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

Estrogen Receptor/ERR

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161740
    PHTPP-1304
    Degrader 99.96%
    PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization and degradation of estrogen receptor ERβ (DC50:~2 nM, HEK293T). PHTPP-1304 also induces the formation of p62+ERβ+ puncta that are affected by autophagic flux in a dose-dependent manner.
    PHTPP-1304
  • HY-I0508S
    Phthalic acid-d4
    Antagonist 98.36%
    Phthalic acid-d4 is the deuterium labeled Phthalic acid. Phthalic acid is the final common metabolite of phthalic acid esters (PAEs). Phthalic acid can be used for the synthesis of synthetic agents, such as isophthalic acid (IPA), and terephthalic acid (TPA). Phthalic acid has applications in the preparation of phthalate ester plasticizers. Phthalic acid exhibits mutagenic effect and causes genetic damage in mammalian germ cells.
    Phthalic acid-d<sub>4</sub>
  • HY-B0216R
    Ethinylestradiol (Standard)
    Agonist 99.86%
    Ethynyl Estradiol (Standard) is the analytical standard of Ethynyl Estradiol. This product is intended for research and analytical applications.
    Ethinylestradiol (Standard)
  • HY-110201
    Estrogen receptor modulator 1
    Modulator 99.91%
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
    Estrogen receptor modulator 1
  • HY-124414
    4'-Hydroxytamoxifen
    Modulator 99.2%
    4'-Hydroxytamoxifen is a metabolite of Tamoxifen. 4'-Hydroxytamoxifen shows higher affinity for the ER than Tamoxifen. 4'-Hydroxytamoxifen induces a non-apoptotic cytotoxic effect in human endometrial adenocarcinoma cells.
    4'-Hydroxytamoxifen
  • HY-P3833A
    Yp537 TFA
    Inhibitor
    Yp537 TFA is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor.
    Yp537 TFA
  • HY-123047
    Tibolone
    Agonist 99.39%
    Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone
  • HY-B0412R
    Estriol (Standard)
    Antagonist 99.62%
    Estriol (Standard) is the analytical standard of Estriol. This product is intended for research and analytical applications.
    Estriol (Standard)
  • HY-D0272
    2,3,4-Trihydroxybenzophenone
    99.92%
    2,3,4-Trihydroxybenzophenone is a hydroxylated benzophenone UV filter with estrogenic activity. 2,3,4-Trihydroxybenzophenone is a quorum sensing inhibitor and an EC 1.14.18.1 (tyrosinase) inhibitor. 2,3,4-Trihydroxybenzophenone is also a human urinary metabolite, a rat metabolite and a drug metabolite.
    2,3,4-Trihydroxybenzophenone
  • HY-B0652
    Etonogestrel
    Agonist 99.14%
    Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel
  • HY-B0234S1
    Estrone-d2
    Agonist 99.78%
    Estrone-d2 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.
    Estrone-d<sub>2</sub>
  • HY-13636S
    Fulvestrant-d3
    Antagonist
    Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
    Fulvestrant-d<sub>3</sub>
  • HY-132194
    ERα degrader-2
    Inhibitor 99.71%
    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-B0234S4
    Estrone-d2-1
    Agonist
    Estrone-d2-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.
    Estrone-d<sub>2</sub>-1
  • 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-W1006471
    Estrogen receptor-agonist-1
    Agonist 98.69%
    Estrogen receptor-agonist-1 (compound 4e) is a estrogen receptor (ER) agonist that binds to ERα with high affinity.
    Estrogen receptor-agonist-1
  • HY-110157
    AC-186
    Agonist 99.61%
    AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease.
    AC-186
  • HY-137004
    Indazole-Cl
    Agonist 98.72%
    Indazole-Cl (Ind-Cl) is an Estrogen receptor (ER)-β-specific agonist with inflammatory effect. Indazole-Cl inhibits cyclooxygenase-2 exression reduction induced by hypoxia. And Indazole-Cl inhibits ROS production. Indazole-Cl also inhibits cell migration and invasion by hypoxia increased by hypoxia. Indazole-Cl is potent inhibitor of hypoxia-induced inflammation in vascular smooth muscle cells (VSMCs).
    Indazole-Cl
  • HY-B1617A
    Zuclomiphene citrate
    Modulator 98.09%
    Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent.
    Zuclomiphene citrate
  • HY-W739985
    7α-(Thiomethyl)spironolactone
    Antagonist
    7α-(Thiomethyl)spironolactone is a nuclear steroid receptor antagonist that can be used for the research of coronaviruses.
    7α-(Thiomethyl)spironolactone
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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