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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 inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
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AR inhibitor downregulator
AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.- Qian Liu, .et al. , Nat Commun, 2024, Feb 7;15(1):1148 PMID: 38326303
- Soumitra Ghosh, .et al. , bioRxiv, 2023, Jun 28:2023.06.28.546870 PMID: 37425957
- Qian Liu, .et al. , Research Square, 2023, Mar 10
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CYP17A1/androgen synthesis inhibitor
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues. -
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 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 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. -
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. -
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. -
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. -
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. -
mTORC1 Pathway Inhibitor
CIDD 0067106 is a selective inhibitor of the mTORC1 pathway, specifically designed for targeting androgen receptor-positive (AR+) triple-negative breast cancer (TNBC). It exhibits potent activity against AR+ TNBC cell lines, with a GI50 value of 0.8 μM, indicating its effectiveness in inhibiting cancer cell proliferation. This compound is valuable for research focused on understanding and developing treatments for AR+ TNBC. -
Androgen Receptor Inhibitor
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of the androgen receptor, exhibiting an IC50 of 69 nM for full-length AR and 309 nM for constitutively active truncated AR splice variants (AR1-651). Its ability to selectively target these receptors makes it a valuable tool for research into androgen signaling pathways. Ailanthone is applicable in studies related to prostate cancer and other conditions influenced by androgen receptor activity. -
Androgen Receptor Inhibitor
Masofaniten is a potent androgen receptor inhibitor, functioning through the selective modulation of androgen receptor activity. It exhibits significant antitumor efficacy against prostate cancer, making it a valuable tool for studying androgen signaling pathways and exploring therapeutic options for prostate cancer treatment. Researchers can utilize Masofaniten to investigate the biological mechanisms of androgen receptor antagonism and its potential in cancer therapy. -
NONO Inhibitor
(R)-SKBG-1 is a covalent inhibitor that targets the RNA binding protein NONO. This compound effectively reduces the expression of the androgen receptor (AR) and its splice variants, demonstrating an IC50 of 3.1 µM for AR-FL mRNA and 5.5 µM for AR-V7 mRNA. By stabilizing the interaction between NONO and mRNA, (R)-SKBG-1 disrupts the gene regulatory networks in cancer cells, thereby inhibiting cell proliferation. This reagent is valuable in research focusing on cancers associated with NONO dysfunction, including prostate cancer. -
AR-DBD Inhibitor
VPC-14449 is a selective inhibitor targeting the DNA-binding domain of the androgen receptor (AR-DBD), demonstrating an IC50 value of 0.34 μM for full-length human AR. This compound effectively diminishes the binding capacity of both full-length AR and its variants to chromatin, thereby influencing androgen receptor-mediated transcription. VPC-14449 is valuable for research focused on prostate cancer and the role of AR in tumor progression. -
Ar-V7 Inhibitor
Ar-V7-IN-1 is a potent inhibitor of the androgen receptor variant 7 (Ar-V7), effectively inhibiting its transcriptional activity. This compound demonstrates an eGFP IC50 value of 1232 nM and a PSA IC50 of 1391 μM. Ar-V7-IN-1 is primarily utilized in research related to prostate cancer, making it a valuable tool for investigating the mechanisms of AR-mediated signaling and the associated implications in cancer biology. -
AR-DBD Inhibitor
VPC-14228 is a selective inhibitor of the androgen receptor DNA binding domain (AR-DBD). It interrupts the interaction between the androgen receptor and DNA, thereby preventing AR-mediated transcriptional activation. VPC-14228 effectively inhibits the activity of both full-length androgen receptors and the splice variant AR-V7 by disrupting AR binding to chromatin, demonstrating high selectivity for other nuclear receptors such as estrogen and progesterone receptors. This compound is applicable for research into prostate cancer. -
Androgen Receptor Inhibitor/GPR142 Antagonist
