Catalog No.
Product Name
Application
Product Information
Citations
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Coactivator-derived Mimic
SRC2-2 peptide is a coactivator-derived mimic that targets the androgen receptor (AR) ligand. It plays a vital role in modulating AR activity, making it a valuable tool for investigating mechanisms of prostate cancer progression and treatment. This peptide is suitable for studies focused on AR signaling pathways and the development of AR-targeted therapies. -
Androgen Receptor Antagonist
YM580 is a selective antagonist of the Androgen Receptor (AR), exhibiting potent activity with an IC50 of 0.11 μM and Ki values of 4.6 nM for human AR and 6.2 nM for rat AR. It demonstrates high selectivity over other steroid hormone receptors, including PR, GR, and ERα, with Kis greater than 3300 nM. In vivo studies show that YM580 effectively reduces ventral prostate weight in mature intact rats in a dose-dependent manner while maintaining serum testosterone levels. This compound is valuable for research into prostate cancer and androgen-related pathways. -
Androgen Receptor Antagonis
Anticancer agent 135 is a potent androgen receptor (AR) antagonist that effectively inhibits AR nuclear translocation and AR/AR-V7 heterodimerization. This compound subsequently disrupts downstream gene transcription, making it a valuable tool in prostate cancer research. Its robust efficacy has been demonstrated in prostate cancer xenograft models, highlighting its potential for therapeutic development in androgen-related malignancies. -
Antiandrogen
RU 58642 is a potent non-steroidal antiandrogen that exhibits strong and selective binding to the androgen receptor. This compound is primarily utilized in research to investigate androgen receptor signaling pathways and to explore its implications in conditions such as prostate cancer and androgen-mediated disorders. RU 58642 serves as a valuable tool for scientists studying the role of androgens in various biological processes and therapeutic interventions. -
Androgen Receptor Antagonist
AR Antagonist 5 is a selective antagonist of the androgen receptor, exhibiting an IC50 value of 134.8 nM. This compound demonstrates favorable pharmacokinetic properties, characterized by high skin exposure and low plasma exposure. AR Antagonist 5 is valuable for research applications targeting androgen receptor signaling pathways in various biological studies related to hormone regulation and therapeutic interventions in androgen-sensitive conditions. -
Androgen Receptor Antagonist
YM-1758735 is an orally active androgen receptor (AR) antagonist that exhibits an IC50 of 0.2 μM. This compound effectively inhibits AR-mediated transcriptional activation, making it a valuable tool for studying androgen signaling pathways. YM-1758735 is particularly relevant for research focused on prostate cancer and other androgen-related disorders. -
AR Antagonist
LG-120907 is a selective androgen receptor (AR) antagonist, exhibiting a Ki value of 26 nM. This compound effectively inhibits testosterone-induced increases in ventral prostate and seminal vesicle tissue weight in vivo. LG-120907 is valuable for research applications focusing on the modulation of androgen signaling and the study of prostate-related pathologies. -
Astrogen antagonist
AR Antagonist 7 is a selective androgen receptor (AR) antagonist. This compound demonstrates significant biological activity by inhibiting AR-mediated signaling pathways, making it a valuable tool for studying androgen-related hair loss and other AR-associated conditions. Its application extends to investigating therapeutic strategies for androgenic alopecia and other disorders influenced by androgen signaling. -
Androgen-receptor Antagonist
WB2838 is a non-steroidal androgen receptor antagonist, exhibiting an IC50 of 0.8 μM for partially purified rat prostate cytosol receptors. This compound demonstrates significant anti-cancer activity against androgen-responsive breast cancer and effectively inhibits the growth of the ventral prostate induced by testosterone propionate. WB2838 is a valuable tool for research on androgen pathway modulation and cancer therapeutic strategies. -
AR Pure Antagonist
CH5137291 is a potent pure antagonist of the androgen receptor (AR) that operates by preventing the translocation of AR from the cytoplasm to the nucleus, thereby inhibiting AR-mediated signaling. This compound demonstrates significant biological activity by completely suppressing tumor growth in both cell lines and mouse models of castration-resistant prostate cancer (CRPC). CH5137291 is a valuable tool for researchers investigating the mechanisms and therapeutic approaches related to CRPC. -
