Catalog No.
Product Name
Application
Product Information
Citations
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Raloxifene Analogue
LY88074 is a Raloxifene analog that lacks the basic side chain. This compound acts as a selective estrogen receptor modulator, exhibiting key biological activity in reducing fracture risk through mechanisms that enhance the mechanical properties of bone. It operates independently of both cells and estrogen receptors, making it a valuable tool for research into bone health and osteoporotic conditions. -
Estrogen Receptor/ERR
ZK164015 is an estrogen-glucocorticoid receptor chimera that primarily targets the estrogen receptor (ER). This compound serves as a valuable screening tool to assess tissue-selective estrogen activity and has been utilized to investigate ER function in osteoblasts. Studies involving osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cell lines demonstrated that ZK164015 modulates ERE-luciferase reporter activity and influences nuclear mobility, revealing its distinct effects in response to ER agonists. -
Estrogen Receptor Ligand
4,4'-Iminodiphenol is a selective estrogen receptor ligand that acts on the estrogen receptor signaling pathways. This compound is primarily utilized in research applications aimed at understanding estrogen-mediated biological processes and receptor interactions. Its structural characteristics may provide insights into the design of novel therapeutics targeting estrogen receptors. -
ERβ Agonist
CIDD-0149897 is a potent and selective agonist for estrogen receptor beta (ERβ). This compound has demonstrated anti-tumor activity in glioblastoma, making it a valuable tool for research into cancer biology and potential therapeutic applications. Its ability to penetrate the blood-brain barrier enhances its applicability in neurological studies and treatments targeting ERβ. -
SERM/Estrogen Receptor Modulator
GW7604 is a selective estrogen receptor modulator (SERM) that acts as a potent antagonist of the estrogen receptor (ER). As a metabolite of GW5638, it demonstrates high affinity for ERs, inhibiting estrogenic activity. This compound is widely utilized in research focused on understanding the role of estrogens in various disease states and for exploring potential therapeutic interventions in hormone-dependent conditions. -
Estrogen Receptor/ERR Inhibitor
Elacestrant (S enantiomer) is a selective estrogen receptor (ERR) inhibitor known for its oral bioavailability. This compound exhibits differential inhibition with IC50 values of 48 nM for ERα and 870 nM for ERβ, demonstrating its potential as a targeted therapeutic agent in estrogen-related disorders. Its application in research includes studies focused on elucidating estrogen signaling pathways and developing treatments for hormone-responsive cancers. -
Medical Intermediate
6-Dehydronandrolone acetate is a pivotal chemical intermediate employed in the synthesis of Fulvestrant, an estrogen receptor antagonist. This compound plays a significant role in breast cancer research, aiding in the investigation of hormone receptor targeting therapies. Its utility in the development of therapeutic agents makes it a valuable resource for researchers focused on oncological applications. -
ERα Agonist/ERβ Antagonist
(R,R)-THC is a selective estrogen receptor alpha (ERα) agonist and estrogen receptor beta (ERβ) antagonist, exhibiting Ki values of 9.0 nM for ERα and 3.6 nM for ERβ. This compound demonstrates higher binding affinity for ERβ than for ERα, with respective values of 25 nM and 3.6 nM. (R,R)-THC is valuable for research applications exploring estrogen receptor signaling pathways and investigating the differential roles of ERα and ERβ in various biological processes. -
Estrogen Receptor/ERR Inhibitor
Elacestrant S enantiomer dihydrochloride is a selective estrogen receptor (ERR) inhibitor that targets the estrogen receptor with distinct pharmacological properties. This compound demonstrates reduced biological activity compared to its R enantiomer, offering potential applications in the study of estrogen signaling pathways. It serves as a valuable tool for researchers investigating the role of estrogen receptors in various biological processes and the development of therapies for estrogen receptor-positive cancers. -
ERRα Modulator
DK1 is a selective modulator of the estrogen-related receptor alpha (ERRα). It demonstrates significant biological activity by reducing blood glucose levels, making it a valuable tool for studying metabolic pathways. This compound holds potential for research applications in diabetes and related disorders. -
Estrogen Receptor Modulator
LY117018 is a selective estrogen receptor modulator (SERM) and an analog of Raloxifene. It exhibits significant antiproliferative activity on breast cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic applications targeting estrogen receptor pathways. This compound can be utilized in studies investigating the modulation of estrogen receptor activity in various cancer models. -
Estrogen Receptor Antagonist
Acolbifene hydrochloride is a selective estrogen receptor modulator (SERM) that acts as an estrogen receptor antagonist. It effectively inhibits estradiol (E2)-induced transcriptional activity of the estrogen receptors ERα and ERβ, with IC50 values of 2 nM and 0.4 nM, respectively. This compound demonstrates strong antiestrogenic activity in both the mammary gland and uterus, highlighting its potential in cancer prevention research and exploration of anticarcinogenic properties. -
Estrogen Receptor/ERR
Cancer-Targeting Compound 1 selectively targets the estrogen receptor (ER), playing a crucial role in the modulation of estrogen-related pathways associated with hormone-driven cancers. This compound is valuable for research focused on the understanding of estrogen receptor signaling and its implications in the development and progression of breast cancer and other hormone-responsive tumors. Through its precise action on the ER, it aids in exploring potential therapeutic strategies and enhancing the knowledge of cancer biology. -
Erα Biomodulator
(Rac)-ErSO-DFP is a selective small molecule biomodulator that targets estrogen receptor alpha (Erα). This compound enhances the Erα-dependent adaptive unfolded protein response (a-UPR), demonstrating potential therapeutic effects against ERα-positive breast cancer, including tumors that exhibit resistance to conventional treatments. Its mechanism suggests possible applications in cancer research and the development of targeted therapies for estrogen-responsive malignancies. -
Estrogen Receptor α Inhibitor
Raloxifene 6-Monomethyl Ether is a derivative of Raloxifene that selectively inhibits Estrogen Receptor α. This compound demonstrates significant biological activity, with an IC50 of 250 nM against MCF-7 breast cancer cells, leading to a pIC50 of 6.6. It is a valuable tool for research in hormone-dependent cancer studies and may provide insights into therapeutic strategies targeting estrogen signaling pathways. -
Estrogen Receptor Modulator
Raloxifene 4'-glucuronide is a major metabolite of Raloxifene that functions as a selective estrogen receptor modulator. It primarily interacts with the estrogen receptor, demonstrating an IC50 of 370 μM. This compound activates the TGFβ3 promoter as a full agonist at nanomolar concentrations while inhibiting expression of the estrogen response element-containing vitellogenin promoter. Raloxifene 4'-glucuronide is useful for research applications in understanding estrogenic activity and signaling pathways. -
ER inhibitor
4,4'-Oxydiphenol is a known estrogen receptor inhibitor, exhibiting an IC50 value of 60 μM. This compound manifests significant biological activity by modulating estrogen signaling pathways, making it a useful tool for exploring estrogen receptor-related mechanisms. It is pertinent for research applications in cancer biology, particularly in studies focused on hormone-dependent tumors and endocrine regulation. -
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.
