Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC AR/AR-V7 degrader
PROTAC AR/AR-V7 Degrader-1 (27c) is a PROTAC-based dual degrader targeting both full-length androgen receptor (AR) and its splice variant AR-V7, which is implicated in resistance to androgen deprivation therapies. It exhibits DC₅₀ values of 2.67 μM for AR and 2.64 μM for AR-V7, effectively promoting their proteasomal degradation. By eliminating both isoforms, compound 27c induces apoptosis in AR-driven cancer cells, making it a promising therapeutic candidate for castration-resistant prostate cancer (CRPC) and other AR/AR-V7–dependent malignancies. -
PROTAC AR degrader
ARD-1676 is an orally bioavailable PROTAC degrader of the androgen receptor (AR), composed of an AR-binding ligand and a cereblon-recruiting moiety. It effectively induces AR degradation both in vitro and in vivo, and demonstrates significant antitumor activity by inhibiting VCaP prostate cancer xenograft growth in mouse models. ARD-1676 represents a promising therapeutic strategy for targeting AR-driven malignancies. -
PROTAC AR degrader
ARD-61 is a highly potent and selective PROTAC degrader of the androgen receptor (AR), also capable of degrading progesterone receptors (PR) in AR-positive cancer cell lines. It induces apoptosis and demonstrates significant antitumor efficacy in vivo, effectively inhibiting tumor growth in the MDA-MB-453 xenograft mouse model. Additionally, ARD-61 is equipped with an alkyne functional group, enabling its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, facilitating conjugation and functionalization for chemical biology applications. -
PROTAC AR Degrader
ARD-2128 is a highly potent, orally bioavailable PROTAC degrader targeting the androgen receptor (AR). It efficiently reduces AR protein levels, downregulates AR-regulated gene expression in tumor tissues, and inhibits tumor growth without observable toxicity. ARD-2128 is a promising tool for prostate cancer research. -
PROTAC AR-V7 degrader
MTX-23 is an androgen receptor (AR)-targeting PROTAC that degrades both AR-FL and the splice variant AR-V7. It effectively inhibits prostate cancer cell proliferation and induces apoptosis, making it a promising tool for studying AR signaling and therapeutic resistance in prostate cancer. -
androgen receptor (AR) PROTAC degrader
BMS-986365 (CC-94676) is an orally active, selective PROTAC degrader targeting the androgen receptor (AR), including AR mutants. It functions via cereblon (CRBN)-mediated ubiquitination and proteasomal degradation of AR. BMS-986365 exhibits strong in vivo efficacy by suppressing AR signaling and inhibiting tumor growth in advanced prostate cancer models, making it a promising candidate for therapeutic development. -
androgen receptor (AR) PROTAC degrader
Bavdegalutamide (ARV-110) is an orally active and highly specific PROTAC degrader targeting the androgen receptor (AR). It induces ubiquitination and proteasomal degradation of AR, offering a novel therapeutic approach for AR-driven diseases such as prostate cancer. -
Androgen Receptor (AR) degrader
ARCC-4 is a low-nanomolar PROTAC degrader targeting the androgen receptor (AR), with a DC₅₀ of 5 nM. Based on enzalutamide and incorporating a von Hippel-Lindau (VHL) E3 ligase ligand, ARCC-4 efficiently degrades both wild-type and clinically relevant AR mutants linked to resistance to antiandrogen therapy. It outperforms enzalutamide in potency and degradation efficacy, making it a promising candidate for advanced prostate cancer research. -
PROTAC Androgen Receptor Degrader
ARD-266 is a potent PROTAC degrader targeting the Androgen Receptor (AR) through a von Hippel-Lindau E3 ligase mechanism. It effectively induces AR protein degradation in AR-positive prostate cancer cell lines, including LNCaP, VCaP, and 22Rv1, with DC50 values ranging from 0.2 to 1 nM. Additionally, ARD-266 features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating versatile applications in chemical biology research. -
PROTAC AR Degrader
ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand. -
Androgen Receptor Inhibitor
SC428 is a selective androgen receptor (AR) inhibitor that targets the N-terminal domain, effectively reducing the transactivation of various isoforms including AR-V7, AR-v567es, and full-length AR (AR-FL) along with its LBD mutants. This compound inhibits the nuclear translocation, chromatin binding, and subsequent transcription of AR-regulated genes in response to androgens. Additionally, SC428 demonstrates significant anti-proliferative effects on tumor cells in vitro and promotes apoptosis in vivo, particularly in mice bearing 22RV1 xenografts. Its application in cancer research highlights its potential utility in targeting androgen-dependent tumors. -
