2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Estrogen Receptor/ERR

Estrogen Receptor/ERR

Estrogen Receptor/ERR

Related Products

PDF 3.53 MB

Estrogen receptors are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-estradiol). Two classes of estrogen receptor exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and GPER (GPR30), which is a member of the rhodopsin-like family of G protein-coupled receptors. The ER's helix 12 domain plays a crucial role in determining interactions with coactivators and corepressors and, therefore, the respective agonist or antagonist effect of the ligand. Different ligands may differ in their affinity for alpha and beta isoforms of the estrogen receptor: estradiol binds equally well to both receptors, estrone, and raloxifene bind preferentially to the alpha receptor, estriol, and genistein to the beta receptor. Estrogen and its receptors are essential for sexual development and reproductive function, but also play a role in other tissues such as bone. Estrogen receptors are also involved in pathological processes including breast cancer, endometrial cancer, and osteoporosis. Alternative promoter usage and alternative splicing result in dozens of transcript variants, but the full-length nature of many of these variants has not been determined.

Estrogen Receptor/ERR Isoform Specific Products:

Estrogen Receptor/ERR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14589R
    Chrysin (Standard)
    		Inhibitor
    Chrysin (Standard) is the analytical standard of Chrysin. This product is intended for research and analytical applications. Chrysin is one of the most well known estrogen blockers.
    Chrysin (Standard)
  • HY-137144
    Fulvestrant-3-boronic acid
    		Inhibitor 99.7%
    Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells.
    Fulvestrant-3-boronic acid
  • HY-W009066
    2-Ethylhexyl diphenyl phosphate
    		Inhibitor
    2-Ethylhexyl diphenyl phosphate is an organophosphate flame retardants (OPFRs) and a PPARG agonist (EC20: 2.04 µM). 2-Ethylhexyl diphenyl phosphate also inhibits ERRγ transcriptional activity (IC50: 1.3 µM). 2-Ethylhexyl diphenyl phosphate upregulates 3β-HSD1, human chorionic gonadotropin (hCG) and progesterone secretion. 2-Ethylhexyl diphenyl phosphate can be used in studies of female reproduction and fetal development.
    2-Ethylhexyl diphenyl phosphate
  • HY-111226A
    (E/Z)-GSK5182
    		Inhibitor 98.90%
    (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma.
    (E/Z)-GSK5182
  • HY-131404
    TPBM
    		Inhibitor 98.51%
    TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth.
    TPBM
  • HY-18719D
    Endoxifen (E-isomer)
    		Inhibitor 98.02%
    Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer exhibits antiestrogenic effects.
    Endoxifen (E-isomer)
  • HY-N1507
    Tracheloside
    		Inhibitor 99.77%
    Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.
    Tracheloside
  • HY-150601
    Estrogen receptor-IN-1
    		Inhibitor 99.87%
    Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC50s of 13, 5µM for ERα and Erβ, respectively.
    Estrogen receptor-IN-1
  • HY-18719C
    Endoxifen E-isomer hydrochloride
    		Inhibitor 98.20%
    Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer hydrochloride exhibits antiestrogenic effects.
    Endoxifen E-isomer hydrochloride
  • HY-132194
    ERα degrader-2
    		Inhibitor 98.30%
    ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research.
    ERα degrader-2
  • HY-153895
    SLU-PP-1072
    		Inhibitor 98.24%
    SLU-PP-1072 is a dual ERRα/γ inverse agonist, used in Prostate cancer (PCa) research. SLU-PP-1072 disrupts PCa cell metabolism, and induces apoptosis via dysregulating cell cycle.
    SLU-PP-1072
  • HY-163561
    CARM1-IN-6
    		Inhibitor 99.59%
    CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC50 of 12.3 μM and a Kd of 0.6785 μM. CARM1-IN-6 suppresses oncogenic estrogen/ERα-target gene expression, activates type I interferon (IFN) and IFN-induced genes (ISGs), induces cell cycle arrest, and inhibits breast cancer cell proliferation both in vitro and in vivo. CARM1-IN-6 can be used for the research of breast cancer.
    CARM1-IN-6
  • HY-19822D
    Elacestrant (S enantiomer)
    		Inhibitor
    Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
    Elacestrant (S enantiomer)
  • HY-179433
    PROTAC AR Degrader-12
    		Inhibitor
    PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer.
    PROTAC AR Degrader-12
  • HY-N2335R
    Coumestrol (Standard)
    		Inhibitor
    Coumestrol (Standard) is the analytical standard of Coumestrol. This product is intended for research and analytical applications. Coumestrol, a phytoestrogen present in soybean products, exhibits activities against cancers, neurological disorders, and autoimmune diseases. It suppresses proliferation of ES2 cells with an IC50 of 50 μM.
    Coumestrol (Standard)
  • HY-19822B
    Elacestrant S enantiomer dihydrochloride
    		Inhibitor
    Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
    Elacestrant S enantiomer dihydrochloride
  • HY-P3833A
    Yp537 TFA
    		Inhibitor
    Yp537 TFA is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor.
    Yp537 TFA
  • HY-13636A
    Fulvestrant (S enantiomer)
    		Inhibitor
    Fulvestrant (ICI 182780; ZD 9238) S enantiomer is the S-enantiomer of Fulvestrant (HY-13636), a potent estrogen receptor inhibitor. Fulvestrant binds to and blocks the estrogen receptor, promotes its degradation, and thereby inhibits receptor dimerization, nucleocytoplasmic shuttling and transcriptional activity. Fulvestrant effectively blocks estrogen signaling, MAPK pathway activation and ER-regulated protein expression. Fulvestrant induces apoptosis, inhibits the proliferation of breast cancer and prolactinoma cells, and reduces the mineralization level, alkaline phosphatase activity and osteocalcin expression of preosteoblasts. Prenatal exposure to Fulvestrant impairs ovarian follicular development and causes ovarian structural damage. Fulvestrant has been widely used in studies related to breast cancer, prolactinoma and other conditions.
    Fulvestrant (S enantiomer)
  • HY-P991358
    XOMA-213
    		Inhibitor 98.46%
    XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer.
    XOMA-213
  • HY-128839
    PROTAC ERRα Degrader-2
    		Inhibitor
    PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.
    PROTAC ERRα Degrader-2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.