Estrogen receptors are a group of proteins found inside cells.They are receptors that the estrogen (17-estradiol) hormone activates. There are two classes of estrogen receptors: GPER (GPR30), a member of the rhodopsin-like family of G protein-coupled receptors, and ER, a member of the nuclear hormone family of intracellular receptors. The interactions between coactivators and corepressors, and consequently, the agonist or antagonist effect of the ligand, are heavily influenced by the ER's helix 12 domain.Different ligands may have different affinities for the estrogen receptor's alpha and beta isoforms. Estradiol binds to both receptors equally well, however raloxifene, estrone, and genistein bind preferentially to the alpha receptor. In addition to being necessary for sexual maturation and reproductive function, estrogen and its receptors also affect other tissues, like bone. In pathological conditions like osteoporosis, endometrial cancer, and breast cancer, estrogen receptors play a role. Numerous transcript variations are produced by alternative promoter use and alternative splicing, however it is unknown how many of these variants are full-length.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V3804 | GDC-0927 Racemate | 1443983-36-5 | GDC-0927 Racemate, the racemic mixture of GDC-0927, is used in the research of ER-related diseases. |
|
V67666 | GLL398 | 2077980-80-2 | GLL398 is an orally bioactive selective estrogen receptor degrader (SERD) that competitively binds to estrogen receptors with IC50 of 1.14 nM. |
|
V67714 | GNE-149 | 1953132-75-6 | GNE-149 is a potent, orally bioactive estrogen receptor alpha (ERα; IC50=0.053 nM) antagonist. |
|
V67659 | GNE-274 | 2369048-69-9 | GNE-274 is a structural analog of the ER degrading agent GDC-0927 and is a non-degrading agent. |
|
V67665 | GNE-502 | 1953134-16-1 | GNE-502 is an orally bioavailable estrogen receptor (ER) degrader. |
|
V67648 | GPR30 agonist-1 | 415919-74-3 | GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. |
|
V3533 | GSK-4716 | 101574-65-6 | GSK4716 is a novel, potent and selective estrogen-related receptor beta/gamma (ERRβ and ERRγ) agonist. |
|
V21885 | GSK5182 | 877387-37-6 | GSK5182 is a novel, potent, highly specific and orally bioactive inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. |
|
V67651 | GW7604 | 361203-06-7 | GW7604 is an antiestrogen. |
|
V67650 | Imlunestrant (LY-3484356) | 2408840-26-4 | Imlunestrant (LY-3484356) is an orally bioactive and selective estrogen receptor degrader (SERD) with purely antagonistic properties. |
|
V67652 | Imlunestrant tosylate (LY-3484356 tosylate) | 2408840-41-3 | Imlunestrant (LY-3484356) tosylate is an orally bioactive and selective estrogen receptor degrader (SERD) with purely antagonistic properties. |
|
V67706 | Inokosterone | 15130-85-5 | Inokosterone is a potentially active molecular target of estrogen receptor 1 in patients with rheumatoid arthritis. |
|
V1994 | Kaempferol (Kempferol; Robigenin) | 520-18-3 | Kaempferol (Kempferol; Robigenin), a naturally occuring flavonoid analog, is a potent ERRα (estrogen receptor α) and ERRγ inverse agonist. |
|
V3805 | LSZ102 | 2135600-76-7 | LSZ-102 is a potent, orally bioactive and selective ERα antagonist and SERD (estrogen receptordegrader) with anIC50of 0.2 nM has the potentialfor the treatment of Estrogen Receptor Positive Breast Cancer. |
|
V67693 | Millewanin G | 874303-33-0 | Millewanin G is a prenylated isoflavonoid compound with antiestrogenic activity (IC50=29 μM). |
|
V67715 | OP-1074 | 1443752-76-8 | OP-1074, a pure anti-estrogen, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity on ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcriptional activity, IC50 are 1.6 and 3.2 nM respectively. |
|
V83563 | OSU-ERb-12 | 2088837-20-9 | |
|
V67657 | Palazestrant (OP-1250) | 2092925-89-6 | Palazestrant is an antiestrogenic and anticancer agent. |
|
V3204 | PHTPP | 805239-56-9 | PHTPP is an antagonist of the ERβ (Estrogen Receptor). |
|
V67643 | Psidial A | 1207181-35-8 | Psidial A is an epimer of the sesquiterpene-diphenylmethane terpenoid. |
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