Catalog No.
Product Name
Application
Product Information
Citations
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CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. -
Androgen Receptor antagonist
EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ?? 6 μM) -
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 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 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 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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Androgen Receptor Antagonist
Androgen Receptor Allosteric Antagonist 1 is a competitive allosteric inhibitor of the androgen receptor, exhibiting a Ki of 9 μM. This compound effectively inhibits R1881-mediated transcriptional activity and cell proliferation, making it a valuable tool for studying prostate cancer. Its unique mechanism of action allows for detailed exploration of androgen receptor signaling pathways in cancer research. -
Progesterone Receptor Inhibitor
CP8754 is a selective antagonist of the human progesterone receptor (hPR), acting primarily by competitively inhibiting the binding of [3H]-progesterone. This compound effectively impedes progesterone-mediated signaling, as evidenced by its ability to inhibit both exogenous luciferase and endogenous alkaline phosphatase expression in vitro, and to suppress rabbit endometrial transformation in vivo. CP8754 exhibits minimal binding affinity for human glucocorticoid receptors, estrogen receptors, and rat androgen receptors, making it a valuable tool for investigating progesterone-related diseases, including breast cancer, endometriosis, uterine fibroids, and hormone-dependent tumors. -
Androgen Receptor PROTAC Degrader
GDC-2992 is an orally bioavailable PROTAC degrader targeting the androgen receptor (AR). With a DC50 of 2.7 nM for AR degradation and an IC50 of 9.7 nM for inhibiting cell proliferation in VCaP cells, GDC-2992 serves as a valuable tool in prostate cancer research. This compound facilitates investigations into the therapeutic potential of targeted protein degradation in androgen receptor-mediated signaling pathways. -
AR Proteolysis-targeting Chimera Degrader
ARD-2051 is a selective and orally active degrader targeting the androgen receptor (AR) via a proteolysis-targeting chimera approach. It demonstrates potent DC50 values of 0.6 nM for AR degradation in prostate cancer cell lines such as LNCaP and VCaP. ARD-2051 exhibits significant anti-tumor efficacy in VCaP xenograft mouse models, making it a valuable tool for prostate cancer research and therapeutic exploration. -
Androgen Receptor Degrader
SARD279 is a potent and selective degrader of the Androgen Receptor, exhibiting a DC50 value of 1099 nM. This compound is particularly valuable for research into prostate cancer, where modulation of androgen receptor levels may play a critical role in disease progression and response to therapy. SARD279's targeted degradation mechanism supports investigations into androgen receptor signaling pathways and its implications in cancer biology. -
PROTAC AR Degrader
AZ'3137 is an orally bioavailable PROTAC-based degrader specifically targeting the androgen receptor (AR). It exhibits a DC50 value of 22 nM for AR degradation and efficiently degrades the L702H mutant variant with a DC50 of 92 nM. AZ'3137 demonstrates significant inhibition of LNCaP cell proliferation with a GI50 of 74 nM and effectively suppresses AR signaling and tumor growth in prostate cancer mouse models. This compound is suitable for studies investigating AR-targeted therapies in prostate cancer. -
AR PROTAC Degrader
(Rac)-GDC-2992 is a PROTAC androgen receptor degrader that effectively reduces androgen receptor levels with a DC50 of 10 nM in VCaP cells. This compound not only disrupts androgen receptor signaling but also facilitates the degradation of the receptor itself. (Rac)-GDC-2992 is primarily utilized in prostate cancer research, providing valuable insights into androgen receptor modulation and therapeutic strategies. -
Androgen Receptor PROTAC Degrader
PROTAC AR Degrader-11 is a targeted degrader of the androgen receptor and androgen receptor splice variant-7, utilizing a proteolysis-targeting chimeric (PROTAC) approach. This compound exhibits significant cytotoxicity against prostate cancer cell lines, specifically CWR22RV1 and VCaP. PROTAC AR Degrader-11 is applicable in prostate cancer research, aiding investigations into androgen receptor modulation and degradation mechanisms. -
Androgen Receptor Degrader
PROTAC AR Degrader-7 is a potent androgen receptor degrader, exhibiting an IC50 value of 3 nM. This bifunctional molecule is designed to engage the androgen receptor through AR ligand-32 while simultaneously recruiting E3 ligase via E3 Ligase Ligand 44 for targeted protein degradation. PROTAC AR Degrader-7 effectively induces ubiquitination and subsequent proteasomal degradation of the androgen receptor, making it a valuable tool for studying androgen receptor signaling and its role in androgen-dependent diseases, particularly prostate cancer. -
AR PROTAC Degrader
TD-802 is an androgen receptor (AR) PROTAC degrader that demonstrates substantial microsomal stability. It exhibits notable antitumor efficacy in vivo, making it a valuable tool for investigating metastatic castration-resistant prostate cancer. This compound is essential for research aimed at understanding AR modulation and its impacts on cancer progression. -
AR PROTAC Degrader
A031 is a potent PROTAC degrader targeting the androgen receptor (AR), demonstrating an IC50 value of less than 0.25 μM for effective AR protein degradation. This compound has shown a significant inhibitory effect on tumor growth in zebrafish models of human prostate cancer (VCaP). A031 is a valuable tool for investigating AR-mediated signaling pathways and potential therapeutic strategies in prostate cancer research. -
AR PROTAC Degrader
PROTAC AR Degrader-5 is a potent androgen receptor (AR) PROTAC degrader, exhibiting an IC50 value of 49 nM. This compound facilitates the targeted degradation of AR, demonstrating significant potential in inhibiting sebaceous plaque formation and promoting hair regeneration. Its mechanism utilizes a bifunctional ligand to recruit an E3 ligase, making it a valuable tool for research in androgen signaling and related therapeutic applications.
