.
PROTAC EED degrader-1 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells.