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Estrogen Receptor/ERR

The ERRs are orphan nuclear receptors, meaning the identity of their endogenous ligand has yet to be unambiguously determined. They are named because of sequence homology with estrogen receptors, but do not appear to bind estrogens or other tested steroid hormones.There are three human estrogen related receptors:ERRα,ERRβand ERRγ .

  • ARV-471
    T397102229711-68-4
    ARV-471 (Vepdegestrant) is a orally active Cereblon -based estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.
    • $265
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  • Tamoxifen
    T690610540-29-1
    • $39
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  • 4-Hydroxytamoxifen
    T442068047-06-3
    4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.
    • $64
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  • Fulvestrant
    T2146129453-61-8
    Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.
    • $42
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  • Genistin
    T2882529-59-9
    Genistin (Genistoside) is the major isoflavonoid of soybeans and soy products.It has been reported to possess various therapeutic effects, including anti-inflammatory and anticancer activities
    • $60
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  • Estradiol
    T104850-28-2
    Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).
    • $30
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  • Chlorotrianisene
    T2569569-57-3
    Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.
    • $37
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  • Ethisterone
    T0301434-03-7
    Ethisterone (17α-Ethynyltestosterone) is a progestogen hormone.
    • $50
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  • Kaempferol
    T2177520-18-3
    Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.
    • $46
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  • Premarin
    T36857L481-97-0
    Premarin (Estrone 3-sulfate) is an an estrogen sulfate with neuroprotective actions during traumatic brain injury.
    • $195
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  • Y134
    T23540849662-80-2
    Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively. The selectivity of Y134 for ERα is 121.1 times higher than that for ERβ. Y134 inhibited the proliferation of ER positive human breast cancer cells stimulated by estrogen.
    • $151
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  • Nylestriol
    T2074439791-20-3
    Nylestriol (LY 49825) is an agonist of estrogen receptor.
    • $50
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  • beta-Estradiol 17-hemisuccinate
    T96047698-93-3
    beta-Estradiol 17-hemisuccinate selectively stains estrogen receptor (ER)-rich cells.
    • $148
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  • Nafoxidine
    T21387L1845-11-0
    Nafoxidine is an estrogen antagonist that has been used in the treatment of breast cancer.
    • $148
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  • Camizestrant TFA
    T11237L In house
    Camizestrant TFA (AZD-9833 TFA) is a potent and orally active antagonist of estrogen receptor (ER).
    • $98
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  • Giredestrant tartrate
    T112362407529-33-1In house
    Giredestrant tartrate (Estrogen receptor antagonist 1) is a novel, orally active, selective and effective non-steroidal estrogen receptor antagonist. Giredestrant tartrate strongly binds to ER, resulting in the failure of ER to activate the transcription of targeted genes and promoting the degradation of ER protein. Giredestrant tartrate can be used to treat tumor diseases.
    • $117
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  • G36
    T227941392487-51-2In house
    G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.
    • $34
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  • Pipendoxifene hydrochloride
    T12482245124-69-0In house
    Pipendoxifene hydrochloride is a selective modulator of estrogen receptor.
    • $48
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  • Erteberel
    T6306533884-09-2In house
    Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.
    • $156
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  • Estradiol 3-sulfamate
    T11235172377-52-5In house
    Estradiol 3-sulfamate (BLE 00084) is an orally active and highly potent steroidal estrone sulfatase (ES) inhibitor.Estradiol 3-sulfamate has a K(i) value of 73 nM for ES in human placental microsomes and can be used in the study of breast cancer.
    • $147 TargetMol
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  • Droloxifene
    T1109882413-20-5In house
    Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.
    • $49
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  • Camizestrant
    T112372222844-89-3In house
    Camizestrant (Estrogen receptor antagonist 2) is an antagonist of the estrogen receptor and can be used in studies about ER+ HER2-advanced breast cancer[1].
    • $158
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  • (Rac)-Acolbifene
    T12654151533-34-5In house
    (Rac)-Acolbifene (EM-343) is the racemic form of Acolbifene. Acolbifene is a estrogen receptor antagonist. (Rac)-Acolbifene exhibits anti-estrogenic and estrogenic activities. (Rac)-Acolbifene contains a piperidine ring and exhibits good pharmacological profile,relative binding affinity (RBA)=380.
