Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
Androgen blocker
Cyproterone is an antiandrogen that functions by blocking androgen receptors, thereby inhibiting the actions of testosterone. It is primarily utilized in research investigating hypersexuality and prostate cancer, offering insights into hormonal regulation and therapeutic approaches to these conditions. Cyproterone serves as a valuable tool in studying androgen-mediated pathways and their implications in various diseases. -
Biochemical Assay Reagent
17β-Acetoxy-2α-bromo-5α-androstan-3-one is a biochemical assay reagent that functions as a steroid derivative. This compound exhibits significant biological activity as a selective androgen receptor modulator, making it useful for research focused on steroid hormone signaling and metabolic processes. It is valuable for studies investigating androgen-related disorders and the mechanistic pathways influenced by androgens in various biological systems. -
Drug Impurity
Enzalutamide impurity 4 is a recognized impurity associated with Enzalutamide, a potent androgen receptor inhibitor. This compound is essential for analytical research, particularly in assessing the purity and stability of Enzalutamide formulations. It serves as a valuable tool in drug development and quality control processes, facilitating the identification and quantification of impurities in pharmaceutical applications. -
Drug Derivative
(3β,5α)-Androstan-3-amine hydrochloride is a synthetic derivative of the steroid hormone androstenedione, targeting androgen receptors. This compound exhibits significant biological activity, facilitating research in hormonal studies and androgenic activity. It is particularly relevant for investigating steroid signaling pathways and may have applications in drug discovery and development related to androgen-mediated physiological processes. -
Endogenous metabolites
2α-Methyl androsterone is an anabolic androgenic steroid that acts as a metabolite of mesterolone and drostanolone. It exhibits key biological activities related to androgen receptors, playing a significant role in various androgen-dependent processes. This compound is primarily utilized in research applications focused on steroid hormone metabolism and the development of anabolic therapies. -
Apalutamide Metabolite
Apalutamide-COOH is a metabolite of the androgen receptor antagonist, Apalutamide, which exhibits competitive inhibition with an IC50 of 16 nM. This compound is useful in biological research for studying metabolite activity and its implications in androgen receptor signaling pathways. Its application can aid in understanding the pharmacokinetics and dynamics of Apalutamide in various cellular contexts. -
Abiraterone Metabolite
Abiraterone sulfate is a metabolite of Abiraterone, functioning as a potent and irreversible inhibitor of the CYP17A1 enzyme. This compound exhibits antiandrogen activity, making it significant in the study of androgen receptor signaling pathways. It is primarily utilized in cancer research, particularly for investigating therapies targeting prostate cancer and androgen biosynthesis. -
Stable Isotope
p,p'-DDE-d8 is a deuterated form of p,p'-DDE, a significant metabolite of the environmental contaminant dichlorodiphenyltrichloroethane (DDT). This compound acts as a potent antagonist of the androgen receptor, exhibiting an IC50 value of 5 μM and a Ki of 3.5 μM. p,p'-DDE-d8 is valuable in biological research for studying receptor interactions and the environmental impact of DDT metabolites on endocrine function. -
Metabolite
Abiraterone sulfate N-oxide is a significant metabolite of Abiraterone, primarily functioning as a carboxylic acid. This compound plays a crucial role in the study of prostate cancer by providing insights into the metabolic pathways and therapeutic effects of Abiraterone. Its biological activity is of interest in research focused on androgen receptor modulation and cancer progression. -
Abiraterone Metabolite
Abiraterone N-oxide is a metabolite of Abiraterone, a potent and irreversible inhibitor of CYP17A1. This compound exhibits significant antiandrogen activity, making it valuable for research on prostate cancer and androgen-dependent tumors. Abiraterone N-oxide can be utilized in studies investigating metabolic pathways and resistance mechanisms associated with androgen receptor signaling. -
Androgen Receptor Antagonist
