Catalog No.
Product Name
Application
Product Information
Citations
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ERα Degarder
X15695 is a selective estrogen receptor alpha (ERα) degrader that functions as an aryl hydrocarbon receptor (AHR) ligand. By facilitating the formation of a complex between AHR and ERα, X15695 promotes the proteasomal degradation of ERα, leading to the inhibition of breast cancer cell proliferation. Additionally, it induces cell cycle arrest and apoptosis. This compound is valuable for research in breast cancer biology and therapeutics. -
ERα Antagonist
ER covalent antagonist-1 is a selective antagonist of estrogen receptor α (ERα). It effectively inhibits the proliferation of ERα-positive MCF-7 cells, with an IC50 value of 0.98 μM, and promotes cell cycle arrest in the G0/G1 phase while inducing apoptosis. In vivo studies demonstrate its significant antitumor efficacy in mouse models, highlighting its potential for research in cancer therapeutics targeting estrogen signaling pathways. -
ERRγ Inverse Agonist
(E/Z)-GSK5182 is a racemic mixture of the (E)- and (Z)-isomers that acts as a selective inverse agonist of estrogen-related receptor γ (ERRγ), exhibiting an IC50 of 79 nM. This compound is notable for its ability to induce the generation of reactive oxygen species (ROS), particularly in hepatocellular carcinoma models. Due to its specificity and biological activity, (E/Z)-GSK5182 is a valuable tool for investigating ERRγ-related signaling pathways and potential therapeutic applications in cancer research. -
Estrogen Receptor Targeting Agent
Fluoroestradiol is an estrogen receptor-targeting agent utilized as a PET imaging tracer for the assessment of estrogen receptor expression. When radiolabeled with 18F, Fluoroestradiol demonstrates high uptake selectivity and an optimal target-to-background ratio, making it particularly effective in distinguishing estrogen receptor activity in various tissues. This reagent has applications in quantifying estrogen receptor expression in breast cancer and monitoring heterogeneity in ovarian cancer, as well as revealing estrogen receptor presence in normal brain tissues and meningiomas. -
PROTAC ERRα Degrader
PROTAC_ERRα is a targeted degrader of the estrogen-related receptor alpha (ERRα), employing a proteolysis-targeting chimera (PROTAC) mechanism for enhanced specificity. This compound induces over 80% proteasomal degradation of ERRα in MCF-7 cells, with a DC50 value of 100 nM. PROTAC_ERRα serves as a valuable tool for investigating the biological functions of ERRα in cancer research and for therapeutic development aimed at ERRα-related pathways. -
GPER Agonist
(3aS,4R,9bR)-G-1 is a selective agonist of the G protein-coupled receptor GPR30, exhibiting a Ki value of approximately 7 nM. This compound activates rapid signaling pathways, including intracellular calcium mobilization and PI3K signaling, which are implicated in promoting uterine epithelial cell proliferation and exhibiting antidepressant effects. (3aS,4R,9bR)-G-1 holds potential for research applications in breast cancer and depression studies. -
Estrogen Receptor Degrader
Rintodestrant is an orally active, non-steroidal selective estrogen receptor degrader. Its primary mechanism involves the degradation of estrogen receptors, leading to reduced estrogen signaling. Additionally, Rintodestrant functions as a CDK4/6 inhibitor, which may further enhance its therapeutic potential. This compound is relevant for research applications in breast cancer treatment and the study of estrogen receptor-related pathways. -
Estrogen Receptor Inhibitor
Indazole-Cl functions as a specific inhibitor of the Estrogen Receptor β, exhibiting anti-inflammatory properties. It effectively impairs the expression of cyclooxygenase-2 induced by hypoxic conditions and reduces reactive oxygen species (ROS) production. Additionally, Indazole-Cl inhibits both cell migration and invasion in response to hypoxia, making it a potent agent against hypoxia-induced inflammation in vascular smooth muscle cells. This compound is valuable for research focusing on estrogen signaling and inflammatory pathways. -
LH-R Agonist
Org 43553 is a selective luteinizing hormone receptor (LH-R) agonist characterized by its oral bioactivity and low molecular weight. It exhibits potent agonistic effects on human LH and follicle-stimulating hormone (FSH) receptors, with EC50 values of 3.7 nM and 110 nM, respectively. This compound is valuable for research focusing on endocrine signaling and receptor-mediated pathways. -
Estrogen Receptor Antagonist
