Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC ER Degrader
SNIPER(ER)-110 is a PROTAC compound designed for targeted degradation of the estrogen receptor (ER). Comprising an IAP ligand and an estrogen ligand linked together, SNIPER(ER)-110 effectively induces ER protein degradation, exhibiting DC50 values of less than 3 nM at 4 hours and approximately 7.7 nM at 48 hours. This reagent is valuable for studies investigating ER-related signaling pathways and therapeutic strategies in hormone-dependent cancers. -
Target Protein Ligand-Linker Conjugates
Fluocinolone acetonide 3-benzylaniline is a glucocorticoid receptor agonist-linker conjugate that serves as a precursor for the development of antibody-drug conjugates (ADCs) targeting CD40. This compound facilitates the targeted delivery of therapeutics, enhancing efficacy while minimizing off-target effects. Its role in the synthesis of ADCs makes it a valuable tool for research applications in immunology and targeted cancer therapy. -
Ligand and Linker Conjugates
ER ligand-9 is a conjugate targeting the estrogen receptor (ER) that serves as a versatile linker for PROTAC synthesis. This compound is essential for the development of targeted protein degraders, particularly in the context of androgen receptor degradation. Its application in research includes studying the modulation of estrogen signaling pathways and investigating therapeutic strategies against ER-positive cancers. -
Androgen Receptor Agonist
11-Ketodihydrotestosterone (11-KDHT) is a potent androgen receptor (AR) agonist, exhibiting a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. This endogenous steroid, a metabolite of 11β-Hydroxyandrostenedione, plays a significant role in regulating gene expression, protein synthesis, and cellular growth, particularly in androgen-dependent prostate cancer cells. Its ability to activate AR makes it valuable for research into androgen signaling pathways and the development of therapeutic strategies for prostate cancer. -
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 Degrader
EN1441 is a covalent degrader that targets the androgen receptor (AR) and its truncated variant AR-V7, exhibiting an EC50 value of 4.2 μM. This compound effectively degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is a valuable tool for research focused on androgen-independent prostate cancers, providing insights into therapeutic strategies for this challenging disease. -
Androgen Receptor Antagonist
EPI-7170 is a potent androgen receptor (AR) antagonist that targets the N-terminal structural domain of the receptor. It effectively inhibits the transcriptional activity of full-length androgen receptor (FL-AR) and its splice variants, providing therapeutic potential against enzalutamide-resistant castration-resistant prostate cancer (CRPC). This compound is valuable for research into mechanisms of resistance in prostate cancer and the development of novel therapeutic strategies. -
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. -
Honokiol Analog
Honokiol DCA, a dichloroacetate analog of Honokiol, primarily targets the androgen receptor (AR). This compound exhibits significant inhibitory activity against the proliferation of human prostate cancer cells in vitro. It is useful for research into cancer biology and androgen receptor signaling pathways. -
Active Androgen
11-Ketotestosterone, an active androgen and oxidized derivative of testosterone, exhibits significant biological activity in androgen receptor modulation. It plays a crucial role in various biological processes such as muscle growth, development of secondary sexual characteristics, and regulation of energy metabolism. This compound is utilized in research applications focused on endocrine function, steroid hormone signaling, and the impact of androgens in muscle physiology and overall health. -
Androgen Receptor Antagonist
Rezvilutamide is an orally active androgen receptor antagonist. This compound exhibits significant biological activity in inhibiting androgen receptor signaling, making it a valuable tool in prostate cancer research. Its application in preclinical studies aids in understanding the mechanisms of androgen-dependent tumors and evaluating potential therapeutic strategies. -
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-NTD Antagonist
Ralaniten is a potent and orally active antagonist of the androgen receptor N-terminal domain (AR-NTD). It effectively inhibits AR transcriptional activity, displaying an IC50 of 7.4 μM. Ralaniten is primarily applied in research concerning castration-resistant prostate cancer (CRPC), offering insights into potential therapeutic strategies targeting this condition. -
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. -
Stable Isotope
Enzalutamide-d6 is a deuterium-labeled version of the androgen receptor antagonist Enzalutamide (MDV3100). This stable isotope is utilized in research to trace metabolic pathways and study the pharmacokinetics of AR-targeted therapies. With an IC50 of 36 nM in LNCaP prostate cancer cells, Enzalutamide serves a critical role in prostate cancer research and drug development. -
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. -
AR Antagonist
JNJ-63576253 is a potent and orally active antagonist of the androgen receptor (AR), exhibiting IC50 values of 37 nM for the F877L mutant AR and 54 nM for wild-type AR in LNCaP cells. This compound serves as a valuable tool for investigating androgen receptor signaling pathways and is particularly relevant for research on castration-resistant prostate cancer (CRPC). Its efficacy in blocking AR activity makes it a significant candidate for therapeutic studies targeting advanced prostate carcinoma. -
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 Antagonist
