Catalog No.
Product Name
Application
Product Information
Citations
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SERM
LY2066948 is a selective estrogen receptor modulator (SERM) that exhibits high affinity for estrogen receptors ERα and ERβ, with Ki values of 0.51 nM and 1.36 nM, respectively. This compound demonstrates potent antiestrogenic activity, effectively blocking uterine weight gain induced by Ethynyl estradiol in immature rats. LY2066948 is employed in research related to uterine fibroids and myomas, contributing to the understanding of estrogen-related pathologies. -
Endocrine-disrupting compound
3-Chlorobisphenol A is a chlorinated derivative of bisphenol A that functions as an endocrine-disrupting compound. It interacts with estrogen receptors, leading to alterations in hormone signaling pathways. This compound is relevant in research focused on endocrine disruption and its implications in environmental health and toxicology, particularly in the study of plastics and their effects on human health. -
Estrogen Receptor/ERR
Lactandrate targets the estrogen receptor alpha (ERα) as a D-high nitrogen steroid alkylating agent. It exhibits a significant growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. In vivo studies have demonstrated its anti-tumor activity in mouse models of breast cancer, including MXT and CD8F1 strain tumors, as well as in human xenograft MX-1 models. Lactandrate serves as a valuable reagent for research in cancer biology, particularly in studying estrogen receptor modulation and breast cancer therapeutics. -
ER Modulator
Glyceollin I is a selective estrogen receptor (ER) modulator that exhibits anticancer, antioxidant, and anti-inflammatory activities. This compound is particularly promising for research in estrogen-related cancers, such as breast and ovarian cancer, as well as metabolic disorders, including hypercholesterolemia. Its unique mechanism enables the investigation of therapeutic strategies targeting estrogen pathways in various disease states. -
Non-steroidal Estrogen
4-tert-Octylphenol monoethoxylate is a non-steroidal estrogen that functions as an alkylphenolethoxylate (APE), specifically deriving from the breakdown of non-ionic surfactants such as 4-tert-octylphenol polyethoxylate. It exhibits estrogenic activity, making it relevant in studies of endocrine disruption and environmental toxicology. This compound has been detected in wastewater effluent, emphasizing its significance in research related to environmental contamination and its impact on aquatic ecosystems. -
ERα/ERβ Antagonist
ERα/ERβ antagonist-1 is a selective antagonist targeting estrogen receptors ERα and ERβ. It inhibits the activity of these receptors in a dose-dependent manner, demonstrating significant effects in HepG2 liver cell lines. This compound is valuable for research applications focused on estrogen signaling and its implications in various biological processes, including hormone-related diseases and cancer studies. -
Antioxidant
4-(Ethoxymethyl)phenol is an effective antioxidant that targets oxidative stress mechanisms. Derived from the leaf extract of Amburana cearensis, it exhibits in vitro cytogenotoxic properties, making it a valuable compound for investigations into respiratory diseases and inflammation. This reagent can be utilized in research focused on oxidative damage and its implications in various biological processes. -
Estrogen Synthesis Promoting Factor
Neo-sagittasine A is an estrogen synthesis promoting factor that enhances estrogen biosynthesis in human ovarian granulosa-like KGN cells. This compound is isolated from the plant Epimedium brevifolium and is useful in research applications related to reproductive biology and hormone regulation. Its ability to promote estrogen production makes it a valuable reagent for studies investigating endocrine functions and associated disorders. -
Estrogen Receptor Anolog
10-Chloroestra-1,4-diene-3,17-dione is an analog of the estrogen receptor, primarily targeting this pathway to modulate estrogenic activity. This compound demonstrates significant biological activity in studies involving hormone-related signaling and receptor interactions. It is commonly utilized in research applications focused on endocrine modulation, cancer biology, and the exploration of estrogen-related mechanisms in cellular processes. -
ERβ Agonist
(-)-Erteberel is a selective agonist of the estrogen receptor beta (ERβ). This compound plays a significant role in the investigation of diseases influenced by ERβ, including prostate cancer. Its specificity for ERβ makes it a valuable tool for exploring the receptor's biological functions and potential therapeutic applications. -
Estrogen Receptor Antagonist
4-Hydroxytoremifene is an estrogen receptor antagonist that effectively inhibits the binding of estradiol to its receptor in target tissues. This compound is utilized in research to explore mechanisms of estrogen action and its role in various hormonal therapies, particularly in the context of breast cancer. Its ability to modulate estrogen signaling makes it a valuable tool for studying hormone-responsive diseases. -
Anti-estrogen Deficiency Agent
LY88074 Trimethyl Ether is an anti-estrogen deficiency agent that targets estrogen signaling pathways. It effectively inhibits conditions associated with estrogen deprivation syndrome, such as osteoporosis and hyperlipidemia. This compound serves as a valuable tool in research applications focused on understanding and mitigating the effects of estrogen deficiency. -
Estrogen Receptor/ERR Agonist
NNC45-0781 is an estrogen receptor (ER) partial agonist with tissue-selective properties. It exhibits key biological activity by modulating ER signaling pathways, making it valuable for research on estrogen-related physiological processes and conditions. NNC45-0781 is particularly relevant in investigations of hormone-dependent cancers and the study of estrogen's role in reproductive biology. -
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. -
Hormone
Nilestriol is an estriol derivative that primarily acts as a non-steroidal estrogen. It has demonstrated the ability to inhibit bone loss associated with osteoporosis, particularly in models such as ovariectomized rats and postmenopausal women. Nilestriol is useful in research aimed at understanding estrogen's role in bone health and its potential therapeutic applications in osteoporosis management. -
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. -
FSHR Agonist
FSHR Agonist 1 is a high-affinity allosteric agonist for the follicle-stimulating hormone receptor (FSHR), exhibiting a pEC50 value of 7.72. This compound forms significant interactions with the transmembrane domain, leading to the direct activation of FSHR. FSHR Agonist 1 is utilized in research applications focusing on reproductive biology and endocrine signaling pathways. -
a-UPR Activator
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator with enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells, exhibiting a broader selectivity profile compared to its predecessor, ErSO. This compound demonstrates significant antitumor activity against MCF-7 cancer models in murine studies. Additionally, ErSO-DFP is capable of crossing the blood-brain barrier, making it a valuable tool for research in cancer therapeutics and neuro-oncology applications. -
ERα Antagonist
GNE-149 is a potent antagonist of estrogen receptor alpha (ERα) with an IC50 of 0.053 nM, demonstrating high selectivity as a selective estrogen receptor degrader (SERD). This compound exhibits significant biological activity in the modulation of ERα signaling pathways, making it a valuable tool in breast cancer research. Its ability to degrade ERα may provide insights into therapeutic strategies targeting estrogen-dependent tumors. -
ERRα Agonist
DS20362725 is an agonist of the estrogen-related receptor alpha (ERRα). It demonstrates potent inhibition of the binding between receptor-interacting protein 140 (RIP140) corepressor peptide and the GST-ERRα ligand-binding domain, with an IC50 value of 0.6 μM. This compound is valuable for research on metabolic disorders, particularly type 2 diabetes mellitus (T2DM), enabling investigations into ERRα's role in metabolic regulation.
