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-144139
    Estrogen receptor antagonist 3
    Antagonist
    Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7).
    Estrogen receptor antagonist 3
  • HY-149584
    CIDD-0149897
    Agonist 99.91%
    CIDD-0149897 is a potent, selective and brain-penetrant ERβ agonist. CIDD-0149897 exert antitumor functions in glioblastoma.
    CIDD-0149897
  • HY-135671
    AhR modulator-1
    Inhibitor
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
    AhR modulator-1
  • HY-126109
    (±)-8-Prenylnaringenin
    Modulator
    (±)-8-Prenylnaringenin, a natural prenylated flavonoid, is a potent phytoestrogen. (±)-8-Prenylnaringenin is an orally active selective estrogen receptor modulator (SERM) (Estrogen Receptor/ERR) that inhibits ERα and ERβ with IC50s of 57 nM and 68 nM, respectively. (±)-8-Prenylnaringenin has anticancer effects, and can be used for osteoporosis research.
    (±)-8-Prenylnaringenin
  • HY-150692
    Estrogen receptor α antagonist 1
    Antagonist
    Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer.
    Estrogen receptor α antagonist 1
  • HY-N6678S
    (Rac)-Zearalanone-d6
    Activator
    (Rac)-Zearalanone-d6 is the racemate of Zearalanone. Zearalenone is a nonsteroidal estrogenic mycotoxin produced by Fusarium species, which colonizes several grains. Zearalenone has low acute toxicity and carcinogenicity. Due to its agonistic effect on the estrogen receptor, Zearalenone exhibits distinct estrogenic and anabolic properties in several animal species, resulting in severe effects on the reproductive system[1][2].
    (Rac)-Zearalanone-d<sub>6</sub>
  • 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
  • HY-114770
    (E,E)-GLL398
    (E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604.
    (E,E)-GLL398
  • HY-133222
    STX140
    STX140 is an orally active microtubule disruptor. STX140 induces apoptosis in the hormone-independent PC-3 prostate cell lines. STX140 has anti-angiogenic and anti-tumour activities.
    STX140
  • HY-163679
    PROTAC ERα Degrader-9
    Degrader
    PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), MCF-7Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
    PROTAC ERα Degrader-9
  • HY-107045
    CHF 4227 free base
    Modulator
    CHF 4227 free base is an orally active and selective estrogen receptor modulator (SERM) with high affinity to the human estrogen receptor-α and -β (Ki values of 0.017 nM and 0.099 nM, respectively).
    CHF 4227 free base
  • HY-13757AS1
    Tamoxifen-d3
    Tamoxifen-d3 is the deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen-d<sub>3</sub>
  • HY-138211
    BE-26263
    Activator
    BE-26263, an antiosteoporotic agent that can be isolated from Scedosporium apiospermum, possesses estrogenic effect.
    BE-26263
  • HY-170340
    PROTAC ER Degrader-14
    PROTAC ER Degrader-14 (compound 86) is a PTORAC-type Estrogen Receptor/ERR degrader, which is composed of E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide (HY-168055), PROTAC Linker (black part) N-Boc-piperazine (HY-30105) and target protein ligand (red part) ER ligand-6 (HY-170341). Among them, E3 ligase + Linker constitute tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate (HY-W998234).
    PROTAC ER Degrader-14
  • HY-117038
    Anordiol
    Antagonist
    Anordiol is an antiestrogenic compound with weak estrogenic activity. It can reduce the parameters of uterine growth (including uterine wet weight, soluble protein content, and DNA content) induced by estradiol in rats and can also regulate the estrous cycle in rats. Anordiol holds potential application value in the research of antiestrogen-related diseases.
    Anordiol
  • HY-110392
    CMP8
    CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively.
    CMP8
  • HY-15449R
    Kaempferide (Standard)
    Inhibitor
    Kaempferide (Standard) is the analytical standard of Kaempferide. This product is intended for research and analytical applications.
    Kaempferide (Standard)
  • HY-135592
    LY88074 Methyl ether
    Activator
    LY88074 Methyl ether (Example 2) is useful for the inhibition of the various estrogen deficient conditions, which are associated with estrogendeprivation syndrome including osteoporosis and hyperlipidemia.
    LY88074 Methyl ether
  • HY-113293BS
    Estrone sulfate-d5 sodium
    Estrone sulfate-d5 (sodium) is the deuterium labeled Estrone sulfate sodium. Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
    Estrone sulfate-d<sub>5</sub> sodium
  • HY-B1100R
    Estradiol cypionate (Standard)
    Inhibitor
    Estradiol cypionate (Standard) is the analytical standard of Estradiol cypionate. This product is intended for research and analytical applications. Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.
    Estradiol cypionate (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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