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Catalog No.
Product Name
Application
Product Information
Citations
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Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. , Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. , Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. , Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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Smurf1 inhibitor
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. -
estrogen receptor (ER) inhibitor
WAY-169916 is a pathway-selective inhibitor of estrogen receptor (ER) that acts by inhibiting NF-kB transcriptional activity. -
Estrogen Receptor/ERR Inhibitor
Estradiol cypionate is a 17β-cypionate ester of estradiol that acts as a selective estrogen receptor modulator. It functions by inhibiting the synthesis of endothelin-1 (ET-1), a key factor in vascular biology. This compound is widely utilized in research exploring estrogenic effects, hormonal signaling pathways, and the therapeutic potential of estrogen receptor modulation in various physiological and pathological conditions. -
EGFR Inhibitor, Estrogen Receptor Inhibitor, Progesterone Receptor Inhibitor
4,7-Dihydroxycoumarin is a potent inhibitor of the epidermal growth factor receptor (EGFR) as well as estrogen and progesterone receptors. It exhibits significant cytotoxicity against breast cancer cells, with an IC50 value of 18.36 μg/mL. This compound is valuable for research focused on breast cancer treatment and the exploration of hormone receptor interactions. -
ERα Inhibitor
Isocurcumenol is an estrogen receptor alpha (ERα) inhibitor derived from the rhizomes of Curcuma zedoaria. It demonstrates significant anti-tumor activity, exhibiting IC50 values of 99.1 μg/mL in Dalton's lymphoma ascites (DLA) cells and 178.2 μg/mL in KB cells. This compound has potential applications in cancer research, particularly in exploring targeted therapies for hormone-dependent tumors. -
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. -
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. -
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. -
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. -
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 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. -
Estrone Sulfatase Inhibitor
3-Formylsalicylic acid is a noncompetitive inhibitor of estrone sulfatase, displaying an IC50 value of 0.15 mM and a Ki value of 0.12 mM. This compound demonstrates low acute toxicity, making it a suitable candidate for research applications aimed at studying estrogen metabolism and related pathways in cancer biology. Its inhibitory effects on estrone sulfatase may provide insights into therapeutic strategies for hormone-dependent tumors. -
ERα Inhibitor
TPBM is a selective estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for the 17β-estradiol (E2)-ERα complex. This compound effectively diminishes the recruitment of E2·ERα to endogenous estrogen-responsive genes. Additionally, TPBM demonstrates the capacity to inhibit E2-dependent proliferation of ERα-positive cancer cells, exhibiting an IC50 of 5 μM. Notably, TPBM is non-toxic to normal cells and does not interfere with estrogen-independent cell growth, making it a valuable tool for research in hormone-responsive signaling pathways and cancer biology. -
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. -
ERα Inhibitor
Fulvestrant-3-boronic acid is a potent estrogen receptor alpha (ERα) inhibitor that exhibits competitive binding with an IC50 of 4.1 nM. This compound effectively induces degradation of ERα in breast cancer cells, making it a valuable tool for research in estrogen receptor-related signaling pathways and breast cancer therapies. Its mechanism of action supports studies aimed at understanding ERα's role in tumor progression and treatment resistance. -
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 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. -
ER inhibitor
4,4'-Oxydiphenol is a known estrogen receptor inhibitor, exhibiting an IC50 value of 60 μM. This compound manifests significant biological activity by modulating estrogen signaling pathways, making it a useful tool for exploring estrogen receptor-related mechanisms. It is pertinent for research applications in cancer biology, particularly in studies focused on hormone-dependent tumors and endocrine regulation. -
ERα Inhibitor
VPC-16606 is a selective inhibitor of the estrogen receptor alpha (ERα), specifically targeting its activation function 2 (AF2) domain. This compound effectively disrupts the interaction between ERα and coactivators, inhibiting the activity of both wild-type and drug-resistant mutant forms of ERα. VPC-16606 demonstrates significant potency against hormone-resistant breast cancer cells, making it a valuable tool for research in breast cancer mechanisms and therapeutic development. -
ERR Inhibitor
Millewanin G is a prenylated isoflavonoid that acts as an estrogen-related receptor (ERR) inhibitor, exhibiting antiestrogenic activity with an IC50 of 29 μM. This compound is primarily isolated from the leaves of M. pachycarpa, which is cultivated in Japan. Millewanin G is valuable for research applications focused on understanding ERR's role in various biological processes and its impact on diseases influenced by estrogen signaling. -
ERRγ Inhibitor
ERRγ-IN-1 is a potent ERRγ inhibitor with an IC50 of 0.040 μM. It demonstrates activation of the MAPK (p44/p42) pathway while effectively inhibiting ERRγ activity. ERRγ-IN-1 has been shown to enhance iodine uptake in anaplastic thyroid carcinoma xenografts and to suppress tumor growth in nude mouse models. This compound is valuable for research focused on anaplastic thyroid carcinoma. -
Estrogen Receptor Inhibitor
Yp537 is an estrogen receptor inhibitor that disrupts the dimerization of the human estrogen receptor. This action effectively impedes estrogen-mediated signaling pathways, making it valuable for research on hormone-dependent cancers and other estrogen-related diseases. Yp537 is suitable for studying the molecular mechanisms underlying estrogen receptor activity and evaluating potential therapeutic strategies targeting these pathways. -
ERα Inhibitor
OBHS is an inhibitor of estrogen receptor α (ERα), providing a crucial tool for studying estrogen signaling pathways. This compound is primarily utilized in research applications focusing on hormone-related cancers and endocrine disorders. Additionally, OBHS can function as a blowing agent, offering versatility for various chemical processes. -
ERRα Inhibitor
Estrogen Receptor Modulator 8 is a potent ERRα inhibitor, exhibiting an IC50 of 0.437 nM in MCF-7 cells. This compound effectively inhibits the proliferation of MCF-7 cells with an IC50 value of 0.1 nM. It serves as a valuable tool for studying estrogen receptor signaling pathways and their implications in cancer research. -
Estradiol Inhibitor
Triisopropyl phosphate is an estradiol inhibitor that exerts anti-estrogenic activity by inhibiting TFF1 and EGR3 gene expression. It demonstrates the ability to suppress estradiol-induced proliferation in MCF-7 cells, with an EC50 of 341 μM. Additionally, it inhibits estrogen response element (ERE)-stimulated luciferase activity in MVLN cells with an EC50 of 900 μM, making it a valuable tool for research in estrogen signaling pathways. -
EstrogenReceptor (E2R) Inhibitor
Metahexestrol functions as an estrogen receptor (E2R) inhibitor, demonstrating significant antitumor activity. It effectively inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells with an ED50 of 1.0 μM. Notably, Metahexestrol also shows inhibitory effects on estrogen receptor-negative MDA-MB-231 cells, indicating that its antiproliferative action may occur independently of the E2R pathway. This compound is valuable for research focused on estrogen-dependent breast cancer.
