GNE-274 T39916

Product Introduction
Bioactivity


英文名: GNE-274

描述: 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.

体外活性: GNE-274 (0.1 nM-1000 nM; 4 hours) fails to trigger increased ER turnover in MCF7, MD-134, HCC1500 and CAMA cells[1].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[1].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[1]. Cell Viability Assay[1]Cell 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: GNE274 | GNE 274 | GNE-274

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途