Gumelutamide is a tetrahydropyridopyrimidine compound functioning as an androgen antagonist. It exhibits significant antiandrogenic and antineoplastic properties, making it valuable in the study of androgen-dependent cancers. This compound is primarily utilized in research applications aimed at understanding the mechanisms of androgen receptor signaling and developing targeted therapies for prostate cancer. -
Androgen Receptor agonist
Cl-4AS-1 is a potent steroidal androgen receptor (AR) agonist with an IC50 of 12 nM. Additionally, it serves as an inhibitor of 5α-reductase types I and II, exhibiting IC50 values of 6 nM and 10 nM, respectively. This compound is valuable for studying androgen signaling pathways and investigating potential therapeutic applications in conditions related to androgen receptor modulation and steroid metabolism. -
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. -
Stable Isotope
Darolutamide-d4 is a deuterium-labeled analog of Darolutamide, a competitive androgen receptor (AR) antagonist. It demonstrates a Ki of 11 nM for rat wild-type AR and an IC50 of 26 nM for human wild-type AR-mediated transcriptional activation, effectively inhibiting testosterone-induced AR nuclear translocation. This reagent selectively impacts AR-positive cells by disrupting AR-dependent signaling pathways, while its active metabolite retains full antagonistic activity against AR mutants. Darolutamide-d4 is valuable for research into prostate cancer, particularly in studies focused on androgen receptor-dependent mechanisms. -
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. -
Nonsteroidal Androgen receptor Antagonist
BMS-641988 is a nonsteroidal androgen receptor antagonist that demonstrates a binding affinity with a Ki of 1.7 nM. This compound exhibits notable anticancer activity, making it valuable for research applications in oncology. Its ability to inhibit androgen receptor signaling positions BMS-641988 as a significant tool for exploring therapeutic strategies against androgen-dependent cancers. -
Stable Isotope
11-Ketodihydrotestosterone-d3 is a deuterium-labeled derivative of 11-Ketodihydrotestosterone, an endogenous steroid and active androgen. This compound acts as a potent agonist of the androgen receptor (AR), exhibiting a Ki value of 20.4 nM and an EC50 of 1.35 nM for human AR. It plays a significant role in the regulation of gene expression, protein synthesis, and cell proliferation in androgen-dependent prostate cancer research. 11-Ketodihydrotestosterone-d3 is valuable for metabolic studies and tracer applications in hormonal and cancer research. -
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. -
SARM/AR Ligand
TFM-4AS-1 is a selective androgen receptor modulator (SARM) that acts as a potent androgen receptor (AR) ligand with an IC50 of 38 nM. This compound functions as a gene-selective agonist, making it valuable for studies focused on muscle wasting and bone density regulation. Its specificity provides a useful tool for exploring androgen receptor signaling pathways in various biological contexts. -
Stable Isotope
Linuron-d6 is a deuterated form of the phenylurea herbicide Linuron, which functions as a photosystem II inhibitor. This compound is primarily utilized in agricultural settings to effectively manage the growth of grass and weeds in crops and orchards. In addition to its herbicidal properties, Linuron exhibits activity as a competitive antagonist of the androgen receptor, with a Ki of 100 μM, and has been shown to induce reproductive toxicity in animal models, acting as an endocrine disruptor in research contexts. -
Androgen Receptor Antagonist
6-Amino-5-bromoquinoxaline is an androgen receptor antagonist that functions through selective inhibition of androgen receptor activity. This compound is noted for its potential applications in research related to hormone signaling pathways and the investigation of androgen-related disorders. Its utility may extend to studies involving prostate cancer and other androgen-sensitive conditions. -
Anti-androgen
SK33 is a trifluoromethylated enobosarm analog that functions as a potent and tissue-selective anti-androgen. It effectively reduces androgen receptor (AR) transcriptional activity, making it a valuable tool for studying androgen-related signaling pathways. This compound is particularly relevant for research in prostate cancer and other androgen-dependent disorders. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 9 is a selective antagonist of the androgen receptor, inhibiting its activity in cellular contexts. This compound is primarily utilized in research focusing on androgen signaling pathways, offering insights into prostate cancer and other androgen-related diseases. Additionally, it contributes to studies aimed at understanding the role of androgens in various physiological processes and conditions. -
Androgen Receptor Modulator
LGD-2226 is a selective androgen receptor modulator (SARM) with high potency, exhibiting an EC50 of 0.2 nM and a Ki of 1.5 nM for the human androgen receptor. It demonstrates tissue selectivity, showing diminished effects on prostate tissue relative to muscle in in vivo models. Researchers can utilize LGD-2226 in studies related to muscle wasting, osteoporosis, and sexual dysfunction to explore therapeutic strategies targeting androgen receptors. -
Androgen Receptor Modulator
GLPG0492 (R enantiomer) is a selective androgen receptor modulator that exhibits significant affinity for the androgen receptor. This compound demonstrates potential for promoting anabolic effects in muscle and bone, making it a valuable tool for research in androgen signaling and related therapeutic applications. Its specificity may provide insights into the mechanisms of androgen action and the development of novel treatments for conditions related to androgen deficiency. -
