PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pK D of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC 50 =8.17) targeting the EED subunit.
性状
Solid
IC50 & Target[1][2]
VHL
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[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.
溶解度数据
In Vitro: DMSO : 150 mg/mL (142.29 mM; Need ultrasonic)配制储备液