GNE-274 (C09-1135-108)

GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research.In VitroGNE-274 (0.1 nM-1000 nM; 4 hours) fails to trigger increased ER turnover in MCF7, MD-134, HCC1500 and CAMA cells. GNE-274 (1-1000 nM; 7-10 days) potently inhibits cellular proliferation, exhibiting greater potency than fulvestrant, 4-OHT, AZD9496, and GDC-0810 in E2-stimulated ER + breast cancer cell lines. In transposaseaccessible chromatin sequencing (ATAC-seq) assay, GNE-274 increase chromatin accessibility at ER-DNA binding sites, it significantly alters chromatin accessibility at 594 sites. But GDC-0927 has considerably less impact on chromatin accessibility. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MCF7, MB-134, HCC1500, EFM-19, CAMA-1, T-47D cells Concentration: 1 nM; 10 nM; 100 nM; 1000 nM Incubation Time: 7-10 days Result: Exhibited IC 50 values approximately ranging from 5nM to 20 nM in different cells.Form:Solid. Specification: 0.98 Molecular Formula: C29H31NO4 Molecular Weight: 457.56