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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.

Targets for  Estrogen Receptor/ERR

Products for  Estrogen Receptor/ERR

  1. Cat.No. Product Name Information
  2. GC11282 β-Estradiol

    Sex hormone

     β-Estradiol  Chemical Structure
  3. GC40753 α-Zearalanol

    α-Zearalenol (α-zol) is a Mycotoxin with high affinity for the estrogen receptors (ER).

    α-Zearalanol  Chemical Structure
  4. GC38008 β-Zearalenol A hepatic metabolite of zearalenone β-Zearalenol  Chemical Structure
  5. GC45968 (±)-Liquiritigenin A flavonoid with anticancer activity (±)-Liquiritigenin  Chemical Structure
  6. GC34962 (±)-Medicarpin (±)-Medicarpin, a pterocarpan, is a type of isoflavonoid isolated from several medicinal plant species with various biological effects, including Sophora japonica, Zollernia paraensis and Platymiscium yucatamun, Machaerium aristulatum, Platymiscium floribundum, and so on. (±)-Medicarpin potently inhibits osteoclastogenesis and promotes bone healing and increases bone mass by osteoblast differentiation with estrogen receptor (ER) β-mediated osteogenic action. (±)-Medicarpin  Chemical Structure
  7. GC65885 (1S,3R)-GNE-502 (1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor. (1S,3R)-GNE-502  Chemical Structure
  8. GC34965 (20S)-Protopanaxatriol An active ginsenoside metabolite (20S)-Protopanaxatriol  Chemical Structure
  9. GC34978 (E)-4-Hydroxytamoxifen (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator. (E)-4-Hydroxytamoxifen  Chemical Structure
  10. GC39747 (E/Z)-GSK5182 (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. (E/Z)-GSK5182  Chemical Structure
  11. GC40643 (R)-Equol Equol is a non-steroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzein by human intestinal microflora. (R)-Equol  Chemical Structure
  12. GC61488 (Rac)-Acolbifene (Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380. (Rac)-Acolbifene  Chemical Structure
  13. GC38542 10β,17β-dihydroxyestra-1,4-dien-3-one 10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain. 10β,17β-dihydroxyestra-1,4-dien-3-one  Chemical Structure
  14. GC13887 25(R)-27-hydroxy Cholesterol 25(R)-27-hydroxy Cholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor. 25(R)-27-hydroxy Cholesterol  Chemical Structure
  15. GC68533 3'-Hydroxymirificin

    3'-Hydroxymirificin (compound 3) is a natural product that can be obtained from the roots of Pueraria lobata. It has estrogenic and anti-proliferative activity against MCF-7 human breast cancer cells.

    3'-Hydroxymirificin  Chemical Structure
  16. GC17803 4-Hydroxytamoxifen 4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. 4-Hydroxytamoxifen is an estrogen receptor modulator. 4-Hydroxytamoxifen  Chemical Structure
  17. GC18362 Acolbifene Acolbifene is a selective estrogen receptor modulator (SERM). Acolbifene  Chemical Structure
  18. GC61514 Acolbifene hydrochloride Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties. Acolbifene hydrochloride  Chemical Structure
  19. GC62723 ARV-471 ARV-471 is an oral estrogen receptor PROTAC protein degrader for breast cancer. ARV-471 is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. ARV-471 leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM. ARV-471  Chemical Structure
  20. GC33381 Arzoxifene hydrochloride (LY 353381 HCl) Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. Arzoxifene hydrochloride (LY 353381 HCl)  Chemical Structure
  21. GC14405 AZD9496 estrogen receptor inhibitor, orally active AZD9496  Chemical Structure
  22. GC35450 AZD9496 maleate AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD). AZD9496 maleate  Chemical Structure
  23. GC17588 Bavachin estrogen receptors ERα and ERβ activator Bavachin  Chemical Structure
  24. GC14883 Bazedoxifene Bazedoxifene  Chemical Structure
  25. GC10852 Bazedoxifene acetate A selective estrogen receptor modulator Bazedoxifene acetate  Chemical Structure
  26. GC33011 BHPI An ERα antagonist BHPI  Chemical Structure
  27. GC32782 Brilanestrant (ARN-810) Brilanestrant (ARN-810) (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM. Brilanestrant (ARN-810)  Chemical Structure
  28. GC17398 Cholesterol

    Major sterol in mammals

    Cholesterol  Chemical Structure
  29. GC64477 Cholesterol-13C2 Cholesterol-13C2 is the 13C labeled Cholesterol. Cholesterol-13C2  Chemical Structure
  30. GC63843 Cholesterol-13C3 Cholesterol-13C3  Chemical Structure
  31. GC64334 Cholesterol-13C5 Cholesterol-13C5  Chemical Structure
  32. GN10028 Chrysin Chrysin  Chemical Structure
  33. GC70175 citrate