RU 56279 is a potent androgen receptor (AR) antagonist that exhibits strong systemic anti-androgenic activity. As a significant metabolite of RU 56187 and RU 58841, it serves as a valuable tool for constructing AR-targeted prodrug systems. RU 56279 is applicable in research focused on AR-positive tumor cells, facilitating studies of AR signaling pathways and potential therapeutic interventions. -
hAR Antagonist
3-Oxochol-5-en-24-oic acid is a potent antagonist of the human androgen receptor (hAR) with an IC50 value of 119.4 nM. This bile acid, produced by the intestinal microbiota, demonstrates significant inhibitory effects on prostate cancer cell growth. Additionally, it enhances the efficacy of anti-PD-1 therapy in animal models by modulating the differentiation of CD8+ T cells. 3-Oxochol-5-en-24-oic acid is valuable for research into host immunity regulation and anti-tumor mechanisms. -
PROTAC Linkers
Boc-Pip-alkyne-Ph-COOH is a PROTAC linker designed for use in the synthesis of targeted protein degraders. It facilitates the development of PROTACs, including ARD-266, which effectively promotes degradation of the androgen receptor in AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, exhibiting DC50 values of 0.2-1 nM. This compound features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it essential for click chemistry applications in chemical biology research. -
AR Antagonist
Androgen Receptor Antagonist 1 is a potent full antagonist of the androgen receptor (AR) with an IC50 of 59 nM. This compound is suitable for the development of PROTAC AR degraders, demonstrating effective AR protein degradation in LNCaP cells—24% degradation at 1 μM and 47% at 10 μM. Its applications extend to studies in prostate cancer research and AR signaling pathways. -
Androgen Receptor Ligand
Androgen Receptor Ligand 3 is a selective ligand for the androgen receptor (AR), designed for targeted protein degradation applications. It is chemically linked to an inhibitor of apoptosis protein (IAP) ligand, facilitating the formation of an ERα PROTAC degrader. This compound provides a valuable tool for studying androgen receptor signaling pathways and can be utilized in research focused on androgen-related diseases, including prostate cancer. -
Ligand for Target Protein
ABM-14 is a ligand that specifically targets the androgen receptor (AR) for use in PROTAC (proteolysis-targeting chimera) applications. It facilitates the recruitment of AR via a linker to the VHL (von Hippel-Lindau) E3 ubiquitin ligase, enabling targeted degradation of AR. This compound is valuable for research in AR-related signaling pathways and therapeutic strategies for conditions such as prostate cancer. -
PROTAC Target Protein Ligand
AR ligand-30 is a potent target protein ligand for PROTAC applications, specifically designed to engage with Bavdegalutamide. This compound facilitates targeted protein degradation, offering vital insights into therapeutic strategies for prostate cancer research. Its ability to modulate androgen receptor signaling makes it a valuable tool for investigating novel cancer treatment pathways.
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AR Ligand
Androgen Receptor Ligand 1 is an androgen receptor (AR) ligand that engages with CRBN E3 ligase through a specialized linker, facilitating the creation of an AR PROTAC degrader. This compound is essential for investigating the mechanisms of AR signaling and can significantly aid in prostate cancer research. Its unique action promotes targeted protein degradation, providing valuable insights into therapeutic strategies against AR-driven malignancies. -
Ligands for Target Protein for PROTAC
AR Antagonist 14 is a potent ligand for specific target proteins utilized in PROTAC (Proteolysis Targeting Chimeras) applications. This compound facilitates the development of targeted protein degraders, allowing for the selective degradation of androgen receptors. AR Antagonist 14 can be effectively combined with VH 101-amide-piperidine-Pip-alkyne to synthesize PROTAC degraders, enhancing research on targeted therapies in cancer and other diseases. -
AR Inhibitor
AR ligand-48 is an inhibitor of the Androgen Receptor (AR), functioning as a ligand for PROTAC applications. By targeting the AR, this compound facilitates the development of PROTAC AR Degrader-12, enabling researchers to investigate AR degradation pathways. Its utility in studying androgen signaling makes it valuable for research in hormone-related diseases and therapeutic development.
