Scientific Reviews
Product Guides
Blogs
Topics
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
24 Results for "
ESR1
" in MedChemExpress (MCE) Product Catalog:
Products (24)
24 Results for "ESR1" in MCE Product Catalog:
6
6 Publications Verification
Synonyms: GDC-9545; RG6171
Target:
Research Areas:
Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER + breast cancer [1].
5
2
1
1 Cited Publications
Research Areas:
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids [1]. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
1
1 Cited Publications
Cat. No.: HY-P70248
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: ESR1; Estrogen Receptor Alpha Delta 4*,5,6,7*/654 Isoform; Prev. ESR; Estrogen Receptor Alpha 3*,4,5,6,7,8*/1032 Isoform; ER-Alpha; Estrogen Receptor Alpha 3*,4,5,6,7,8*/1068 Isoform; ER; Estrogen Receptor Alpha 3*,4,5,6,7,8*/984 Isoform; Nuclear Receptor
Species:
Human
Source:
E. coli
Cat. No.: HY-RS04529
Target:
Research Areas:
ESR1 Human Pre-designed siRNA Set A contains three designed siRNAs for ESR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS04530
Target:
Research Areas:
Esr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Esr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-163650
CAS No.: 252950-56-4
Target:
Research Areas:
DTPD-Q is an antioxidant and an oxidative derivative of methylbenzenesulfonyl-p-phenylenediamine DTPD. DTPD-Q is a molecule that binds to AKT1 and ESR1, with high binding affinity to core targets associated with male infertility and its subtypes. DTPD-Q can be used in studies related to male infertility [1] .
Cat. No.: HY-N1508
CAS No.: 78285-90-2
Cat. No.: HY-RS04531
Target:
Research Areas:
Esr1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Esr1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-135903
CAS No.: 2407529-33-1
Synonyms: GDC-9545 tartrate; RG6171 tartrate
Target:
Giredestrant tartrate (GDC-9545 tartrate) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant tartrate promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant tartrate reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant tartrate induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant tartrate can be used for the research of ER + breast cancer [1].
Cat. No.: HY-164924
CAS No.: 3026007-23-5
Target:
Research Areas:
ERD-12310A is an orally active ERα PROTAC degrader, with a Ki value of 0.95 nM against human ERα and a DC50 of 47 pM for ERα in MCF-7 cells. ERD-12310A forms a ternary complex with ERα and the CRBN E3 ubiquitin ligase, thereby inducing ubiquitination and proteasomal degradation of wild-type and ESR1 Y537S mutant ERα. ERD-12310A induces tumor regression in ER+ breast cancer xenografts and inhibits tumor growth in ESR1 Y537S mutant breast cancer xenografts. ERD-12310A can be used in studies related to ER-positive breast cancer and ESR1-mutant breast cancer [1] .
Cat. No.: HY-147165A
Target:
Research Areas:
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids [1]. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-144314
CAS No.: 2906869-08-5
Target:
Research Areas:
PSDalpha is a photoactivatable PS-Degron targeting estrogen receptor α (ERα/ESR1), with a Ki of 72.8 nM for ERα. PSDalpha consists of an ERα-targeting estradiol moiety conjugated via an alkyne bond to triphenylamine-benzothiadiazole (TB), an aggregation-induced emission (AIE) photosensitizer. Upon visible light irradiation, PSDalpha generates singlet oxygen ( 1O2) and induces controllable ERα degradation. PSDalpha also induces G1 phase arrest and apoptosis. PSDalpha can be used in studies related to ERα-positive breast cancer and light-controlled targeted protein degradation [1].
Cat. No.: HY-N1508R
CAS No.: 78285-90-2
Category:
Target:
Research Areas:
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] .
Cat. No.: HY-N0259R
CAS No.: 110623-73-9
Synonyms: Epmedin B (Standard)
Cat. No.: HY-109176R
CAS No.: 1953133-47-5
Synonyms: GDC-9545 (Standard); RG6171 (Standard)
Giredestrant (Standard) (GDC-9545 (Standard); RG6171 (Standard)) is the analytical standard of Giredestrant (HY-109176). This product is intended for research and analytical applications. Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER + breast cancer [1].
Cat. No.: HY-187225
Target:
Research Areas:
NCP07 is a PROTAC degrader targeting the coactivator-binding site (CBS) of ERα. NCP07 induces the formation of the ERα-NCP07-VHL ternary complex and promotes ERα degradation via the ubiquitin-proteasome system. NCP07 induces apoptosis and cell cycle arrest in endocrine therapy-resistant breast cancer cells. NCP07 inhibits the proliferation of wild-type and ESR1-mutant breast cancer cells. NCP07 is applicable to breast cancer-related research [1].
- 1
- 2
-
-
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
