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
- Cat.No. Product Name Information
- GC38990 Lindleyin Lindleyin, isolated from Rhei rhizoma, mediates hormonal effects through estrogen receptors.
- GN10673 Liquiritigenin
- GC19224 LSZ-102 LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM.
- GC13477 Mestranol Estrogen used in contraceptives
- GC31589 MK-6913 (Tetrahydrofluoroene 52) MK-6913 (Tetrahydrofluoroene 52) (Tetrahydrofluoroene 52) is a potent and selective estrogen receptor β agonist.
- GC38931 N-Desmethyltamoxifen hydrochloride N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
- GC32445 Nitromifene (CI628) Nitromifene (CI628) is an antagonist of estrogen receptor (ER).
- GC31565 NNC45-0781 NNC45-0781 is a tissue-selective estrogen partial-agonist.
- GC64345 OP-1074 OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2?nM, respectively.
- GC11996 Ospemifene non-hormonal selective estrogen receptor modulator (SERM)
- GC48613 Ospemifene-d4
- GC34151 PAC PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
- GC11863 PHTPP estrogen ERβ receptor antagonist
- GC34153 Pipendoxifene hydrochloride Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer.
- GC14370 PPT PPT (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of PPT for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
- GC44686 Prochloraz Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death.
- GC34733 PROTAC ER Degrader-2 PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
- GC34734 PROTAC ER Degrader-3 PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
- GC64350 PROTAC ER Degrader-4 PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.
- GC34735 PROTAC ERα Degrader-2
- GC34341 PROTAC ERα Degrader-1 PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
- GC62307 PROTAC ERRα Degrader-3 PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
- GC38383 PROTAC ERRα ligand 2 PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
- GC36983 PROTAC ERRalpha Degrader-1 PROTAC ERRalpha Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.
- GC36984 PROTAC ERRalpha Degrader-2 PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.
- GC12644 Quinestrol synthetic estrogen that is effective in hormone replacement therapy
- GC44804 Raloxifene 4'-Glucuronide Raloxifene 4'-glucuronide is a metabolite of the selective estrogen receptor modulator raloxifene.
- GC44805 Raloxifene 6-Glucuronide Raloxifene 6-glucuronide is a metabolite of the selective estrogen receptor modulator raloxifene.
- GC13350 Raloxifene HCl Raloxifene HCl (Keoxifene hydrochloride) is a second generationselective and orally active estrogen receptor modulator.
- GC63464 Rintodestrant Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.
- GN10164 Saikosaponin D
- GC63185 Segetalin B Segetalin B, a cyclopentapeptide from Vaccaria segetalis, possesses estrogen-like activity.
- GC37657 SNIPER(ER)-110 SNIPER(ER)-110 consists of a IAP ligand and an estrogen ligand, connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively.
- GC17901 Tamoxifen Tamoxifen(TAM) serves as a selective estrogen receptor regulator (SERM), inhibiting estrogen's effects in breast cells while potentially stimulating estrogen activity in cells found in different tissues.
- GC11669 Tamoxifen Citrate Antiestrogen drug
- GC48124 Tamoxifen-d5 An internal standard for the quantification of tamoxifen
- GC67695 Taragarestrant meglumine
- GC41153 Tibolone Tibolone is an estrogen-like compound used for the treatment of the symptoms associated with menopausal transition (i.e., climacteric symptoms) and also for the treatment of osteoporosis.
- GC11544 Toremifene
- GC13835 Toremifene Citrate Oral selective estrogen receptor modulator (SERM)
- GC63329 Toremifene-d6 citrate
- GC38974 Tracheloside Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.
- GC13309 WAY 200070 ERβ receptor agonist
- GC10789 XCT790 ERRα agonist
-
GC70159
Yp537 TFA
Yp537 TFA is an estrogen receptor (ER) inhibitor that can prevent dimerization of human estrogen receptors.
- GC10684 Zearalanone estrogen receptor agonist
- GC61390 Zuclomiphene citrate Zuclomiphene citrate is a cis isomer of Clomiphene citrate.
- GC61391 Zuclomiphene D4 citrate
- GC11734 α-Zearalenol estrogen receptor agonist
-
GC19498
β-Estradiol 17-acetate
β-Estradiol 17-acetate is a metabolite of estradiol