Androgen Receptor PROTAC Degrader
PROTAC AR Degrader-8 is an androgen receptor (AR) PROTAC degrader that effectively induces degradation of full-length AR (AR-FL) with DC50 values of 0.018 μM in 22Rv1 cells and 0.14 μM in LNCaP cells, as well as degrading the AR-V7 variant with a DC50 of 0.026 μM in 22Rv1 cells. This compound exhibits potent inhibition of cancer cell proliferation, with IC50 values of 0.038 μM and 1.11 μM in 22Rv1 and LNCaP cells, respectively. PROTAC AR Degrader-8 induces G2/M cell cycle arrest and promotes apoptosis in 22Rv1 cells, demonstrating significant anticancer efficacy in both murine and zebrafish models. It is a valuable tool for investigating mechanisms underlying prostate cancer and castration-resistant prostate cancer. -
Androgen Receptor Degrader
ZC9 is a novel androgen receptor (AR) degrader that directly binds to AR, inhibiting its Dihydrotestosterone-induced nuclear translocation. By promoting AR degradation through the ubiquitin-proteasome system, ZC9 effectively suppresses AR transcriptional activity, leading to a significant decrease in the mRNA levels of downstream genes such as PSA, TMPRSS2, and PMEPA1. Additionally, ZC9 induces apoptosis and demonstrates notable anticancer effects in prostate cancer models, making it a valuable tool for research in androgen signaling and cancer therapeutics. -
Androgen Receptor Antagonist
AR Antagonist 15 is an orally bioavailable antagonist of the androgen receptor (AR), exhibiting an IC50 of 97 nM for ART787A. This compound inhibits AR nuclear translocation, prevents AR homodimerization, and suppresses transcription of AR-regulated genes through competitive binding at the ligand binding pocket. Additionally, AR Antagonist 15 significantly reduces prostate-specific antigen (PSA) levels and induces apoptosis by decreasing the expression of proteins involved in apoptotic pathways. This reagent is relevant for studies investigating the mechanisms of prostate cancer. -
Androgen Receptor Inhibitor
Ac-PPPHPHARIK-NH2 is an androgen receptor inhibitor that disrupts the interaction between the androgen receptor and Src. By preventing this binding, it effectively inhibits androgen or estrogen-induced receptor activation in cancer cells, thereby modulating related signaling pathways. This compound has been shown to impede cell cycle progression and suppress tumor growth, making it a valuable tool for research in cancer biology and hormone receptor signaling. -
Androgen Receptor Antagonist
Deutenzalutamide-d3 is a deuterium-labeled analog of Enzalutamide, an androgen receptor (AR) antagonist. It exhibits potent activity with an IC50 of 36 nM in LNCaP prostate cancer cells. This reagent is valuable for studying androgen receptor signaling pathways and resistance mechanisms in prostate cancer research. -
Androgen Receptor Inhibitor
Androgen receptor-IN-7 is a potent inhibitor of the androgen receptor (AR), demonstrating significant anticancer activity against PC-3 (IC50 = 370.37 nM) and LNCaP cell lines through both AR-dependent and AR-independent mechanisms. This compound induces reactive oxygen species (ROS) production in PC-3 cells, highlighting its potential role in oncological studies. Androgen receptor-IN-7 is useful for research focused on prostate cancer and related therapeutic strategies. -
Androgen Receptor Antagonist
Atraric acid, known as Methyl atrarate, functions as a specific antagonist of androgen receptors (AR). This compound demonstrates significant anti-inflammatory and anticancer properties by downregulating the expression of the prostate-specific antigen gene in LNCaP and C4-2 cell lines. Additionally, atraric acid inhibits nitric oxide synthesis and cytokine production while suppressing the MAPK-NFκB signaling pathway. Its utility in research extends to investigations of prostate diseases and inflammatory conditions. -
Androgen Receptor Inhibitor
Fenarimol is a selective androgen receptor inhibitor with an IC50 value of 19 µM. This compound has been shown to downregulate the mRNA expression of key genes, including PBP C3, ODC, and IGF-1. Fenarimol serves as a valuable tool in research investigating androgen signaling pathways and its role in various biological processes. Additionally, its fungicidal properties may provide insights into the interplay between hormonal regulation and fungal growth mechanisms. -
Androgen Receptor Inhibitor
