Catalog No.
Product Name
Application
Product Information
Citations
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ER-α Degrader
Bexirestrant is an orally bioavailable ER-α degrader that targets estrogen receptor alpha for degradation. This compound exhibits significant antiestrogenic and antineoplastic activities, making it a valuable tool in studies of estrogen-related cancers. Bexirestrant is ideal for research focused on therapeutic strategies in hormone-driven malignancies. -
Estrogen Receptor Modulator
Y134 is a selective estrogen receptor modulator (SERM) that exhibits significant antagonist activity against both ERα and ERβ. With a remarkable 121.1-fold selectivity for ERα (Ki=0.09 nM) compared to ERβ (Ki=11.31 nM), Y134 effectively inhibits estrogen-stimulated proliferation in ER-positive human breast cancer cells. This compound is valuable for research applications focused on breast cancer biology and the modulation of estrogenic signaling pathways. -
Estrogen Receptor/ERR Agonist
Zeranol is an estrogen receptor agonist derived from the mycoestrogen zearalenone. It exhibits potent estrogenic activity, making it valuable in research focused on endocrine function and estrogen signaling. Additionally, Zeranol is utilized in agricultural studies as a growth promoter in livestock, providing insights into its effects on animal physiology and growth enhancement. -
Selective ER Degrader (PA-SERD)
OP-1074 is a selective estrogen receptor degrader (PA-SERD) that exhibits potent anti-estrogenic activity against both estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). It effectively inhibits 17β-estradiol (E2)-stimulated transcription, demonstrating IC50 values of 1.6 nM for ERα and 3.2 nM for ERβ. This compound is valuable for research applications focused on hormonal signaling pathways and targeting estrogen-related cancers. -
Partial ER Agonist
GNE-274 is a selective partial estrogen receptor (ER) agonist that enhances the chromatin accessibility of ER-DNA binding sites, distinguishing it from traditional ER degrader compounds. This compound functions by inhibiting the ligand-binding domain (LBD) of ER, making it a valuable tool in breast cancer research. GNE-274 offers insights into ER signaling pathways and can be instrumental in studies investigating ER-mediated gene regulation and cancer progression. -
Estrogen Receptor Modulator
Endoxifen (E-isomer) is an estrogen receptor modulator that primarily exerts its effects through antiestrogenic activity. This compound is of interest in cancer research, particularly in the study of hormone-dependent tumors, as it can inhibit the growth of estrogen-responsive tissues. Endoxifen (E-isomer) is often utilized in research to explore therapeutic strategies in breast cancer treatment. -
Estrogen Receptor/ERR Activator
Lindleyin is an estrogen receptor (ER) activator derived from Rhei rhizoma. It exhibits estrogenic activity by specifically binding to the ERα subtype, thereby mediating hormonal effects. This compound is useful for research related to hormonal signaling, women's health, and estrogen receptor-related pathways. -
Estrogen Receptor/ERR Modulator
Zuclomiphene citrate is a cis isomer of Clomiphene citrate that functions as an estrogen receptor modulator. This compound exhibits antiestrogenic activity and has been shown to reduce cholesterol levels. Its unique properties make Zuclomiphene citrate valuable in studies related to endocrinology and metabolic diseases, providing insights into hormonal regulation and metabolic pathways. -
Estrogen Receptor Modulator
Estrogen receptor modulator 1 is a selective estrogen receptor modulator (SERM) that demonstrates oral bioactivity with a pIC50 of 0.46. This compound effectively induces regression of Tamoxifen-resistant and hormone-independent xenograft tumors, making it a valuable tool for studying estrogen receptor signaling pathways and tumor resistance mechanisms. Its unique properties support research in cancer therapeutic strategies targeting estrogen receptors. -
Estrogen Receptor Inhibitor
Estrogen receptor-IN-1 is a potent inhibitor of the estrogen receptor (ER), demonstrating IC50 values of 13 µM for ERα and 5 µM for ERβ. This compound is utilized in research to investigate estrogen signaling pathways and the role of estrogen receptors in various biological processes, including cancer progression and hormone-related disorders. Its selective inhibition provides a valuable tool for studying ER function and therapeutic potential in related diseases. -
Selective Estrogen Receptor Degrader
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that effectively targets the estrogen receptor (ER) with an IC50 of 1.14 nM. It demonstrates significant binding affinity to the ER Y537S mutant (IC50 = 29.5 nM), making it a valuable tool for research applications in oncology. GLL398 has shown its ability to inhibit tumor growth in xenograft models of breast cancer, highlighting its potential for therapeutic strategies in ER-positive breast cancer. -
ERα Degrader
ERα degrader-2 is a selective estrogen receptor degrader (SERD) that exhibits potent binding affinity for the estrogen receptor alpha (ERα) with an IC50 of 17.1 nM and demonstrates robust degradation efficacy with an EC50 of 0.3 nM. This compound possesses favorable pharmacokinetic properties, making it a valuable tool for studying HER2-positive breast cancer. ERα degrader-2 is suitable for applications in cancer research, particularly in investigating therapeutic strategies targeting ERα signaling pathways. -
