| In Vitro |
PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pKD of 9.27±0.05 and inhibits PRC2 function with a pIC50 of 8.11±0.09[1]. PROTAC EED degrader-2 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1]. PROTAC EED degrader-2 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1]. PROTAC EED degrader-2 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells[1]. Cell Proliferation Assay[1] Cell Line: Karpas422 cells Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: 4, 8, 12, 14 days Result: Reduced proliferation. GI50=0.057 μM (Day 14). Western Blot Analysis[1] Cell Line: Karpas422 cells Concentration: 0.1, 1, and 3 μM Incubation Time: 48 hours Result: The protein levels of EED, EZH2, H3K27me3 was reduced. Western Blot Analysis[1] Cell Line: Karpas422 cells Concentration: 1 μM Incubation Time: 1, 2, 4, 6, 8, 24 hours Result: EED protein levels decreased within 1-2 h of treatment.
|
