Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Androgen Receptor Modulator
S-40503 is a selective androgen receptor modulator that exhibits oral bioavailability. This compound has been shown to significantly enhance bone mineral density (BMD) and improve the biomechanical strength of femoral cortical bone. S-40503 is valuable for research applications focusing on bone health, skeletal muscle function, and the therapeutic potential of androgen modulation. -
AR/ARV7 Inhibitor
AR/AR-V7-IN-1 is a potent inhibitor of the androgen receptor (AR) and its splice variant AR-V7, with an IC50 of 172.85 nM. This compound effectively suppresses cell proliferation in LNCaP and 22RV1 cell lines, exhibiting IC50 values of 4.87 μM and 2.07 μM, respectively. Additionally, AR/AR-V7-IN-1 demonstrates significant tumor growth inhibition in 22RV1 xenograft models, making it a valuable tool for prostate cancer research. -
Linker of RNAi Agent To Antibodies
Di(5-(methylsulfonyl)-1,3,4-oxadiazol-2-yl)-benzene-amide-PEG4-ester-2,3,5,6-F-Ph serves as a linker for conjugating RNA interference (RNAi) agents targeting the Androgen Receptor (AR). This compound facilitates the inhibition of AR gene expression and reduces AR activity, making it valuable for studies in spinal and bulbar muscular atrophy (SBMA). Its unique design enables efficient targeting of ligands, such as antibodies, enhancing therapeutic strategies in gene regulation research. -
Androgen Receptor Modulator
Androgen Receptor Modulator 3 is a selective modulator targeting the androgen receptor. This compound demonstrates potential in promoting muscle growth and mitigating sarcopenia in research settings, making it valuable for studies focused on muscle wasting disorders and related therapeutic strategies. Its ability to selectively influence androgen receptor activity offers a unique tool for investigating muscle biology and age-related health conditions. -
Androgen Receptor Antagonist
(rel)-BMS-641988 is a nonsteroidal androgen receptor antagonist that selectively inhibits androgen receptor activity. This compound demonstrates potent biological activity in blocking androgen-dependent signaling pathways, making it a valuable tool in prostate cancer research. Its application in studies of androgen receptor regulation contributes to the understanding of therapeutic strategies for prostate cancer treatment. -
AR antagonists
Androgen Receptor Antagonist 11 (compound N29) is a selective and orally bioavailable antagonist of the androgen receptor (AR), exhibiting an IC50 value of 18 nM. This compound is designed to inhibit AR activity, making it valuable for studies related to androgen-dependent diseases, such as prostate cancer and androgenic alopecia. Its specificity and potency allow for targeted research into AR-related signaling pathways and therapeutic interventions. -
AR BF3 Inhibitor
VPC13163 is a potent inhibitor of the androgen receptor (AR) BF3 domain, exhibiting an IC50 value of 0.31 µM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in prostate cancer and other androgen-dependent malignancies. Its ability to selectively target the AR BF3 domain allows for the exploration of new therapeutic strategies in androgen receptor-mediated pathways. -
Selective Androgen Receptor Modulator
MK-3984 is a selective androgen receptor modulator (SARM) that primarily targets androgen receptors to elicit anabolic effects in muscle tissue. It demonstrates potential for promoting muscle growth and mitigating muscle wasting, particularly in cancer-related cachexia research. MK-3984 serves as a valuable tool for studying the therapeutic applications of SARMs in muscle preservation and enhancement. -
Androgen Receptor Antagonist
AR Antagonist 10 is a potent androgen receptor (AR) antagonist that demonstrates an IC50 value of 0.04 μM. It employs dual mechanisms of action by disrupting AR dimerization and promoting AR degradation through the ubiquitin-proteasome pathway. This compound shows significant efficacy against drug-resistant AR variants and effectively inhibits tumor growth in LNCaP xenograft models. AR Antagonist 10 has potential applications in the treatment of drug-resistant prostate cancer. -
Androgen Receptor Antagonist