GPER Agonist
LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). This compound facilitates the activation of downstream signaling pathways, notably enhancing the production of cyclic adenosine monophosphate (cAMP) and stimulating the cAMP response element-binding protein (CREB) pathway. LNS8801 demonstrates anti-tumor properties, including the inhibition of tumor cell proliferation, induction of cell differentiation, and enhancement of tumor immunogenicity. Its research applications are relevant across various cancer types, such as melanoma, pancreatic cancer, colorectal cancer, and lung cancer, as well as investigations into the physiological and pathological roles of GPER. -
Estrogen Receptor/ERR Modulator
Zuclomiphene-d4 citrate is a deuterium-labeled analog of Zuclomiphene citrate, which acts as an estrogen receptor modulator. Exhibiting antiestrogenic properties, it is orally active and has been shown to reduce cholesterol levels. This compound is useful in research focused on endocrinology and metabolic diseases, providing insights into estrogen-related hormonal pathways and their physiological effects. -
Estrogen Receptor Modulator
LY117018 TFA is a selective estrogen receptor modulator with a structure similar to Raloxifene. It demonstrates significant antiproliferative activity in breast cancer cell lines, making it a valuable tool for research on estrogen receptor-related pathways. This compound can be utilized in studies aimed at understanding the modulation of estrogen receptor activity and its implications in cancer therapy. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Androgen Receptor Antagonist
Androgen Receptor Allosteric Antagonist 1 is a competitive allosteric inhibitor of the androgen receptor, exhibiting a Ki of 9 μM. This compound effectively inhibits R1881-mediated transcriptional activity and cell proliferation, making it a valuable tool for studying prostate cancer. Its unique mechanism of action allows for detailed exploration of androgen receptor signaling pathways in cancer research. -
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. -
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. -
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 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. -
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 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. -
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. -
Estrogen Receptor Modulator
Levormeloxifene fumarate is a stable salt form of Levormeloxifene, functioning as an estrogen receptor modulator. It is particularly significant in the prevention of postmenopausal bone loss, demonstrating key biological activity in bone density preservation. This compound is of interest in research focused on osteoporosis and other estrogen-related conditions. -
Estrogen Receptor Antagonist
Estrogen Receptor Antagonist 8 functions as a potent antagonist of the estrogen receptor, exhibiting significant in vivo anti-uterotrophic activity with an EC50 of 4.160 μM. This compound is valuable for research applications aimed at understanding estrogen signaling pathways and developing hormone-related therapies. Its ability to inhibit estrogen receptor activity makes it a crucial tool in investigations of endocrine disruption and related biological processes. -
Estrogen Receptor Degrader
ER Degrader 12 is an estrogen receptor (ER) degrader with demonstrated IC50 values of 2.3 nM for ERα and 80.2 nM for ERβ, as shown in TR-FRET assays. This compound effectively inhibits the proliferation of MCF-7 breast cancer cells, exhibiting an IC50 of 1.53 nM. ER Degrader 12 is primarily utilized in research applications focused on understanding breast cancer biology and therapeutic strategies targeting estrogen signaling pathways. -
Estrogen Receptors Modulator
Psidial A is a selective estrogen receptor modulator derived from the epimer of a sesquiterpenoid-diphenylmethane meroterpenoid. This compound exhibits significant interactions with estrogen receptors, suggesting potential applications in cancer research, particularly in targeting estrogen-dependent pathways. Its unique structure and activity make it a valuable tool for investigating estrogen-mediated biological processes and therapeutic strategies in oncology. -
ERα Degrader
ERα Degrader 13 is a potent degrader of estrogen receptor alpha (ERα) with an IC50 value of 0.55 μM. This compound effectively induces tumor regression in breast cancer xenograft mouse models, making it a valuable tool for studying ERα-related signaling and therapeutic approaches in breast cancer. Its targeted degradation mechanism provides insights into the role of ERα in cancer progression and treatment resistance. -
ER Degrader
ER Degrader 13 is an estrogen receptor (ER) degrader that effectively induces the degradation of ER, thereby reducing its activity. This compound demonstrates a substantial inhibitory effect on the proliferation of estrogen receptor-positive breast cancer MCF-7 cells. ER Degrader 13 is utilized in research focused on targeted cancer therapies and mechanisms of hormone-driven cancers.
