gne-274

GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibility at ER-DNA binding sites, unlike GDC-0927. Acting as a potent inhibitor of the ER-ligand binding domain (LBD), GNE-274 exhibits potential for cancer research purposes.

(R)-GNE-274 是 GNE-274 的一个手性异构体。GNE-274 为 ER 降解剂 GDC-0927 的结构类似物，并且作为一种非降解剂使用。