Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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 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. -
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. -
Antiestrogenic Agent
2-Hydroxyestrone is a specific receptor-mediated antiestrogenic agent that plays a significant role in modulating estrogen-related pathways. This compound exhibits anticarcinogenic properties, making it valuable in cancer research and therapeutic studies. Its ability to interact with estrogen receptors positions it as a key reagent for investigating the effects of estrogen in various biological contexts. -
Estrogen Receptor/ERR Inhibitor
BHPI is a selective inhibitor of the estrogen receptor ERα, regulating downstream signaling pathways by activating phospholipase C gamma (PLCγ) and inducing the unfolded protein response (UPR). This compound exhibits significant antitumor activity, making it relevant for research in breast, endometrial, and ovarian cancers. Its ability to modulate estrogen-related signaling pathways positions BHPI as a valuable tool in the study of hormone-driven malignancies and therapeutic interventions. -
REV-ERB Agonist
STL1267 is a potent REV-ERB agonist, demonstrating a Ki value of 0.16 µM for REV-ERBα. This compound effectively crosses the blood-brain barrier and has been shown to inhibit the gene expression of BMAL1. STL1267 is an invaluable tool for research into circadian rhythms and metabolic processes. Its lack of cytotoxicity further enhances its suitability for in vitro studies. -
REV-ERBα/β Antagonist
BE2012 is a potent and selective antagonist of REV-ERBα and REV-ERBβ, exhibiting EC50 values of 0.285 μM and 0.346 μM, respectively. By binding to the ligand-binding domain of REV-ERB, BE2012 inhibits the recruitment of co-inhibitory factors, leading to the release of transcriptional repression on downstream target genes. This compound has been demonstrated to upregulate myogenic transcription factors, such as Myf5 and Myod, and is applicable in research focused on muscle regeneration and repair in models of acute muscle injury. -
REV-ERB-specific Synthetic Ligand
SR12418 is a synthetic ligand that specifically targets REV-ERBα and REV-ERBβ, exhibiting IC50 values of 68 nM and 119 nM, respectively. This compound is valuable for studying the role of REV-ERBs in various biological processes and is particularly applicable in research related to experimental autoimmune encephalomyelitis (EAE) and colitis. Researchers can leverage SR12418 to investigate its potential therapeutic effects and the underlying mechanisms involved in these inflammatory conditions. -
REV-ERB Inverse Agonist
GSK1362 is a selective inverse agonist of REV-ERB, targeting the disruption of its interaction with repressive co-modulators such as NCoR1, SMRT2, and RIP140. By promoting the transcriptional activity of BMAL1, GSK1362 alleviates the repression caused by endogenous REV-ERB ligands. This compound has been shown to reduce LPS-induced inflammatory cytokine expression and inhibit IL-1β-induced Cxcl5 transcription in various cell types, making it a valuable tool for research into inflammatory diseases. -
Estrogen Receptor/ERR PTORAC
PROTAC ER Degrader-14 is a PTORAC-type degrader targeting the Estrogen Receptor (ER). This compound facilitates the degradation of ER through the recruitment of E3 ubiquitin ligase, effectively modulating estrogen signaling pathways. The specific design incorporates a linker derived from N-Boc-piperazine, combined with a ligand that binds to the target protein, enhancing selectivity and efficacy. It is applicable in studies focused on estrogen-related diseases, providing insights into cellular mechanisms and potential therapeutic interventions. -
PROTAC ER Degrader
PROTAC ER Degrader-10 is a selective PROTAC aimed at degrading estrogen receptors (ERs) within cancer cells. This compound exhibits significant efficacy in promoting targeted degradation of the ER, thereby disrupting cellular pathways linked to tumor growth and survival. Its primary application lies in cancer research, striving to elucidate mechanisms of ER-mediated signaling and provide insights into potential therapeutic strategies for estrogen-dependent malignancies. -
ERRα PROTAC Degrader
His-TERRα is a targeted degrader designed for estrogen receptor-related alpha (ERRα) via the PROTAC mechanism. Utilizing a histidine residue as the E3 ligase ligand, it engages the N-end rule pathway to facilitate the degradation of ERRα, effectively diminishing its presence in cells. His-TERRα demonstrates potent inhibition of proliferation and migration in MCF7 breast cancer cells, making it a valuable tool for investigating breast cancer biology and therapeutic strategies. -
ERα Protac Degrader
Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader that induces the degradation of ERα through the ubiquitin-proteasome pathway, utilizing the E3 ubiquitin ligase N-recognin 5. This compound presents significant potential for cancer research by modulating estrogen receptor signaling. Its unique design combines inhibition and degradation strategies, making it a valuable tool for studying ERα-related pathways and therapeutic interventions in estrogen-dependent cancers. -
ER Degrader
PROTAC ER Degrader-11 is a potent PROTAC designed to target estrogen receptor (ER) degradation, with an IC50 of 0.66 nM. This compound plays a critical role in cancer research by modulating ER levels, providing valuable insights into ER-related signaling pathways and therapeutic strategies. Its unique structure includes a Cereblon ligand and a specific linker, making it a valuable tool for exploring targeted protein degradation in cancer biology. -