6-Raloxifene-β-D-glucopyranoside functions as a selective estrogen receptor antagonist, exhibiting a strong affinity for estrogen receptors. This compound is known for its biological activities in inhibiting bone loss and resorption, as well as in reducing lipid levels. It has potential applications in research related to osteoporosis and cardiovascular health, providing insights into estrogen-related metabolic processes. -
ERα Degrader
ERα degrader 6 (Compound 31q) is a selective degrader of estrogen receptor alpha (ERα), exhibiting a binding affinity (KI) of 75 nM. It also demonstrates impressive inhibitory activity against aromatase (ARO) with an IC50 of 37.7 nM. This compound has been shown to effectively inhibit tumor growth in the MCF-7 tumor xenograft model, making it a valuable tool for breast cancer research and therapeutic studies. -
ER Degrader
ER Degrader 10 is a selective orally active degrader and antagonist of the estrogen receptor (ER), demonstrating a DC50 of 0.43 nM and an IC50 of 0.56 nM. This compound effectively inhibits the proliferation of ER-positive cancer cells, with IC50 values ranging from 0 to 15 nM. While it shows minimal inhibitory activity against the hERG channel (IC50 > 40 μM), ER Degrader 10 is capable of crossing the blood-brain barrier, with a brain/plasma ratio of 3.05. Additionally, it has demonstrated significant antitumor efficacy in mouse models, making it a valuable tool for cancer research. -
Estrogen Receptor Modulator
Fispemifene is an orally active selective estrogen receptor modulator that exhibits both anti-inflammatory and antiestrogenic properties. It has been demonstrated to reduce glandular inflammation in animal models of chronic nonbacterial prostatitis, making it a valuable tool for research in inflammatory and hormonal regulation. Its mechanism of action targets estrogen receptors, providing insights into treatment strategies for associated conditions. -
Estrogen Receptor Degrader
Taragarestrant is a selective estrogen receptor degrader (SERD) that exhibits potent oral activity. It effectively degrades estrogen receptors in various estrogen receptor-positive (ER+) breast cancer cell lines and xenograft models. This compound is valuable for research focused on targeting ER+ breast cancer and investigating therapeutic strategies for estrogen-driven malignancies. -
SERM
Bazedoxifene hydrochloride is a nonsteroidal selective estrogen receptor modulator (SERM) that targets estrogen receptors ERα and ERβ, with IC50 values of 23 nM and 99 nM, respectively. This compound exhibits significant biological activity by inhibiting IL-6/GP130 protein-protein interactions, making it valuable in osteoporosis research. Additionally, Bazedoxifene hydrochloride is also utilized in studies related to pancreatic cancer, providing insights into its therapeutic potential and mechanisms of action. -
Estrogen Receptor Degrader
ZN-c5 is a selective estrogen receptor degrader (ERD) that effectively targets both estrogen receptor alpha (ERα) and beta (ERβ) with high affinity, exhibiting IC50 values of 0.4 nM and 0.8 nM, respectively. This compound demonstrates significant potency in cellular assays, specifically in MCF-7 breast cancer cells, with an IC50 of 0.3 nM. ZN-c5 has also been shown to inhibit tumor growth in xenograft models, including MCF-7 and WHIM20, making it a valuable tool for research in breast cancer therapeutics. -
ER Degrader
GNE-502 is a potent oral degrader targeting the estrogen receptor (ER). It exhibits significant biological activity by promoting the degradation of ER, which is crucial for the regulation of breast cancer cell proliferation. This compound is valuable for research applications aimed at understanding ER signaling pathways and developing therapeutic strategies for estrogen-dependent tumors. -
Estrogen Receptor/ERR Antagonist
Giredestrant tartrate is a non-steroidal estrogen receptor (ER) antagonist, specifically targeting the ER. This compound demonstrates potent competition with estradiol for binding to the receptor, leading to a conformational alteration in the ER ligand binding domain. Giredestrant tartrate is primarily utilized in research applications focused on exploring anti-tumor mechanisms linked to estrogen signaling pathways. -
ER Antagonist
Estrogen receptor antagonist 2 is a selective downregulator of estrogen receptors, particularly targeting the estrogen receptor alpha (ERα). By inhibiting estrogen signaling, this compound may play a critical role in breast cancer research, as estrogen is a key driver of breast cancer progression. Estrogen receptor antagonist 2 is suitable for studies focused on understanding and potentially treating estrogen-dependent malignancies. -
