Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
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[1].
ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
GDC-0810 is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer[1].
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[1][2].
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor[1].
ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER), with an DC50 of 0.17 nM in MCF-7 cells[1].
Miroestrol is a highly active phytoestrogen. Miroestrol can produce mammogenic effect. Miroestrol exhibits bone loss prevention and neuroprotective in ovariectomized mice. Miroestrol also can reduce cancer risk[1][2][3][4].
Tamoxifen is a 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.
(-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
Estrogen receptor modulator 10 (compound G-5b) is an Estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 can induce apoptosis. Estrogen receptor modulator 10 can block cells at the G1/G0 phase. Estrogen receptor modulator 10 can be used in cancer studies[1].
Ospemifene is a selective estrogen for the prevention of postmenopausal osteoporosis with IC50 values of 827nM and 1633nM for ERα and ERβ, respectively. target: ERα and ERβIC50:827 and 1633 nm for ERα and -β, respectively[1] IN vitro: The estrogen-dependent MCF-7 human breast cancer cells were used as a model for studies on the effects of Ospemifene on breast cancer cells. The addition of the compound at concentrations of 0.1 nm to 10 μm did not cause a significant increase in MCF-7 cell growth in vitro when studied by measuring ATP or 3-[4,5-dimethylthiazol-2-yl]2,5-diphenyltetrazolium bromide levels, cell numbers, and rate of [3H]thymidine incorporation during a 7-day culture period. On the other hand, the compound did not inhibit the growth stimulation caused by 1 nm estradiol, except at a concentration 10 mm by only 30%. Similar results were obtained with ZR 75–1 cells, another estrogen-dependent human breast cancer cell line. The cytotoxicity of FC1271a at high concentrations was therefore markedly lower than that for TAM, TOR, or RAL.[1]In ER+ MCF-7 cells, TOR VI and FC-1271a exhibited anti-estrogenic activity. The anti-estrogenic effects of these compounds were less potent as anti-estrogens when compared with TOR and RAL.[2]"In vivo: In the DMBA rat mammary carcinoma model, Ospemifene showed a clear antitumor effect that seemed to be caused primarily by a decrease in the appearance of new tumors but also by a retardation of tumor progression without stimulating the growth of human breast cancer cells.[1]Tumor growth was shown to be inhibited at these doses, indicating anti-estrogenic activity at all doses including 50 and 100 mg/kg Ospemifene. By the end of treatment, MCF-7 tumors in Ospemifene treated mice were statistically smaller compared with control tumors.[2]
Gypenoside XVII, a novel phytoestrogen belonging to the gypenosides, can activate estrogen receptors.
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist[1].
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property[1].
SLU-PP-1072 is a dual ERRα/γ inverse agonist, used in Prostate cancer (PCa) research. SLU-PP-1072 disrupts PCa cell metabolism, and induces apoptosis via dysregulating cell cycle[1].
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].
Dehydrodiconiferyl alcohol is an estrogen receptor agonist that can promote BMP-2-induced osteoblastogenesis. Dehydrodiconiferyl alcohol also exerts anti-inflammatory activity through inactivation of NF-κB pathways[1][2].
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[1][2].
Enclomiphene ((E)-Clomiphene) is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes[1].
Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity.
AZD9496 maleate is a potent and selective estrogen receptor (ERα)antagonist with IC50 of 0.28 nM.
Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC50s of 13, 5µM for ERα and Erβ, respectively[1].
Endoxifen hydrochloride, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor.
Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability[1][2][3][4].