PROTAC ER Degrader
SNIPER(ER)-87 is a PROTAC compound designed to efficiently degrade estrogen receptor α (ERα) through targeted ubiquitination. It consists of an IAP ligand (LCL161 derivative) linked to the ERα ligand (4-hydroxytamoxifen) via a PEG linker, resulting in an IC50 of 0.097 μM for ERα degradation. This compound preferentially recruits XIAP, the primary E3 ubiquitin ligase, to facilitate the selective degradation of ERα in cellular contexts. SNIPER(ER)-87 is valuable for research on hormone receptor regulation, breast cancer studies, and the development of targeted protein degradation strategies. -
PROTAC ER Degrader
SNIPER(ER)-110 is a PROTAC compound designed for targeted degradation of the estrogen receptor (ER). Comprising an IAP ligand and an estrogen ligand linked together, SNIPER(ER)-110 effectively induces ER protein degradation, exhibiting DC50 values of less than 3 nM at 4 hours and approximately 7.7 nM at 48 hours. This reagent is valuable for studies investigating ER-related signaling pathways and therapeutic strategies in hormone-dependent cancers. -
AR Degrader
EN1441 is a covalent degrader that targets the androgen receptor (AR) and its truncated variant AR-V7, exhibiting an EC50 value of 4.2 μM. This compound effectively degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is a valuable tool for research focused on androgen-independent prostate cancers, providing insights into therapeutic strategies for this challenging disease. -
Androgen Receptor Ligand/Estrogen Receptor Agonist
4-sec-Butylphenol is an androgen receptor ligand, exhibiting a binding affinity with a pIC50 value of 4.07. Additionally, it acts as an estrogen receptor agonist, contributing to its significant biological activity. This compound is commonly detected in industrial effluents and production water from oil and gas extraction, as well as in samples from river water, making it relevant for environmental research and toxicology studies. -
AR Degrader/CYP17A1 Inhibitor
YXG-158 is an orally active androgen receptor (AR) degrader and CYP17A1 inhibitor. It exhibits AR degradation activity with a DC50 value of 1.28 μM and inhibits CYP17A1 with an IC50 value of 100 nM. This compound is particularly relevant for research applications focused on enzalutamide-resistant prostate cancer, providing a valuable tool for investigating therapeutic strategies in this context. -
AR Antagonist/Degrader
AR Antagonist 4 is a potent orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wild-type AR. In addition to its antagonistic properties, it functions as an AR degrader with a DC50 of 2.84 μM. This dual activity positions AR Antagonist 4 as a valuable tool in research related to androgen signaling, hormone-dependent cancers, and potential therapeutic approaches targeting the AR pathway. -
Selective Estrogen Receptor Modulator
Raloxifene is a selective estrogen receptor modulator (SERM) derived from benzothiophene. Its primary mechanism involves exerting estrogen-agonistic effects on bone and lipid metabolism while acting as an estrogen antagonist in breast and uterine tissues. Raloxifene is utilized in research focused on breast cancer and osteoporosis, offering insights into estrogen modulation for therapeutic applications. -
Estrogen Receptor Antagonist
Camizestrant is a potent and orally active estrogen receptor (ER) antagonist. It is primarily utilized in research related to estrogen receptor-positive (ER+) HER2-negative advanced breast cancer, facilitating investigations into its therapeutic potential and mechanisms of action. This compound serves as a valuable tool for understanding ER signaling and developing targeted therapies in breast cancer treatment. -
Estrogen Receptor Degrader
Imlunestrant is a potent and selective estrogen receptor degrader (SERD) that functions as a pure antagonist of the estrogen receptor. This compound effectively leads to sustained inhibition of estrogen receptor-dependent gene transcription and cell proliferation. Imlunestrant is primarily utilized in research focused on ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC). -
Estrogen Receptor/ERR Inhibitor
Coumestrol is a phytoestrogen that targets the estrogen receptor, functioning as an ERR inhibitor. It demonstrates significant anti-proliferative activity against ES2 cells, with an IC50 value of 50 μM. Coumestrol is of interest in research related to cancer, neurological disorders, and autoimmune diseases due to its potential therapeutic effects. -
Estrogen Receptor Antagonist
Palazestrant is a potent estrogen receptor antagonist with significant antineoplastic properties. It effectively inhibits the activity of 17β-estradiol (E2) with an IC50 value of 6.4 nM and demonstrates strong anti-proliferative effects on MCF7 and CAMA-1 breast cancer cell lines with IC50 values ranging from 1.4 to 1.6 nM. Palazestrant is particularly relevant for research involving ER+/HER2+ cancer models, making it a valuable tool in cancer biology studies. -
Estrogen Receptor Modulator
Lasofoxifene is a selective estrogen receptor modulator (SERM) with oral bioactivity. It demonstrates significant anti-osteoporotic properties while also inhibiting primary tumor growth and metastatic spread. This compound is valuable for research related to breast cancer and postmenopausal osteoporosis. -
Estrogen Receptor/ERR
Isoflavone is a bioactive compound primarily targeting estrogen receptors, exerting its effects as a phytoestrogen derived from soy. It demonstrates lipid-lowering and antioxidant activities, contributing to the modulation of fatty acid oxidation in the liver and influencing gene expression in adipose tissue. Isoflavone is of significant interest in research related to chronic diseases, including cancer and cardiovascular disorders. -