Estrogen Receptor/ERR Modulator
Zuclomiphene-d5 citrate is a deuterium-labeled analog of Zuclomiphene citrate, functioning as an estrogen receptor modulator. This compound exhibits antiestrogenic activity and has demonstrated potential in reducing cholesterol levels. It is suitable for research applications in endocrinology and the study of metabolic diseases. -
Isomer
(R)-OP-1074 is an isomer of OP-1074, designed as a control compound for experimental studies. It serves as a valuable tool in evaluating the selective estrogen receptor degradation activity of OP-1074, a potent anti-estrogen drug. Specifically, OP-1074 acts as a selective ER degrader with demonstrated anti-estrogenic effects against both estrogen receptors ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription at IC50 values of 1.6 and 3.2 nM, respectively. Its role in research applications includes studies on hormone signaling and estrogen receptor biology. -
ERα Activator
Desketoraloxifene is a selective estrogen receptor alpha (ERα) activator that functions at an AP-1 site. This compound demonstrates significant biological activity in modulating estrogen signaling pathways, making it a valuable tool in research focused on osteoporosis and breast cancer. Its ability to selectively activate ERα provides insights into the therapeutic potential of estrogen-related treatments in these diseases. -
ER-α Binder
CHEMBL4224880 is a selective binder of estrogen receptor-alpha (ER-α), which plays a critical role in mediating estrogen signaling pathways. This compound exhibits biological activity that can influence gene expression and cellular processes associated with hormonal regulation. It is applicable in research focused on understanding hormone-driven diseases, such as breast cancer, and for the development of therapeutics targeting estrogen-related pathways. -
ERα Degrader
PVTX-321 is a potent estrogen receptor α (ERα) degrader, exhibiting an effective degradation capacity with a DC50 value of 0.15 nM in MCF-7 cells. Additionally, it demonstrates inhibitory activity against mutant ERα with an IC50 of 59 nM. This compound offers valuable research applications in the study of ER+/HER2- breast cancer, providing a mechanism for targeting estrogen receptor signaling in therapeutic contexts. -
Estrogen Receptor Modulator
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene and functions as an estrogen receptor modulator. This compound is metabolized predominantly by UGT1A1 and UGT1A8, demonstrating an IC50 of 290 μM for estrogen receptor binding. Raloxifene 6-glucuronide acts as a full agonist at nanomolar concentrations, activating the TGFβ3 promoter while also inhibiting the expression of the vitellogenin promoter that contains the estrogen response element. It is valuable in research applications involving estrogen signaling and receptor modulation. -
Estrogen Receptor Degrader
ERα degrader 5 is a selective estrogen receptor degrader (SERD) that targets estrogen receptor alpha (ERα) with a reported EC50 of 1.1 nM. This compound effectively induces degradation of ERα, demonstrating significant antitumor activity in vivo. It is a valuable tool for research focused on breast cancer and estrogen receptor signaling pathways. -
Estrogen Receptor/ERR
Conjugated estrogen sodium primarily targets estrogen receptors (ERR) and functions as a replacement therapy for menopausal symptoms. It exhibits key biological activities including alleviation of moderate to severe hot flashes and improvements in vaginal atrophy associated with decreased estrogen levels. This compound is widely used in research to investigate estrogen's physiological effects and its role in various hormonal therapies. -
Estrogen Receptor Degrader
ERα degrader 8 is a selective estrogen receptor degrader that effectively targets and degrades the estrogen receptor alpha (ERα). It demonstrates potent biological activity, exhibiting an IC50 value of 0.15 μM in MCF-7 breast cancer cells. This compound is valuable for research applications aimed at exploring mechanisms of hormone-dependent cancer progression and therapeutic strategies for ERα-positive tumors. -
GPER activator
GPER Activator 1 is a selective activator of the G protein-coupled estrogen receptor (GPER). This compound has been shown to exhibit dual inhibition of inflammation induced by TNFα and IL-6, making it a valuable tool for investigating the role of GPER in inflammatory responses. Its non-cytotoxic nature further supports its application in various biological research settings. -
Antiestrogenic Compound