Antiandrogen Agent
Pentomone, also known as LY-113935, functions as an antiandrogen agent through the inhibition of androgen receptor activity. Its primary biological activity is the suppression of prostate growth, making it a valuable tool for research related to prostate cancer and androgen-related disorders. Pentomone can be utilized to investigate the mechanisms of hormone signaling and the therapeutic potential of antiandrogens in cancer treatment. -
Androgen Receptor Antagonist
JNJ-26146900 is a potent nonsteroidal androgen receptor antagonist, exhibiting a Ki value of 400 nM for the rat androgen receptor. This compound is effective in reducing prostate tumor size and preventing bone loss, making it valuable for cancer research applications. JNJ-26146900 serves as a critical tool for investigating the roles of androgen receptors in prostate cancer progression and therapeutic strategies. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 5 is a potent inhibitor of the androgen receptor (AR) with an IC50 value of 6.17 μM. This compound effectively hinders AR nuclear translocation, lowering nuclear AR levels and disrupting AR-mediated gene regulation. It demonstrates antiproliferative effects against LNCaP cells and exhibits antitumor activity in LNCaP xenograft mouse models. Androgen Receptor Antagonist 5 is suitable for research applications focused on prostate cancer. -
AR Antagonist
JJ-450 is a non-competitive antagonist of the androgen receptor (AR) that effectively inhibits both wild-type AR and the mutant variant ARF876L. With an IC50 ranging from 1-10 μM in PC3 cells, JJ-450 selectively binds to AR without competing with androgens for the ligand binding domain. It disrupts AR nuclear translocation and promotes the degradation of unliganded AR, leading to decreased transcriptional activity. This compound is relevant for research applications involving castration-resistant prostate cancer (CRPC), particularly in studies focusing on resistance to Enzalutamide. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 8 is a potent antagonist of the androgen receptor, effectively inhibiting prostate-specific antigen (PSA) secretion in LNCaP cells with an IC50 of 88 nM. This compound serves as a valuable tool in prostate cancer research, helping to elucidate the role of androgen signaling in tumorigenesis and potential therapeutic interventions. -
Androgen Receptor Dimerization Inhibitor
M17-B15 is an androgen receptor dimerization inhibitor that demonstrates an IC50 of 30 nM. By effectively disrupting androgen receptor self-association, M17-B15 suppresses androgen receptor signaling pathways. This compound exhibits significant anti-prostate cancer efficacy in both in vitro studies and in mouse xenograft tumor models, making it a valuable tool for research in prostate cancer biology. -
Androgen Receptor Antagonist
AR Antagonist 17 is a potent, selective androgen receptor (AR) antagonist, exhibiting an IC50 value of 0.010 μM. This compound effectively inhibits AR dimerization and nuclear translocation, demonstrating significant efficacy in castration-resistant prostate cancer (CRPC) cell lines, including those with drug-resistant AR mutations. In preclinical models, AR Antagonist 17 has shown the ability to suppress tumor growth in LNCaP xenografts without noticeable toxicity. This reagent serves as a valuable tool for investigations into CRPC mechanisms and potential therapeutic strategies. -
ERβ Agonist And AR Antagonist
ERβ agonist-1 is a selective agonist for estrogen receptor beta (ERβ) with an EC50 of 46.8 nM, while also functioning as an androgen receptor (AR) antagonist with an IC50 of 1555 nM. This compound activates ERβ signaling through specific binding, simultaneously inhibiting AR activity. It is particularly valuable in research applications related to prostate cancer and demonstrates selective ERβ agonist effects in mouse models, supporting investigations into hormone-related pathologies. -
Stable Isotope
Ketodarolutamide-d3 is a deuterium-labeled derivative of Ketodarolutamide, a potent and high-affinity nonsteroidal androgen receptor (AR) antagonist. It exhibits a Ki value of 8 nM for rat wild-type AR and an IC50 of 38 nM in AR-HEK293 cells, effectively inhibiting testosterone-induced nuclear translocation of the AR. This compound specifically suppresses the proliferation of AR-dependent prostate cancer cells and demonstrates antitumor activity in models of castration-resistant prostate cancer (CRPC). Ketodarolutamide-d3 is a valuable tool for mechanistic and therapeutic research in prostate cancer studies. -
