2369048-69-9
Chemical Structure
GNE-274
- CAS No.: 2369048-69-9
- Formula:C29H31NO4
- Molecular Weight:457.56
IUPAC Name: (S)-3-(3-hydroxyphenyl)-4-methyl-2-(4-((1-propylazetidin-3-yl)methoxy)phenyl)-2H-chromen-6-ol
InChIKey: ABSGIUXAPWSTBC-LJAQVGFWSA-N
SMILES: CCCN1CC(C1)COC2=CC=C([C@@H]3OC4=CC=C(C=C4C(C)=C3C5=CC(O)=CC=C5)O)C=C2
Biological Activity: 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[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GNE-274 | 98.00% | 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. | ||||||||||||||||||||
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References
- [1]. Guan J, et al. Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility. Cell. 2019 Aug 08;178(4):949-963.e18. [Content Brief]
- [2]. Munne PM, et al. Compressive stress-mediated p38 activation required for ERα + phenotype in breast cancer. Nature communications. 2021 Nov 29;12(1):6967.