AZD9750 is an orally bioavailable proteolysis-targeting chimera (PROTAC) that acts as an androgen receptor (AR) inhibitor. It facilitates the proteasome-dependent degradation of both wild-type AR and the ARL702H resistance mutant by targeting and binding to AR and cereblon (CRBN). In in vitro studies, AZD9750 effectively inhibits AR signaling and demonstrates significant anti-tumor activity in mouse prostate cancer xenograft models. This compound is valuable for research focused on prostate cancer. -
Androgen Receptor/glucocorticoid Receptor Inhibitor
GA32 is a dual inhibitor of the androgen receptor (AR) and glucocorticoid receptor (GR), exhibiting IC50 values of 0.13 μM for AR and 0.83 μM for GR. This compound effectively inhibits the proliferation of castration-resistant prostate cancer cells that exhibit resistance to Enzalutamide, demonstrating its potential in both in vitro and in vivo research applications. GA32 serves as a valuable tool for studies focused on targeting AR and GR pathways in cancer biology. -
Antiandrogen
RU 59063 is an N-substituted arylthiohydantoin that functions as a potent antiandrogen through its high binding affinity for the rat androgen receptor (Ki: 0.71 nM, rAR). This nonsteroidal compound serves as a valuable radioprobe for studies involving androgen receptor signaling. It is widely utilized in research applications focusing on androgen signaling pathways and related therapeutic targets. -
Metandienone Metabolite
6β-Hydroxy Metandienone is a metabolic derivative of the anabolic androgenic steroid Metandienone, primarily acting as an androgen receptor agonist. This compound exhibits anabolic properties, contributing to muscle growth and strength enhancement. Its biological activity makes it valuable for research in steroid metabolism, performance enhancement, and the study of anabolic steroid effects in various biological systems. -
Stable Isotope
p,p'-DDE-13C12 is a stable isotope-labeled variant of p,p'-DDE, a well-known metabolite of the persistent pesticide dichlorodiphenyltrichloroethane (DDT). This compound functions 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-13C12 can be utilized in biological research to study endocrine disruption and receptor signaling pathways related to androgen activity. -
Abiraterone acetate Degradation Product x
Anhydro abiraterone is a degradation product of Abiraterone acetate, a selective and irreversible inhibitor of CYP17A1, known for its antiandrogen activity. This compound plays a critical role in the study of metabolic pathways and pharmacokinetics of steroidogenesis inhibitors. Research applications include the investigation of androgen receptor signaling and the development of therapeutic strategies for prostate cancer. -
Abiraterone Metabolism
5,6-Dihydroabiraterone is a metabolic derivative of Abiraterone, an irreversible inhibitor of CYP17A1 that exhibits significant antiandrogen effects. This compound plays a crucial role in studying the metabolic pathways of Abiraterone and contributes to understanding its antitumor activity in castration-resistant prostate cancer (CRPC). Research applications include evaluating the pharmacokinetics and metabolic fate of androgen receptor-targeting agents in cancer models. -
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. -
CYP11A1 Inhibitor
CYP11A1-IN-1 is an inhibitor of cytochrome P450 11A1 (CYP11A1), exhibiting an IC50 range of 201-2000 nM. This compound is valuable for research focusing on steroid hormone synthesis and the role of androgens in diseases such as prostate cancer. It offers potential applications in studies related to androgen receptor-dependent pathways and their therapeutic implications. -
Androgen Receptor Antagonist
N-Desmethyl-Apalutamide is an active metabolite of Apalutamide, primarily functioning as an androgen receptor antagonist. This compound exhibits moderate potency in inhibiting androgen receptor activity and accounts for approximately one-third of the pharmacological effect of its parent compound. N-Desmethyl-Apalutamide is predominantly metabolized by CYP2C8 and CYP3A4 enzymes, while also serving as a moderate to strong inducer of CYP3A4 and CYP2B6. Its high plasma protein-binding capacity further enhances its utility in research applications related to androgen receptor modulation and therapeutic exploration in prostate cancer treatment. -
Flutamide Metabolite
Flu-6 is a metabolite of Flutamide, primarily targeting androgen receptors. It is generated in the liver through the action of NADPH: cytochrome P450 reductase (CPR). Flu-6 exhibits significant biological activity in inhibiting the progression of prostate cancer, making it a valuable reagent for research in oncology and drug metabolism studies. -