Androgen Receptor Degrader
Androgen Receptor Degrader-5 is a selective degrader of the androgen receptor (AR), promoting targeted degradation of AR proteins. This compound exhibits potent antiproliferative effects in androgen-dependent cancer models, making it an ideal tool for studying AR signaling and its role in tumor growth. Its utility extends to research applications in hormone-sensitive cancers and androgen receptor-related signaling pathways. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 3 is an effective antagonist of the androgen receptor, exhibiting an IC50 of 2.4 μM. This compound demonstrates significant anticancer activities, making it a valuable tool in the study of androgen-dependent cancers. Researchers can utilize Androgen Receptor Antagonist 3 to explore mechanisms of tumor growth inhibition and to develop targeted therapies in androgen-related malignancies. -
Antiandrogen
VPC-13789 is a selective antiandrogen that effectively inhibits androgen receptor (AR) transcriptional activity, with an IC50 value of 0.19 μM in LNCaP cells. This compound is orally bioavailable and serves as a valuable research tool in the study of castration-resistant prostate cancer (CRPC) therapeutics. Its potency and specificity make it suitable for elucidating AR-mediated signaling pathways and developing targeted treatment strategies. -
Androgen Receptor Modulator
LG-121071 is an orally active selective modulator of the androgen receptor, exhibiting a binding affinity (Ki) of 17 nM. This compound demonstrates significant potential in the study of androgen receptor signaling pathways and offers valuable insights into therapeutic applications related to muscle wasting, osteoporosis, and androgen-related disorders. Its specificity makes it a useful tool for investigating the role of androgen receptors in various biological processes. -
Androgen Receptor Antagonist
p-Hydroxyphenylacetone is an androgen receptor (AR) antagonist, demonstrating an IC50 of 420 μM in MDA-kb2 human breast cancer cells. This compound can be utilized in breast cancer research to investigate the role of androgen signaling pathways and their potential implications in disease progression and therapeutic strategies. -
Androgen Receptor Antagonist
VPC-3033 is a potent androgen receptor antagonist that effectively inhibits androgen receptor transcriptional activity with an IC50 of 0.3 µM. This compound demonstrates significant degradation of the androgen receptor, enhancing its efficacy in therapeutic contexts. VPC-3033 is particularly valuable in research involving prostate cancer cells resistant to Enzalutamide, providing a critical tool for studying anti-androgen resistance mechanisms and developing novel treatment strategies. -
Androgen Receptor Modulator
LGD-2941 is a potent and selective androgen receptor modulator (SARM) that exhibits significant anabolic effects on muscle tissue while minimizing impact on the prostate. In preclinical studies involving hypogonadic rat models, LGD-2941 has demonstrated substantial muscle-building properties. Additionally, this compound enhances bone strength in rat models simulating post-menopausal osteoporosis, making it a valuable tool for research in muscle and bone health. -
Androgen Receptor Modulator
FL442 is an androgen receptor (AR) modulator that demonstrates potent inhibitory effects in AR-dependent prostate cancer cells. It exhibits comparable efficacy to traditional antiandrogen therapies while retaining activity against the AR mutant F876L, known for its resistance to standard treatments. Pharmacokinetic studies in mice reveal a long half-life of 8 hours, favorable targeting of prostate tissue, and metabolic stability. FL442 effectively inhibits LNCaP tumor growth at low plasma concentrations, positioning it as a valuable tool for research in prostate cancer therapeutics. -
Androgen Receptor Inhibitor
Androgen receptor-IN-3 is a selective inhibitor of the androgen receptor (AR), effectively reducing AR-driven transcriptional activity in LNCaP prostate cancer cells, with an IC50 of 5.04 μM. This compound is primarily utilized in research applications investigating androgen receptor signaling pathways and their role in prostate cancer progression. Its inhibitory effects on AR activity present a valuable tool for studying potential therapeutic strategies targeting androgen-dependent tumors. -