    • $32
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  • Acolbifene
    T10239182167-02-8In house
    Acolbifene (SCH 57068) is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.
    • $76
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  • Clomiphene citrate
    T119350-41-9
    Clomiphene citrate (NSC 35770) is a selective estrogen receptor modulator.
    • $45
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  • Chrysin
    T2837480-40-0
    Chrysin (5,7-Dihydroxyflavone) exhibits many biological activities and pharmacological effects, including antioxidant, anti-inflammatory, anticancer, and antiviral activities.
    • $42
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  • Liquiritigenin
    T3325578-86-9
    Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.
    • $48
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  • DPN
    T76441428-67-7
    DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .
    • $32
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  • Raloxifene hydrochloride
    T154982640-04-8
    Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.
    • $38
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  • Brilanestrant
    T51181365888-06-7
    Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).
    • $48
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  • (E/Z)-4-Hydroxytamoxifen
    T674368392-35-8
    (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.
    • $47
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  • Bazedoxifene hydrochloride
    T6404198480-56-7
    Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6 GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.
    • $55
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  • Cholesterol
    T076057-88-5
    Cholesterol (cholesteryl alcohol) is a natural product that is the major sterol in mammals and an agonist of estrogen-related receptor α (ERRα). Cholesterol is widely found in the cell membranes of animals and is also used in the synthesis of several important hormones and bile acids.
    • $45
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  • Isopsoralenoside
    TN1148905954-18-9
    Isopsoralenoside shows estrogen-like, osteoblastic proliferation accelerating, antitumor, and antibacterial effects.
    • $106
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  • Bavachin
    T384619879-32-4
    Bavachin (Corylifolin) is a phytoestrogen that activates the estrogen receptors ERα and ERβ.
    • $30
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  • Dienestrol
    T003584-17-3
    Dienestrol (Restrol) is a synthetic and nonsteroidal estrogen, which is an estrogen receptor agonist. Estrogens can increase a normal clear discharge from the vagina and make the vulva and urethra healthy.
    • $30
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  • PHTPP
    T4388805239-56-9
    PHTPP is a selective ERβ antagonist.
    • $30
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  • Ethynyl estradiol
    T142457-63-6
    Ethynyl estradiol is a semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.
    • $32
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  • Endoxifen
    T4281110025-28-0
    (E/Z)-Endoxifen ((E/Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.
    • $41
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  • kaempferide
    T3806491-54-3
    kaempferide (4'-Methylkaempferol) inhibits the proliferation of native and estrogen receptor beta overexpressing colon cancer cells through a mechanism not mediated by ligand binding dependent estrogen receptor activation.
    • $80
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  • Endoxifen Z-isomer hydrochloride
    T68271032008-74-4
    Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.
    • $46
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  • Estradiol benzoate
    T038450-50-0
    Estradiol benzoate (Benzhormovarine) is the synthetic benzoate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.
    • $45
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  • Bazedoxifene acetate
    T2544198481-33-3
    Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).
    • $39
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  • Raloxifene
    T2041984449-90-1
    Raloxifene (LY-139481) is a selective oestrogen receptor modulator. It has effects on bone and breast cancer and cardiovascular disease risk.
    • $49
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  • Estetrol
    T1524815183-37-6
    Estetrol(Donesta) is an orally available, selective modulator of the estrogen receptor, a naturally occurring estrogen synthesized by the human fetal liver during pregnancy.Estetrol has effects on the endometrium or central nervous system, but is antagonistic to the breast.Estetrol may help to reduce thrombosis at low concentrations. Estetrol may be used to relieve menopausal symptoms.
    • $128
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  • Estrogen receptor modulator 10
    T824392991504-90-4
    Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].
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  • CIDD-0149897
    T827222862784-20-9
    CIDD-0149897 is a potent, selective, and brain-penetrant agonist of ERβ that exhibits antitumor activity in glioblastoma [1].
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  • GLL 398
    T99972077980-80-2
    GLL 398 is an orally active and selective degrader of estrogen receptor with an IC50 of 1.14 nM. GLL 398 blocks tumor growth in xenograft breast cancer models.
    • $195
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  • H3B-5942
    T56332052128-15-9
    H3B-5942 belongs to a class of ERα antagonists referred to as selective estrogen receptor covalent antagonists (SERCA).
    • $78
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  • FLTX1
    T89841481401-71-1
    FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.
    • $88
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