GNE-274

GNE-274 is a small molecule, non-degrading partial agonist of the estrogen receptor (ER). Developed by Genentech as a structural analog of the selective estrogen receptor degrader (SERD) GDC-0927, GNE-274 binds potently to the ER ligand-binding domain (LBD) but fails to induce ER protein turnover or degradation. Instead, it functions as a partial agonist in breast cancer cell lines and the uterus, maintaining high ER mobility and increasing chromatin accessibility at ER-DNA binding sites. GNE-274 is primarily utilized as a chemical biology tool compound in cancer research to study the mechanisms of ER antagonism, degradation, and transcriptional activation.

Other names

(S)-3-(3-hydroxyphenyl)-4-methyl-2-(4-((1-propylazetidin-3-yl)methoxy)phenyl)-2H-chromen-6-olCAS 2369048-69-9CAS2369048-69-9CAS-2369048-69-9