Androgen Receptor
(3β,4β,17β)-17-(2-Pyridinylmethyl)androst-5-ene-3,4,17-triol is a selective androgen receptor modulator that exhibits potential anticancer activity. This compound is primarily used in research to investigate androgen receptor signaling pathways and the development of targeted therapies for hormone-driven cancers. Its unique structure enables modulation of androgenic effects, making it an important tool for studying the role of androgens in cancer biology. -
AR Antagonist
(+)-JJ-74-138 is a novel non-competitive antagonist of the androgen receptor (AR) that demonstrates significant potency against Enzalutamide-resistant castration-resistant prostate cancer (CRPC). This compound effectively inhibits AR signaling, making it a valuable tool for investigating alternative therapeutic strategies in prostate cancer research. Its application in preclinical studies may provide insights into overcoming resistance mechanisms in androgen-targeted therapies. -
AR Antagonist
Zanoterone is an orally active antagonist of the androgen receptor (AR), exhibiting a Ki of 2.2 μM. By inhibiting the binding of androgens, including testosterone and dihydrotestosterone (DHT), Zanoterone effectively disrupts the androgen signaling pathway. This action is significant for reducing androgen-dependent conditions such as prostate hyperplasia and prostate cancer growth, making it a valuable tool in androgen-related research and therapeutic development. -
Nonsteroidal Antiandrogen
Inocoterone acetate is a nonsteroidal antiandrogen that selectively binds to the androgen receptor, exerting antiandrogenic activity. This compound has been demonstrated to reduce inflammatory papules and pustules in various animal models. It serves as a valuable reagent for research into conditions driven by androgenic activity, including acne and other androgen-related disorders. -
Androgen Receptor
ONC1-13B is a potent antagonist of the androgen receptor (AR), effectively inhibiting PSA expression in prostate cancer cells. This compound markedly reduces prostate cancer cell proliferation in the presence of dihydrotestosterone (DHT) stimulation. ONC1-13B exerts its anti-tumor effects by preventing androgen binding to AR and inhibiting its nuclear translocation, making it a valuable tool for prostate cancer research. -
Androgenic Steroid
Trestolone acetate is a synthetic anabolic androgenic steroid that primarily targets androgen receptors. It exhibits strong anabolic activity, promoting muscle growth and strength enhancements. This compound is commonly utilized in research focused on hormone regulation, anabolic processes, and potential therapeutic applications in conditions associated with muscle wasting and hormonal imbalances. -
Androgen Receptor Agonist
Mebolazine is an androgen receptor agonist that exhibits both androgenic and anabolic properties. Its binding to the androgen receptor facilitates the modulation of gene expression associated with muscle growth and development. This compound is commonly utilized in research settings to investigate the physiological effects of androgens and their role in anabolic processes. -
Androgen Receptor
Silandrone is a synthetic anabolic-androgenic steroid (AAS) that functions primarily as an androgen receptor modulator. It exhibits significant anabolic activity, promoting muscle growth and strength gains while also exhibiting properties that can help mitigate muscle wasting. Silandrone is utilized in research applications related to androgen receptor signaling, performance enhancement, and muscle physiology studies. -
Androgen Receptor Antagonist
Topterone is an androgen receptor antagonist that specifically inhibits the action of androgens. It demonstrates potent antiandrogenic activity, making it valuable for research focused on androgen-related conditions. This compound is primarily utilized in studies investigating skin conditions and hormonal therapies. -
Androgen Receptor Inhibitor
Carbazole derivative 1 is an androgen receptor inhibitor that effectively reduces androgen and estrogen levels in mammals, including humans. This compound demonstrates significant potential in research applications focusing on hormone-related disorders and cancer treatments involving hormonal regulation. Its unique mechanism may provide insights into therapeutic strategies for managing conditions influenced by androgen and estrogen signaling pathways. -
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.
