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-111226
    GSK5182
    Inhibitor 99.10%
    GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC).
    GSK5182
  • HY-B1100
    Estradiol cypionate
    Inhibitor 99.47%
    Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.
    Estradiol cypionate
  • HY-N0233
    Bavachin
    Agonist 99.94%
    Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
    Bavachin
  • HY-A0037
    Lasofoxifene
    99.27%
    Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis.
    Lasofoxifene
  • HY-19822A
    Elacestrant dihydrochloride
    Inhibitor 99.54%
    Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.
    Elacestrant dihydrochloride
  • HY-18719E
    Endoxifen
    99.51%
    Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
    Endoxifen
  • HY-129079
    TFMB-(R)-2-HG
    Inhibitor 98.26%
    TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG and acute myeloid leukemia (AML) oncogenic factor. TFMB-(R)-2-HG competitively inhibits α-ketoglutarate-dependent dioxygenases such as KDM2B and FTO. TFMB-(R)-2-HG impairs cell differentiation in response to Estrogen withdrawal. TFMB-(R)-2-HG is used in acute myeloid leukemia and glioma research.
    TFMB-(R)-2-HG
  • HY-103454B
    MPP hydrochloride
    Modulator 99.25%
    MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
    MPP hydrochloride
  • HY-110195
    Smurf1-IN-A01
    99.81%
    Smurf1-IN-A01 is a Smurf1 inhibitor. Smurf1-IN-A01 has anticancer activity and can be used for the research of osteoporosis and age-related macular degeneration.
    Smurf1-IN-A01
  • HY-B0005A
    Toremifene
    Modulator 99.73%
    Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
    Toremifene
  • HY-113293A
    Estrone sulfate potassium
    99.94%
    Estrone sulfate potassium is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate potassium is also a substrate of the OATP1B3 transporter. Estrone sulfate potassium can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate potassium stimulates the growth of nitrosomethylurea-induced mammary tumors in ovariectomized rats and the colony formation of dispersed nitrosomethylurea mammary cells, with conversion into Estrone and Estradiol occurring both in vivo and in vitro during this process. Estrone sulfate potassium is applicable to breast cancer-related research.
    Estrone sulfate potassium
  • HY-B0005
    Toremifene citrate
    Modulator 99.88%
    Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively.
    Toremifene citrate
  • HY-B0141S1
    Estradiol-d4
    Agonist 99.55%
    Estradiol-d4 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
    Estradiol-d<sub>4</sub>
  • HY-30270
    Mequinol
    Activator 99.98%
    Mequinol (4-Methoxyphenol)yes MercurialisOne of the bioactive ingredients, mainly used for skin discoloration. MequinolIs an antioxidant that has additive/synergistic effects on carcinogenesis when combined with other phenolic antioxidants. Mequinolalso promote hERαDependent chaperone production with potential estrogenic activity.
    Mequinol
  • HY-A0038
    Lasofoxifene tartrate
    Modulator 99.93%
    Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis.
    Lasofoxifene tartrate
  • HY-14933
    Prinaberel
    Agonist 98.05%
    Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.
    Prinaberel
  • HY-A0087
    Octocrylene
    Activator 98.68%
    Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes.
    Octocrylene
  • HY-I0508
    Phthalic acid
    Antagonist 99.94%
    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
  • HY-W006405
    Isoflavone
    Isoflavone is an orally available bioactive component of soy phytoestrogen with lipid-lowering and antioxidant activities. Isoflavone prevents a variety of chronic diseases by regulating fatty acid oxidation in the liver and gene expression in adipose tissue. In addition, isoflavone has important value in the research of cancer and cardiovascular diseases.
    Isoflavone
  • HY-B0723
    Ospemifene
    Modulator 99.84%
    Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer.
    Ospemifene
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

Your Search Returned No Results.

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

Please try each isoform separately.