PROTAC EED degrader-1 是靶向 EED 的 PROTAC 分子，pKD 为 9.02。PROTAC EED degrader-1 是靶向 EED 亚基的多梳抑制复合物 2 (PRC2) 抑制剂 (pIC50=8.17)。
PROTAC EED degrader-1 is a 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[1].
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[1]. PROTAC EED degrader-1 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1]. PROTAC EED degrader-1 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1].PROTAC EED degrader-1 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells[1].
[1]. Hsu JH, et al. EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex. Cell Chem Biol. 2019 Nov 26. pii: S2451-9456(19)30362-9.
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