Trioxifene mesylate is an antiestrogenic compound that exhibits mixed agonist-antagonist activity on estrogen receptor target tissues. This unique profile enables it to modulate estrogen signaling, making it a valuable tool for studying estrogen-related biological processes. Trioxifene mesylate is primarily utilized in cancer research, particularly in investigations of estrogen receptor-positive malignancies and therapeutic strategies for breast cancer. -
ER modulator
Estrogen Receptor Modulator 7 is a selective modulator targeting estrogen receptors, exhibiting significant activity in altering receptor signaling pathways. It serves as a valuable tool for investigating the role of estrogen in cancer biology, particularly in studies examining hormone-driven tumors. This compound facilitates research into therapeutic approaches for estrogen-related malignancies. -
Estrogenic Substance
4-Chlorodiphenyl ether is an estrogenic compound that mimics the action of endogenous estrogens. It has been shown to support the survival of endometriotic cysts and is linked to the proliferation of endometriotic implants. This reagent is valuable for research focused on understanding the mechanisms of endometriosis and the role of estrogenic substances in this condition. -
ER Degrader
ER Degrader 2 is a potent degrader of the estrogen receptor (ER), which is crucial for regulating various cellular processes such as growth, differentiation, and apoptosis. This compound is particularly relevant for cancer research, especially in studies focused on hormone-dependent malignancies. By selectively targeting ER, ER Degrader 2 facilitates the investigation of estrogen signaling pathways and their implications in oncogenesis. -
ERβ Agonist
WAY-166818 is a synthetic nonsteroidal estrogen that acts as a selective agonist of estrogen receptor beta (ERβ). This compound exhibits prominent biological activity related to the modulation of estrogenic signaling pathways, making it valuable for studying ERβ functions in various physiological and pathological contexts. Its application extends to research in areas such as reproductive biology, cancer, and cardiovascular health. -
Estrogen Agonist
4',2-Dihydroxy-4,6-dimethoxydihydrochalcone is an estrogen agonist that demonstrates binding affinity for the bovine uterine estrogen receptor, exhibiting an IC50 of 15 μM. This compound is valuable for research applications related to estrogen signaling pathways and can be utilized in studies investigating hormone-related biological processes, including cell proliferation and differentiation. Its structural characterization enables further exploration in drug discovery and developmental biology. -
Estradiol Prodrug
Estradiol acetate is an orally active prodrug of estradiol, designed to be converted into its active form in the body. It exhibits significant activity in alleviating the frequency and severity of symptoms associated with menopause. This compound is valuable for research focused on understanding and treating menopausal symptoms and related hormonal changes. -
GDC-0927 (R)-enantiomer
(R)-GDC-0927 is the (R)-enantiomer of GDC-0927, a potent inhibitor of the Src family kinases. This compound exhibits significant biological activity in modulating cell signaling pathways involved in cancer progression and metastasis. It is utilized in research related to oncogenesis, therapeutic targets in cancer biology, and the exploration of kinase inhibitors for potential therapeutic applications. -
ERβ Agonist
(S)-STO021 is a selective agonist of estrogen receptor beta (ERβ), demonstrating oral bioactivity. This compound exhibits a dual mechanism by inhibiting osteoclast activity while promoting osteoblast function, making it a valuable tool for research into osteoporosis and bone health. Its specific action on ERβ positions (S)-STO021 as a potential candidate for studying therapeutic strategies in bone-related disorders. -
Herbal Remedy
Cimicifuga racemosa extract exhibits antiestrogenic properties originating from the plant Cimicifuga racemosa. This extract is primarily utilized for its potential to alleviate menopausal symptoms, including hot flashes and night sweats. It serves as a valuable resource in research focused on herbal remedies and their applications in women's health. -
ER Antagonist
Estrogen Receptor Antagonist 1 is a selective antagonist of the estrogen receptor, primarily targeting the estrogen receptor alpha (ERα). This compound exhibits significant biological activity in inhibiting estrogen (E2) signaling, which plays a crucial role in the progression of breast cancer. Estrogen Receptor Antagonist 1 is intended for research applications focused on breast cancer pathology and therapeutic interventions. -
ERα Degrader