Antiandrogen/Antitumor Agent
Gridegalutamide is an antiandrogen that functions by inhibiting androgen receptor signaling, contributing to its antitumor effects. This compound is primarily utilized in research focused on prostate cancer and other androgen-sensitive malignancies, making it valuable for investigating therapeutic strategies targeting the androgen receptor pathway. -
Anabolic Androgenic Steroid Metabolite
19-Noretiocholanolone is a metabolite of the anabolic androgenic steroid Nandrolone, functioning primarily as an androgen receptor agonist. This compound exhibits significant anabolic activity, promoting muscle growth and strength enhancement. It is commonly used in research applications focused on the effects of anabolic steroids and their metabolic byproducts on physiological processes. -
Androgen Receptor Antagonist
(Rac)-PF-998425 is a potent, selective nonsteroidal antagonist of the androgen receptor (AR). It exhibits IC50 values of 26 nM in AR binding assays and 90 nM in cellular assays, demonstrating significant efficacy in inhibiting AR activity. This compound is particularly relevant for research applications in androgenetic alopecia and related androgen-mediated conditions. -
AR Antagonist
Apalutamide-d4 is a deuterium-labeled derivative of Apalutamide, functioning as a potent competitive antagonist of the androgen receptor (AR). It demonstrates a binding affinity with an IC50 of 16 nM, making it valuable for studies involving androgen signaling pathways. This reagent is primarily used in research applications focused on prostate cancer and androgen-related disorders, facilitating the investigation of AR-mediated mechanisms and potential therapeutic strategies. -
Stable Isotope
Apalutamide-d3 is a deuterium-labeled derivative of Apalutamide, a highly selective androgen receptor (AR) antagonist with an IC50 of 16 nM. This stable isotope is designed for applications in pharmacokinetic studies and metabolic profiling, facilitating the investigation of AR signaling pathways and the pharmacodynamics of AR-targeted therapies in various models. Its use in research enables precise tracking and quantification in biological systems, enhancing our understanding of androgen receptor modulation in cancer therapies. -
AR Antagonist
AR Antagonist 3 is a selective androgen receptor (AR) antagonist with a measured IC50 of 0.47 µM, demonstrating strong potency in blocking AR activity. It effectively reduces FRET signal in a dose-dependent manner, with an IC50 of 18.05 μM. In preclinical studies, AR Antagonist 3 has shown significant inhibition of tumor growth upon intratumoral administration, making it a valuable tool for research in androgen receptor-related cancer therapies. -
AR Antagonist
Galloylalbiflorin is an androgen receptor (AR) antagonist with an IC50 of 53.3 μM, isolated from the roots of Paeonia lactiflora. This compound demonstrates notable anti-androgenic activity, making it valuable for research related to androgen signaling pathways and its implications in diseases such as prostate cancer. It serves as a useful tool for investigating AR-related biological processes and therapeutic applications in hormone-related disorders. -
Stable Isotope
Ostarine-d4 is a deuterated form of Ostarine, primarily functioning as a stable isotope. This labeled compound is utilized in pharmacokinetic studies, enabling accurate tracking of Ostarine metabolism and distribution within biological systems. Its application is critical for research on selective androgen receptor modulators and their effects on muscle and bone metabolism. -
Androgen Receptor
Trestolone is a synthetic anabolic-androgenic steroid that primarily targets the androgen receptor. It exhibits significant anabolic activity, promoting muscle growth and development while also enhancing physical performance. Trestolone is commonly utilized in research applications focused on muscle physiology, testosterone effects, and various anabolic processes. -
Androgen Receptor Modulator
GTx-027 is a selective androgen receptor modulator (SARM) that exhibits potent transactivation of the androgen receptor (AR) with an EC50 of 1.8 nM. This non-steroidal compound selectively promotes anabolic processes, leading to increased muscle weight while sparing androgenic effects on secondary sexual organs. GTx-027 is primarily utilized in research related to breast cancer and stress urinary incontinence (SUI). -
Androgen Receptor Antagonist
PF-998425 is a selective nonsteroidal androgen receptor (AR) antagonist, demonstrating significant potency with an IC50 of 37 nM in AR binding assays and 43 nM in cellular assays. This compound exhibits minimal activity towards common receptors and enzymes, such as the progesterone receptor. PF-998425 is relevant for research applications involving sebum control and the investigation of androgenetic alopecia. -
NSAA
RD162 is a diarylthiohydantoin and a non-steroidal antiandrogen (NSAA) that exhibits selective binding to the androgen receptor (AR). This compound is notable for its ability to induce tumor regression in mouse models of castration-resistant human prostate cancer, highlighting its potential as a therapeutic agent in prostate cancer research. RD162 serves as a valuable tool for studying AR-targeted therapies and the mechanisms underlying castration resistance in prostate malignancies. -
Anti-Androgenic Agent
N-Nitrosodicyclohexylamine (NDCHA) is an N-nitroso compound known for its anti-androgenic properties. It acts as a competitive antagonist of the androgen receptor (AR), effectively inhibiting the binding of 5α-dihydrotestosterone. Additionally, NDCHA reduces the protein levels of AR, making it a valuable tool for investigating androgen signaling pathways and potential therapeutic targets in androgen-related disorders.