CLP-3094 is a selective androgen receptor (AR) inhibitor that targets the binding function 3 (BF3) region, effectively reducing AR transcriptional activity with an IC50 of 4 μM. In addition, CLP-3094 serves as a potent antagonist of GPR142, making it a valuable compound for research into androgen receptor modulation and its implications in various biological processes. Its dual function positions CLP-3094 as a useful tool in studies related to androgen signaling and GPR142-related pathways. -
Androgen Receptor Inhibitor
ET516 is a potent inhibitor of the Androgen Receptor (AR), effectively disrupting AR signaling pathways. This compound demonstrates significant anti-proliferative effects and inhibits tumor growth in prostate cancer cells with AR-resistant mutants. ET516 is valuable for research applications focused on understanding AR-related mechanisms in prostate cancer and developing targeted therapies. -
Androgen Receptor Inhibitor
Androgen receptor-IN-6 is a potent inhibitor of the androgen receptor, specifically targeting the disordered N-terminal domain (NTD) with an in vitro IC50 of 0.12 μM. This compound demonstrates favorable membrane permeability in Caco2 cells and exhibits oral bioavailability in male CD-1 mice, with an F/% of 16%. It serves as a valuable tool for research into androgen receptor signaling pathways and the development of therapeutic strategies for androgen-dependent conditions. -
AR NTD Inhibitor
Ralaniten triacetate is an orally active inhibitor that targets the N-terminal domain (NTD) of the androgen receptor (AR). This first-in-class compound demonstrates efficacy against full-length androgen receptors as well as resistance-related variants, including AR-v7. It is primarily utilized in research focusing on androgen receptor signaling pathways and their role in hormone-driven cancers. -
Androgen Receptor Inhibitor
A4B17 is an androgen receptor N-terminal inhibitor that selectively targets the androgen receptor, interfering with its transcriptional activity. It is primarily used in research related to androgen-responsive prostate cancer, allowing for investigations into therapeutic strategies and mechanisms of resistance. A4B17 provides a valuable tool for studying androgen receptor signaling pathways and their implications in tumor progression. -
AR Inhibitor
VPC-13566 is a selective inhibitor of the androgen receptor (AR), exerting its effects via inhibition of AR transcriptional activity. This compound effectively suppresses the proliferation of AR-dependent prostate cancer cell lines in vitro. VPC-13566 is a valuable tool for investigating the AR signaling pathway and identifying novel AR-interacting partners, making it relevant for cancer research applications. -
Androgen Receptor Inhibitor
Faznolutamide is an androgen receptor inhibitor that interferes with androgen signaling. This compound exhibits significant antiandrogenic activity, making it a valuable tool for investigating androgen-dependent biological processes. It is used in research focused on prostate cancer and other conditions influenced by androgens. -
Androgen Receptor Inhibitor
Bifluranol is an androgen receptor inhibitor that functions by blocking the action of androgens, which are hormones that can promote the growth of certain cancers. This compound exhibits anti-androgenic activity, making it valuable in research addressing hormone-dependent cancers, such as prostate cancer. Bifluranol can be utilized in studies focused on understanding androgen signaling pathways and developing therapeutic strategies targeting androgen-related conditions. -
Androgen receptor Inhibitor
Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor, demonstrating significant anticancer activity. This compound also disrupts the production of pro-inflammatory cytokines, including IL-17A, IL-17F, and IFN-γ, making it a valuable tool for studying androgen receptor signaling and its role in cancer and immune responses. Its multifaceted activity positions Androgen receptor-IN-5 as a promising candidate for research in cancer therapeutics and inflammation modulation. -
AR Degrader/CYP17A1 Inhibitor
YXG-158 is an orally active androgen receptor (AR) degrader and CYP17A1 inhibitor. It exhibits AR degradation activity with a DC50 value of 1.28 μM and inhibits CYP17A1 with an IC50 value of 100 nM. This compound is particularly relevant for research applications focused on enzalutamide-resistant prostate cancer, providing a valuable tool for investigating therapeutic strategies in this context. -
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. -
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. -
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 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 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 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 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. -
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.