    Zuclomiphene-d4 (citrate) is the deuterated form of Zuclomiphene citrate. Zuclomiphene citrate has anti-estrogenic effects and is more effective than its trans-isomer in inhibiting the secretion of luteinizing hormone (LH). It is also an orally active cholesterol-lowering agent.

    citrate  Chemical Structure
  34. GC15366 Clomiphene citrate Selective estrogen receptor modulator Clomiphene citrate  Chemical Structure
  35. GC10002 Coumestrol competitive binder of the estrogen receptors ERα Coumestrol  Chemical Structure
  36. GC17688 Diarylpropionitrile(DPN) Diarylpropionitrile(DPN) (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC50 of 0.85 nM. Diarylpropionitrile(DPN)  Chemical Structure
  37. GC31008 Dienestrol

    Dienestrol is a synthetic, non-steroidal estrogen, is an estrogen receptor agonist, for the treatment of menopausal and postmenopausal symptoms.

    Dienestrol  Chemical Structure
  38. GC11215 Diethylstilbestrol synthetic nonsteroidal estrogen Diethylstilbestrol  Chemical Structure
  39. GC38098 Dihydroresveratrol Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations. Dihydroresveratrol  Chemical Structure
  40. GC63988 DK1 DK1 is a potent modulator of estrogen related receptor. DK1  Chemical Structure
  41. GC63989 DK3 DK3 is a potent and selective estrogen-related receptor alpha (ERRα) agonist. DK3  Chemical Structure
  42. GC39707 Droloxifene A selective estrogen receptor modulator Droloxifene  Chemical Structure
  43. GC64652 DS20362725 DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725  Chemical Structure
  44. GC64533 DS45500853 DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853  Chemical Structure
  45. GC10394 DY131 An ERRβ/γ agonist DY131  Chemical Structure
  46. GC33349 E3 ligase Ligand 5 E3 ligase Ligand 5 is an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively. E3 ligase Ligand 5  Chemical Structure
  47. GC33025 Elacestrant (RAD1901) Elacestrant (RAD1901) (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant (RAD1901)  Chemical Structure
  48. GC62379 Elacestrant (S enantiomer) 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)  Chemical Structure
  49. GC32696 Elacestrant dihydrochloride (RAD1901 dihydrochloride) Elacestrant dihydrochloride (RAD1901 dihydrochloride) (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride (RAD1901 dihydrochloride)  Chemical Structure
  50. GC34293 Elacestrant S enantiomer (RAD1901 S enantiomer) Elacestrant S enantiomer (RAD1901 S enantiomer)  Chemical Structure
  51. GC34294 Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride)  Chemical Structure
  52. GC35985 Enclomiphene citrate Enclomiphene ((E)-Clomiphene) citrate is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene citrate  Chemical Structure
  53. GC60806 Enclomiphene D4 hydrochloride Enclomiphene D4 hydrochloride ((E)-Clomiphene D4 hydrochloride; trans-Clomiphene D4 hydrochloride; Enclomifene D4 hydrochloride)?is a deuterium labeled Enclomiphene. Enclomiphene D4 hydrochloride  Chemical Structure
  54. GC12140 Endoxifen Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen  Chemical Structure
  55. GC35988 Endoxifen E-isomer Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer drug substance. Endoxifen E-isomer exhibits antiestrogenic effects. Endoxifen E-isomer  Chemical Structure
  56. GC35989 Endoxifen E-isomer hydrochloride Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer drug substance. Endoxifen E-isomer hydrochloride exhibits antiestrogenic effects. Endoxifen E-isomer hydrochloride  Chemical Structure
  57. GC35990 Endoxifen hydrochloride Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study. Endoxifen hydrochloride  Chemical Structure
  58. GC35991 Endoxifen Z-isomer hydrochloride Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen Z-isomer hydrochloride  Chemical Structure
  59. GC34006 Equilin (7-Dehydroestrone) Equilin (7-Dehydroestrone) (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin (7-Dehydroestrone)  Chemical Structure
  60. GC16292 Equol non-steroidal estrogen Equol  Chemical Structure
  61. GC67927 ERα degrader-2 ERα degrader-2  Chemical Structure
  62. GC10389 ERB 041 ERB 041 (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. ERB 041 displays >200-fold selectivity for ERβ over ERα. ERB 041 is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. ERB 041 induces ovarian cancer apoptosis. ERB 041  Chemical Structure
  63. GC30650 ERB-196 (WAY-202196) ERB-196 (WAY-202196) is a nonsteroidal selective estrogen receptor-β (ERβ) agonist. ERB-196 (WAY-202196)  Chemical Structure
  64. GC36001 ERD-308 ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively). ERD-308  Chemical Structure
  65. GC38777 ERRα antagonist-1 ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1. ERRα antagonist-1  Chemical Structure
  66. GC11822 Erteberel (LY500307) Erteberel (LY500307) (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel (LY500307)  Chemical Structure
  67. GC19478 Estetrol

