1 Result for "

ERα L539D mutant

" in MedChemExpress (MCE) Product Catalog:
Products (1)

1 Results for "ERα L539D mutant" in MCE Product Catalog:

Cat. No.: HY-141551
CAS No.: 2369048-69-9
Purity:  98.00%
Target:  

Estrogen Receptor/ERR

Research Areas:  

Cancer

GNE-274 is a non-degrading estrogen receptor α (ERα/ESR1) modulator structurally similar to GDC-0927 (HY-111484). GNE-274 competes for binding to the ligand-binding domain of ERα and induces a coregulator-binding conformation similar to that of antagonists, yet retains partial agonistic transcriptional activity and does not promote ERα turnover. GNE-274 effectively inhibits E2-stimulated proliferation of ER-positive, HER2-negative breast cancer cells. GNE-274 promotes the recruitment of ERα to the nucleus and chromatin, increases chromatin accessibility, while largely maintaining the intranuclear mobility of ERα. GNE-274 can be used in research on ER-positive breast cancer and ERα transcriptional dynamics .
loading...
    loading...