Stable Isotope
Abiraterone acetate-d4 is the deuterium-labeled form of Abiraterone acetate, a potent and selective irreversible inhibitor of CYP17A1 with notable antiandrogen activity. This stable isotope is utilized in various biological research applications, including pharmacokinetic studies and metabolic profiling, allowing for precise tracking of the compound's fate in biological systems. As a proagent of Abiraterone, it provides valuable insights into androgen receptor signaling pathways and related therapeutic interventions. -
3βHSD1 Inhibitor
3βHSD1-IN-1 is a potent inhibitor of 3β-hydroxysteroid dehydrogenase 1 (3βHSD1), demonstrating an IC50 value of 55 nM. This compound effectively suppresses androgen receptor activity, making it a valuable tool for the investigation of androgen-dependent processes. 3βHSD1-IN-1 is applicable in research related to prostate cancer and other disorders linked to steroid hormone metabolism. -
Steroid Anti-androgen Agent
Osaterone acetate is an orally active steroid anti-androgen agent that primarily targets the androgen receptor. It acts as a competitive antagonist and inhibits 5α-reductase, leading to decreased levels of dihydrotestosterone (DHT) and mitigating the proliferative effects of both testosterone and DHT on prostate cells. This compound is predominantly used for the treatment of benign prostatic hyperplasia (BPH) in dogs, providing rapid symptom relief while preserving the fertility of breeding animals. -
Androgen Receptor Modulator
MK-4541 is a selective androgen receptor modulator (SARM) that functions primarily as an antagonist to inhibit 5α-reductase activity. This compound demonstrates potent anti-proliferative effects and induces apoptosis in androgen receptor-positive prostate cancer cells. In preclinical studies, MK-4541 significantly inhibited the growth of R3327-G prostate tumors in a xenograft mouse model, highlighting its potential for targeted prostate cancer therapy. -
Finerenone Racemate
(Rac)-Finerenone is a racemate of the selective, orally bioavailable nonsteroidal mineralocorticoid receptor (MR) antagonist, exhibiting an IC50 value of 18 nM. This compound demonstrates significant selectivity over glucocorticoid receptors (GR), androgen receptors (AR), and progesterone receptors, with a selective ratio exceeding 500-fold. (Rac)-Finerenone is utilized in research applications focused on cardiovascular and renal health, and is being investigated for its potential therapeutic benefits in managing disorders related to mineralocorticoid receptor activation. -
Aromatase Inhibitor/AR Agonist
17β-Hydroxy exemestane is an aromatase inhibitor and androgen receptor (AR) agonist with an IC50 of 69 nM and 39.6 nM, respectively. This compound exhibits selective binding towards the AR compared to estrogen receptor α (ERα), demonstrating an IC50 of 21.2 μM. In biological assays, 17β-Hydroxy exemestane promotes the growth of AR- and ERα-positive MCF-7 cells and T47D breast cancer cells, with EC50 values of 2.7 μM and 0.43 nM for AR-mediated growth. Notably, it also mitigates proliferation in testosterone-treated aromatase-overexpressing MCF-7 cells and demonstrates protective effects on serum cholesterol and bone density in ovariectomized rat models. -
Phenylurea Herbicide
Linuron is a phenylurea herbicide that functions primarily as a photosystem II inhibitor, effectively controlling the growth of grasses and weeds in diverse agricultural settings. In addition to its herbicidal properties, Linuron acts as an orally active competitive antagonist of the androgen receptor, displaying an EC50 of 200 μM in rat systems and 20 μM in human systems. Notably, Linuron is associated with reproductive toxicity in animal models and exhibits endocrine-disrupting capabilities, making it a significant compound for research into environmental health and toxicology. -
Metabolite of 17α-methyltestosterone
11β-Hydroxy-17α-methyltestosterone is a metabolite of 17α-methyltestosterone, acting primarily through androgen receptors. This compound exhibits significant androgenic activity, making it useful for research in steroid metabolism and pharmacological studies. Its role in understanding anabolic steroid effects and potential therapeutic applications in hormone-related disorders is noteworthy. -
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. -
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.