Estrogen Receptor/ERR Agonist
Equilin (7-Dehydroestrone) is an estrogen receptor (ER) agonist that plays a significant role in modulating estrogenic activity. This compound promotes the growth of cortical neurons through a mechanism that is dependent on NMDA receptor activation. It is valuable for research applications investigating neuroprotection and the effects of estrogens on neuronal development and function. -
Estrogen Receptor/ERR Modulator
Dihydroresveratrol is a potent modulator of estrogen receptors, functioning as a phytoestrogen with significant biological activity. It exhibits proliferative effects in androgen-independent prostate and breast cancer cell lines, demonstrating activity at picomolar and nanomolar concentrations. This compound is valuable for research applications focused on hormone receptor signaling and cancer biology. -
Estrogen Receptor Degrader
Imlunestrant tosylate is a potent and selective estrogen receptor degrader (SERD) that exhibits pure antagonistic properties. This compound effectively leads to prolonged inhibition of estrogen receptor-dependent gene transcription and cellular proliferation. Imlunestrant tosylate is valuable for research focused on estrogen receptor-positive advanced breast cancer (ER+ aBC) and endometrial endometrioid cancer (EEC). -
Estrogen Receptor Modulator
Pipendoxifene is a selective estrogen receptor modulator (SERM) that targets estrogen receptors to modulate their activity. It exhibits key biological activity by influencing estrogenic effects in tissues, making it useful in the study of estrogen-related physiological processes and diseases. Its applications include research into hormone-dependent cancers, osteoporosis, and other conditions linked to estrogen signaling. -
Androgen Receptor Antagonist/Degrader
UT-34 is a selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader. It exhibits potent inhibition with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR and variants F876L-AR and W741L-AR, respectively. By binding to the ligand-binding domain and the functional AF-1 domain of AR, UT-34 employs the ubiquitin-proteasome pathway to facilitate AR degradation. This compound demonstrates promising anti-prostate cancer activity, making it valuable for research in androgen signaling and cancer therapeutics. -
Estrogen Receptor/ERR Inhibitor
α-Zearalenol is a mycotoxin that acts as an inhibitor of estrogen receptors (ER). As a derivative of zearalenone, it exhibits a high affinity for these receptors, leading to significant xenoestrogenic effects that can result in reproductive disorders in animals. This compound is utilized in research to study the impact of estrogenic exposure and its implications in endocrine disruption and reproductive health. -
Estrogen Receptor/ERR Antagonist
Nafoxidine is a nonsteroidal estrogen receptor (ER) antagonist that exhibits notable antitumor activity, particularly in breast cancer models. By inhibiting estrogen receptor-mediated signaling pathways, Nafoxidine is instrumental in studying the biological effects of estrogen in cancer research. Its ability to block ER activity makes it a valuable tool for investigating therapeutic strategies and understanding estrogen's role in tumor progression. -
Estrogen Receptor Modulator
(E)-4-Hydroxytamoxifen is an estrogen receptor modulator that exhibits anti-estrogenic activity. As a selective agent, it is primarily utilized in research related to breast cancer, where it helps to investigate the effects of estrogen receptor signaling on tumor growth and progression. This compound serves as a valuable tool in studies exploring therapeutic approaches to hormone-responsive cancers. -
Estrogen Receptor/ERR Modulator
Idoxifene is a selective estrogen receptor modulator (SERM) that exhibits tissue-specific activity. Its primary mechanism involves selective modulation of estrogen receptors, influencing estrogen-dependent biological processes. Idoxifene has shown promise in research applications related to hormone-responsive cancers and other conditions influenced by estrogen signaling. Its unique properties make it a valuable tool for investigating the role of estrogens in various biological contexts. -
Estrogen Receptor Degrader
Taragarestrant meglumine is a selective estrogen receptor degrader (SERD) known for its potent activity against estrogen receptors. This compound effectively inhibits the growth of estrogen receptor-positive (ER+) breast cancer cell lines and demonstrates significant efficacy in xenograft models. It serves as a valuable tool for research into targeted therapies for ER+ breast cancer, aiding in the understanding of estrogen receptor biology and the potential for innovative treatment strategies. -
Estrogen Receptor Antagonist
(Rac)-Acolbifene is a racemic estrogen receptor antagonist with dual anti-estrogenic and estrogenic properties. It features a piperidine ring in its structure and demonstrates a relative binding affinity (RBA) of 380. This compound is utilized in research applications focused on endocrine regulation, potential therapies for hormone-related conditions, and studies exploring estrogen receptor signaling pathways. -
Estrogen Receptor Antagonist
Enclomiphene is a potent non-steroidal estrogen receptor antagonist, primarily acting through its antioestrogenic properties. This compound is instrumental in research related to ovarian dysfunction, testosterone deficiency, male hypogonadism, and type 2 diabetes. Its oral bioavailability allows for convenient administration in various experimental settings. -
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.