ERα Degrader 11 is a selective degrader targeting the estrogen receptor alpha (ERα). This compound effectively facilitates the degradation of ERα, making it a valuable tool for probing estrogen receptor status in ER-positive breast cancer cells. Its specific action allows researchers to investigate the role of ERα in cancer biology and develop targeted therapeutic strategies. -
ERα Inhibitor
VPC-16606 is a selective inhibitor of the estrogen receptor alpha (ERα), specifically targeting its activation function 2 (AF2) domain. This compound effectively disrupts the interaction between ERα and coactivators, inhibiting the activity of both wild-type and drug-resistant mutant forms of ERα. VPC-16606 demonstrates significant potency against hormone-resistant breast cancer cells, making it a valuable tool for research in breast cancer mechanisms and therapeutic development. -
ERα Degrader
F0840-0093 is a selective estrogen receptor α (ERα) degrader. It demonstrates potent antiproliferative activity against T47D breast cancer cells, with an IC50 value of 4.65 μM. This compound holds promise for advancing research in estrogen receptor-positive (ER+) breast cancer therapies. -
Anticancer Agent
Tamoxifen analog II is a cyclopropyl derivative of Stilbene, functioning as a nonsteroidal antiestrogen. It exhibits notable antiestrogenic activity, effectively inhibiting the growth of DMBA-induced rat mammary tumors. This compound is valuable for research applications focused on cancer biology and the evaluation of therapeutic strategies in breast cancer treatment. -
ERβ Agonist
FERb 033 is a selective and potent estrogen receptor beta (ERβ) agonist with a Ki value of 7.1 nM and an EC50 of 4.8 nM. This compound demonstrates remarkable 62-fold selectivity over the estrogen receptor alpha (ERα), making it a valuable tool for research applications focused on ERβ signaling pathways. FERb 033 is useful for studies related to hormone regulation, endocrine system research, and potential therapeutic interventions involving estrogen receptors. -
FSH Negative Allosteric Modulators
ADX68692 is a selective negative allosteric modulator of the follicle-stimulating hormone (FSH) receptor, exhibiting a log IC50 of -5.71. This compound effectively inhibits hCG-induced cAMP production and β-arrestin 2 recruitment in HEK293 cells. ADX68692 demonstrates partial efficacy in mLTC-1 and primary rat Leydig cells, leading to reduced FSHR-mediated cAMP, progesterone, and estradiol production. Additionally, it has been shown to decrease the number of oocytes recovered from the ampullae, making it a valuable tool for studying reproductive biology and hormonal regulation. -
Estrogen Derivative
J 628 is an estrogen derivative that primarily targets estrogen receptors. It exhibits antifertility effects and is utilized in research to explore reproductive health and associated mechanisms in animal models such as mice, rats, and rabbits. This compound serves as a valuable tool for investigating the physiological impacts of estrogen signaling and its implications for fertility regulation. -
Estrogen Receptor/ERR
RU-39411 is a steroidal anti-estrogen that targets the estrogen receptor (ERR) with mixed estrogenic and antiestrogenic properties. It demonstrates significant inhibitory effects on cell proliferation in the MCF-7 breast cancer model, linked to its binding affinity for the estrogen receptor. RU-39411 effectively downregulates the estrogen binding capacity in cells without altering estrogen receptor mRNA levels, suggesting that the incorporation of its side chain modifies typical steroidal estrogen antagonist behavior. Additionally, RU-39411 promotes the synthesis of progesterone receptors, supporting its role as an active estrogen. -
Estrogen Receptor Antagonist
Enclomiphene hydrochloride is a potent non-steroidal estrogen receptor antagonist. It exhibits antioestrogenic properties, making it valuable for research into ovarian dysfunction, testosterone deficiency, male hypogonadism, and type 2 diabetes. This compound's mechanism of action supports its use in exploring endocrine disorders and developing potential therapeutic strategies in related conditions. -
Estrogen Receptor Antagonist
4'-Raloxifene-β-D-glucopyranoside is a selective estrogen receptor antagonist, primarily targeting estrogen receptors to modulate their activity. This compound is a metabolite of Raloxifene and exhibits orally active properties, making it effective in research related to osteoporosis by inhibiting bone loss and resorption. Additionally, it has potential applications in studies focused on lipid metabolism and the management of lipid levels.
