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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
6 Results for "
ERα ligand binding domain
" in MedChemExpress (MCE) Product Catalog:
Products (6)
6 Results for "ERα ligand binding domain" in MCE Product Catalog:
Cat. No.: HY-172937
CAS No.: 3070968-56-5
Research Areas:
ERα degrader 13 is an orally active, methylene blue-Raloxifene (HY-13738) conjugated photoactivatable ERα degrader with a Kd value of 27.1 nM. Upon irradiation at 660 nm, ERα degrader 13 generates ROS and heat near the ligand-binding domain of ERα, triggering oxidation, residue unfolding, and ERα degradation via the ubiquitin-proteasome system. ERα degrader 13 inhibits cancer cell proliferation and induces tumor regression in breast cancer xenograft models. ERα degrader 13 can be used in breast cancer-related research .
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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 .
Cat. No.: HY-121372
CAS No.: 43000-65-3
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Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
Cat. No.: HY-181171
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HIT-2 is an estrogen receptor alpha (ERα) inhibitor that can bind to the ERα ligand binding domain. HIT-2 forms stable interactions including hydrogen bonds, π-π stacking, and hydrophobic contacts to disrupt ERα-driven signaling. HIT-2 exhibits antineoplastic activity against breast cancer. HIT-2 can be used for the research of breast cancer .
Cat. No.: HY-187217
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ERα-IN-2 is a ERα inhibitor. ERα-IN-2 blocks agonist-induced recruitment of nuclear receptor-binding peptides to the ligand-binding domain of ERα and exerts selective antiproliferative effects in breast cancer cells. ERα-IN-2 can be used in breast cancer-related research .
Cat. No.: HY-181345
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OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC50 values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