    An estrogen steroid hormone

    Estetrol  Chemical Structure
  68. GC15245 Estradiol Benzoate Estrogen/progestogen receptor agonist Estradiol Benzoate  Chemical Structure
  69. GC10139 Estradiol Cypionate Estrogen receptor inhibitor Estradiol Cypionate  Chemical Structure
  70. GC60815 Estradiol dipropionate Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist. Estradiol dipropionate  Chemical Structure
  71. GC66878 Estradiol enanthate Estradiol enanthate is a shorter-acting estrogen. The combination of Estradiol enanthate and dihydroxyprogesterone acetophenide can be used as a monthly injectable contraceptive. Estradiol enanthate  Chemical Structure
  72. GC11796 Estradiol valerate Estradiol valerate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs. Estradiol valerate  Chemical Structure
  73. GC63643 Estradiol-d4 Estradiol-d4 (β-Estradiol-d4) is the deuterium labeled Estradiol. Estradiol-d4  Chemical Structure
  74. GC12182 Estriol Estrogen receptor antagonist Estriol  Chemical Structure
  75. GC60816 Estrogen receptor modulator 1 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  Chemical Structure
  76. GC14385 Estrone Estrogenic hormone Estrone  Chemical Structure
  77. GC64437 Estrone-d4 Estrone-d4  Chemical Structure
  78. GC16852 Estropipate Estrogen receptor agonist Estropipate  Chemical Structure
  79. GC12148 Ethinyl Estradiol Ethinyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethinyl Estradiol  Chemical Structure
  80. GC62484 FLTX1 FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus. FLTX1  Chemical Structure
  81. GC18000 Fulvestrant (ICI 182,780)

    Fulvestrant is a selective estrogen receptor (ER) antagonist. It binds, blocks and degrades ER, then inhibits ER-mediated transcriptional activity with an IC50 of 9.4 nM.

    Fulvestrant (ICI 182,780)  Chemical Structure
  82. GC12766 G-1

    G-1 is a selective and potent agonist of GPR30 with EC50 value about 2 nM.

    G-1  Chemical Structure
  83. GC16618 G-15

    A GPER receptor antagonist

    G-15  Chemical Structure
  84. GC32920 GDC-0927 (SRN-927) GDC-0927 (SRN-927) (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist. GDC-0927 (SRN-927)  Chemical Structure
  85. GC33193 GDC-0927 Racemate (SRN-927 Racemate) GDC-0927 Racemate (SRN-927 Racemate) (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases. GDC-0927 Racemate (SRN-927 Racemate)  Chemical Structure
  86. GC31746 Gestrinone (R 2323) An androgen and progesterone receptor ligand used to treat endometriosis Gestrinone (R 2323)  Chemical Structure
  87. GC65609 Glicoricone Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone  Chemical Structure
  88. GC65606 GNE-274 GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines.?GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research. GNE-274  Chemical Structure
  89. GC65590 GNE-502 GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer. GNE-502  Chemical Structure
  90. GC61817 GPR30 agonist-1 GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1  Chemical Structure
  91. GC10558 GSK 4716 estrogen-related receptors ERRβ and ERRγ agonist GSK 4716  Chemical Structure
  92. GC64453 GSK5182 GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182  Chemical Structure
  93. GC36201 GW7604 GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist. GW7604  Chemical Structure
  94. GN10566 Gypenoside XVII Gypenoside XVII  Chemical Structure
  95. GC33262 H3B-5942 A selective estrogen receptor covalent antagonist H3B-5942  Chemical Structure
  96. GC32406 H3B-6545 H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer. H3B-6545  Chemical Structure
  97. GC33378 H3B-6545 Hydrochloride H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer. H3B-6545 Hydrochloride  Chemical Structure
  98. GC63899 hFSH-β-(33-53) (TFA) hFSH-β-(33-53) (TFA)  Chemical Structure
  99. GC33402 Idoxifene (CB7432) Idoxifene (CB7432) (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM). Idoxifene (CB7432)  Chemical Structure
  100. GC15730 Kaempferide A flavonoid with diverse biological activities Kaempferide  Chemical Structure
  101. GC11425 Lasofoxifene (tartrate) third-generation, non-steroidal selective estrogen receptor modulator (SERM) Lasofoxifene (tartrate)  Chemical Structure

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