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. -
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. -
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. -
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. -
STS Inhibitor/ERα Modulator
SR-16157 is a dual-action steroid sulfatase (STS) inhibitor and selective estrogen receptor alpha (ERα) modulator, with an IC50 of 0.1 µM. This compound displays potent STS inhibitory and anti-estrogenic effects in breast cancer cells, making it a valuable tool for understanding the role of estrogen signaling in cancer progression. SR-16157 is applicable in breast cancer research, particularly in studies exploring therapeutic strategies targeting estrogen metabolism and receptor modulation. -
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. -
Gonadal Steroid Agonist
Tibolone is a gonadal steroid agonist that exhibits progestagenic, androgenic, and estrogenic properties. It is primarily utilized in research related to postmenopausal osteoporosis, facilitating studies on its effects on bone health and hormonal balance. This compound serves as a valuable tool for investigating the multifaceted roles of steroids in reproductive health and aging. -
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. -
ER Antagonist
Giredestrant is a selective, non-steroidal estrogen receptor (ER) antagonist that effectively competes with estradiol for binding to the ER. By inducing a conformational change within the ligand binding domain of the receptor, Giredestrant exhibits significant anti-tumor activity. This agent is primarily utilized in research focused on targeting estrogen-dependent cancers and studying the mechanisms of ER-mediated signaling pathways. -
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. -
GPER/GPR30 Antagonist
G36 is a cell-permeable antagonist of the G protein-coupled estrogen receptor GPER (GPR30). It selectively inhibits estrogen-induced activation of the PI3K pathway and effective calcium mobilization, with an IC50 value of 112 nM. G36 holds significant promise for research applications in cancer biology, particularly in studies focusing on estrogen signaling pathways and their implications in tumorigenesis. -
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. -
ERR Antagonist
ERRα antagonist-1 is a selective antagonist of estrogen-related receptor α (ERRα), effectively inhibiting its interaction with coactivators Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, with IC50 values of 170 nM and 180 nM, respectively. This compound is valuable for research applications focused on metabolic regulation and mitochondrial function, providing a tool for exploring ERRα's role in various physiological processes and disease states. ERRα antagonist-1 facilitates investigations into the therapeutic potential of targeting ERRα pathways in metabolic disorders and cancer. -
Serum Albumin Binder
Zearalanone is a reductive metabolite of Zearalenone, primarily functioning as a serum albumin binder. This compound demonstrates the ability to bind effectively to serum albumin across various species, thereby influencing pharmacokinetics. Additionally, Zearalanone enhances the binding affinity of Warfarin to serum albumin, making it a valuable tool for research applications in drug metabolism and pharmacodynamics. -
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). -
a-UPR Activator
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator that targets estrogen receptor alpha (ERα). It induces robust and sustained cytotoxic effects through the activation of the a-UPR pathway. This compound is valuable for research in cancer biology, particularly in studies investigating the role of ERα in tumor cell stress responses and therapeutic resistance. -
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. -
ERRα Agonist
DS45500853 is an agonist of estrogen-related receptor α (ERRα), functioning by inhibiting the interaction between the receptor-interacting protein 140 (RIP140) corepressor peptide and the GST-ERRα ligand-binding domain, with an IC50 value of 0.80 μM. This compound is relevant for research into metabolic disorders, particularly type 2 diabetes mellitus (T2DM), providing insights into ERRα signaling pathways and their implications in metabolic regulation. -
Viral Endonuclease Inhibitor
Licoflavone C is a viral endonuclease inhibitor with broad-spectrum antiviral activity. It exhibits estrogen-like properties and effectively inhibits the replication of various bunyaviruses, including severe fever with thrombocytopenia syndrome virus (SFTSV) and lymphocytic choriomeningitis virus, through a non-substrate competitive mechanism. Licoflavone C demonstrates an IC50 of 35.5 μM against SFTSV CEN, with a Kd of 9.53 μM. Additionally, it exhibits low cytotoxicity and genotoxicity while inducing apoptosis and alleviating chemotherapy-induced chromosomal damage. This compound is valuable for research on viral infections, particularly mechanisms related to severe fever with thrombocytopenia syndrome. -
Estrogen Precursor
10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor of the primary human estrogen, 17β-estradiol. It exhibits significant therapeutic potential in alleviating hot flashes associated with thermoregulatory dysfunction in rat models. This compound is valuable for research focused on hormonal regulation and the neuroendocrine system, particularly in the context of menopausal symptoms and estrogen-related physiological processes.
