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  3. GNE-274

GNE-274 

Cat. No.: HY-141551
Handling Instructions

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.

For research use only. We do not sell to patients.

GNE-274 Chemical Structure

GNE-274 Chemical Structure

CAS No. : 2369048-69-9

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Description

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[1][2].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 values approximately ranging from 5nM to 20 nM in different cells.
Molecular Weight

457.56

Formula

C₂₉H₃₁NO₄

CAS No.
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GNE-274
Cat. No.:
HY-141551
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