PROTAC EED degrader-2

PROTAC EED degrader-2 is a von Hippel-Lindau -based PROTAC targeting EED with a pK D of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 ( PRC2 ) inhibitor ( pIC 50 =8.11) targeting the EED subunit In Vitro PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pK D of 9.27±0.05 and inhibits PRC2 function with a pIC 50 of 8.11±0.09. PROTAC EED degrader-2 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422. PROTAC EED degrader-2 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells. PROTAC EED degrader-2 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Karpas422 cells Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: 4, 8, 12, 14 days Result: Reduced proliferation. GI 50 =0.057 μM (Day 14). Western Blot AnalysisCell 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 AnalysisCell 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. Form:Solid IC50& Target:VHL

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