AR Antagonist 12 is a potent androgen receptor (AR) antagonist that selectively targets wild-type AR and the AR-F877L variant, demonstrating IC50 values of 119.3 μM and 98.2 μM, respectively. This compound effectively reduces the protein levels of AR, AR-V7, and PSA in a dose-dependent and time-dependent manner, showcasing its therapeutic potential. AR Antagonist 12 is particularly useful for investigating resistance mechanisms in prostate cancer, including studies related to Enzalutamide responsiveness. -
Androgen Receptor Antagonist
Androgen receptor antagonist 4 is a potent antagonist of the androgen receptor (AR) with an IC50 of 0.15 μM. This compound effectively inhibits AR transcriptional activity, suppresses downstream target gene expression of AR, and prevents dihydrotestosterone (DHT)-induced AR nuclear translocation. It demonstrates promising anticancer properties, making it a valuable tool for studies related to androgen receptor signaling and its implications in cancer research. -
Androgen Receptor Modulator
(+)-JNJ-37654032 is a selective androgen receptor modulator (SARM) that demonstrates oral bioactivity. This compound has been shown to exhibit anabolic effects on muscle tissue, making it a valuable tool for researching muscle-wasting diseases and related disorders. Its specificity for androgen receptors allows for targeted studies in the context of therapeutic applications for conditions involving muscle loss. -
AR Inhibitor
AR Antagonist 6 is a diphenyl ether compound that acts as a selective androgen receptor (AR) antagonist, binding to the receptor with an affinity of 120 nM. This compound demonstrates low toxicity and shows promising in vitro activity in the golden Syrian hamster ear model. It serves as a valuable tool for research applications involving the modulation of androgen receptor signaling in various biological contexts. -
Androgen Receptor Inhibitor
Androgen receptor-IN-4 is a potent androgen receptor inhibitor that selectively targets the androgen receptor signaling pathway. This compound is particularly valuable for investigating the mechanisms underlying androgen-dependent conditions, including Kennedy's disease. Its application in research can contribute to a better understanding of therapeutic strategies for androgen receptor-related disorders. -
Androgen Receptor
HG122 is a selective compound that targets the androgen receptor (AR), promoting its degradation via the proteasome pathway. This mechanism inhibits the proliferation of castration-resistant prostate cancer cells, making HG122 a valuable tool for research in prostate cancer therapeutics and androgen signaling pathways. Its efficacy in disrupting AR signaling underscores its potential in studying therapeutic strategies for hormone-resistant cancers. -
Androgen Receptor Inhibitor
AR Antagonist 2 is a potent inhibitor of the androgen receptor (AR), demonstrating an IC50 of 0.95 μM. This compound is crucial for cancer research, particularly in studies exploring androgen-driven pathways and potential therapeutic strategies in hormone-dependent malignancies. Its efficacy makes it a valuable tool for investigating AR-related biological mechanisms. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 12 is a potent orally active antagonist of the androgen receptor, exhibiting an IC50 of 0.30 μM. It effectively inhibits the transcriptional activity of variant androgen receptor mutants and suppresses the proliferation of androgen receptor-positive prostate cancer cell lines. Additionally, this compound obstructs androgen receptor nuclear translocation and demonstrates tumor growth inhibition in a C4-2B xenograft mouse model. Androgen Receptor Antagonist 12 is a valuable tool for research in prostate cancer biology. -
Antiandrogen Agent
Ludaterone is an antiandrogen agent that functions by inhibiting androgen receptor activity. It exhibits strong antiandrogenic properties, making it relevant in research focused on androgen-dependent diseases, such as prostate cancer. This compound is valuable for studies investigating hormonal modulation and potential therapeutic strategies for androgen-related disorders. -
Androgen Receptor Ligand
Androgen Receptor Ligand 4 is a selective ligand for the androgen receptor, exhibiting an IC50 greater than 100 µM. This compound is valuable in research applications focused on androgen signaling pathways and their role in adolescent development. Its function in modulating androgen receptor activity makes it essential for studies investigating hormonal influences on growth and maturation. -
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.
