EED PROTAC
Molecular Target
EED (Embryonic Ectoderm Development)
E3 Ligase
von Hippel-Lindau (VHL) and Cereblon (CRBN)
Biological Role
EED, SUZ12, and EZH2 form the core essential subunits of the PRC2 complex that regulate gene expression through the methylation of H3K27.
Brief Description
Activity
EED PROTACs can potently inhibit proliferation of an EZH2 mutant DLBCL cell line (Karpas422 AZ14117230 0.057μM GI50, AZ14118579 0.045μM GI50), and an EZH2 WT rhabdoid cancer cell line in vitro, and induce degradation of EED and its associated proteins EZH2 and SUZ12 in the PRC2 complex using the EED-targeted VHL PROTACs. Global proteomics analysis suggests that AZ14117230 is highly selective against EED, EZH2 and SUZ12.
| AZ14117230 | AZ14118579 | |
| MTase Glo (pIC50) | 8.1 | 8.2 |
| SPR(pKd) | 9.3 | 9.0 |