Catalog No.
Product Name
Application
Product Information
Citations
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Endogenous Metabolite
Rofleponide epimer is an endogenous metabolite that targets glucocorticoid receptors, exhibiting significant anti-inflammatory activity. It demonstrates high selectivity for lung tissues and effectively binds to the rat thymic glucocorticoid receptor, reinforcing its pharmacological efficacy. Additionally, Rofleponide epimer has a biotransformation rate that is ten times greater than that of similar compounds, highlighting its potential for therapeutic applications in managing inflammatory diseases affecting mucosal surfaces. -
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. -
Renin Inhibitor
CP-69799 is a potent renin inhibitor that functions as a transition-state analogue, specifically targeting hog renin with an IC50 value of 6 nM and human plasma renin with an IC50 of 300 nM. This inhibitor engages the active site of endothiapepsin, inducing domain rotation and impacting thermal dynamics. CP-69799's unique design, featuring a polar lysine residue at the P2' position, allows for effective binding and has implications for hypertension research. Its mechanistic insights make it a valuable reagent for studies focused on modulating renin activity and understanding cardiovascular functions. -
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. -
AR Ligand
AR Ligand-44 is a potent androgen receptor (AR) ligand that serves as a crucial component in the development of proteolysis-targeting chimeras (PROTACs). Its high affinity for the androgen receptor makes it a valuable tool for investigating AR-mediated signaling pathways. This compound is particularly relevant in research focused on prostate cancer and hormone-related disorders, facilitating the exploration of targeted therapy strategies. -
Androgen Receptor Ligand
AR ligand 42 is a potent androgen receptor ligand that functions by selectively binding to the androgen receptor. It is utilized in the synthesis of the androgen receptor PROTAC degrader ITRI-90, facilitating targeted degradation of the androgen receptor in research applications. This compound is instrumental for studies exploring androgen signaling pathways and potential therapeutic strategies in prostate cancer and other androgen-related conditions. -
Androgen Receptor Antagonist
AR ligand-39 is an androgen receptor (AR) antagonist that serves as a critical component in PROTAC technology. It functions by binding specifically to the AR, facilitating the targeted degradation of the receptor. This compound is primarily utilized in research applications focused on modulating AR-mediated signaling pathways and studying the effects of androgen signaling in various biological contexts. -
AR Ligand
AR ligand-4 is a potent ligand for the androgen receptor (AR), serving as a crucial building block for the synthesis of PROTACs, including ARD-1676. Its role in targeted protein degradation makes it a valuable tool for investigating AR biology and therapeutic strategies in androgen-dependent diseases. Researchers can use AR ligand-4 to explore the implications of AR modulation in various biological contexts. -
Target Protein Ligand
AR ligand-32 is a target protein ligand that plays a crucial role in the synthesis of PROTAC AR Degrader-7. This compound effectively engages the androgen receptor, facilitating its degradation through the ubiquitin-proteasome pathway. It is primarily utilized in research focused on targeted protein degradation and androgen signaling pathways, providing valuable insights into therapeutic strategies for diseases linked to androgen receptor activity. -
Target Protein Ligand
AR ligand-29 is a targeted protein ligand designed for use with PROTAC VinclozolinM2-2204. This compound plays a critical role in cancer research by facilitating the selective degradation of androgen receptors, making it a valuable tool for studies focused on androgen receptor-mediated pathways and their implications in cancer biology. Its specificity enhances the understanding of therapeutic strategies aimed at addressing androgen-dependent malignancies. -
Molecular Glue Stabilizer
GR-14-3-3 stabilizer-1 is a molecular glue stabilizer that effectively enhances the stability of glucocorticoid receptors (GR) by preventing their interaction with 14-3-3 proteins. This compound is instrumental in research involving the modulation of GR signaling pathways, providing a valuable tool for studying glucocorticoid-related cellular responses and their implications in various disease states. Its applications extend to the development of novel therapeutic strategies targeting GR dynamics in cellular contexts. -
AR Degrader
AR Degrader-2 is a molecular glue that targets and promotes the degradation of the androgen receptor (AR) with a DC50 of 0.3-0.5 μM in VCaP cells. This compound is essential for research applications aimed at investigating AR signaling pathways and developing therapeutic strategies for androgen receptor-associated diseases, particularly in prostate cancer. Its potent activity facilitates the study of AR dynamics and may contribute to the advancement of targeted degradation approaches in drug discovery. -
RORγt Inhibitor
RORγt inverse agonist 36 is a selective inverse agonist targeting the retinoid-related orphan receptor gamma t (RORγt). This compound modulates RORγt activity, leading to inhibition of Th17 cell differentiation and cytokine production. It is primarily utilized in research focused on inflammation and immunology, offering valuable insights into therapeutic approaches for autoimmune diseases. -
RORγt Inverse Agonist
RORγt Inverse Agonist 30 is a selective inverse agonist of the RORγt nuclear receptor, exhibiting an IC50 of 46 nM. This compound effectively modulates RORγt activity, making it a valuable tool in the study of autoimmune disorders. Its ability to inhibit RORγt function positions it as a promising candidate for research into therapeutic strategies for conditions such as multiple sclerosis and other inflammatory diseases. -
RORC modulator
RORC modulator-1 is a selective modulator of the retinoic acid receptor-related orphan receptor C (RORC). It demonstrates the ability to regulate RORC activity, impacting the expression of genes involved in immune response and inflammation. This compound is valuable for research applications focused on T helper cell differentiation, autoimmune diseases, and the study of related signaling pathways. -
ROR-γ Inhibitor
CID 7309015 is a selective inhibitor of retinoic acid-related orphan receptor gamma (ROR-γ). This compound demonstrates significant potential in modulating inflammatory pathways, particularly in the context of NF-κB signaling and inflammatory arthritis research. CID 7309015 serves as a valuable tool for investigating the roles of ROR-γ in immune response and inflammatory diseases. -
RORγt Inhibitor
RORγt inhibitor 3 is a potent and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), which plays a crucial role in Th17 cell differentiation. This compound demonstrates high binding affinity and effectively modulates immune responses, making it particularly relevant for research in autoimmune disorders. Its efficacy has been validated in mouse models of experimental autoimmune encephalomyelitis (EAE) and collagen-induced arthritis (CIA), highlighting its potential for therapeutic applications in inflammatory diseases. -
RORγ Agonist
Cintirorgon sodium is a selective and orally bioavailable RORγ agonist that modulates gene expression in RORγ-expressing T lymphocytes. This compound enhances effector functions and reduces immunosuppressive mechanisms, contributing to decreased tumor growth and improved survival rates in various preclinical models. Cintirorgon sodium is a valuable tool for research applications focused on immunotherapy and cancer biology. -
AUTOTAC Control
YT 6-2 analog-1 is a p62/SQSTM1-targeting autophagy ligand designed for use in AUTOTAC control applications. This compound effectively facilitates the degradation of the androgen receptor (AR), leading to reduced nuclear AR levels and downregulation of AR target gene expression, including AR-v7. Additionally, YT 6-2 analog-1 demonstrates efficacy against common AR mutants found in prostate cancer, making it a valuable tool for research in hormone signaling and targeted therapy. -
AUTOTAC
ATC-324 is a bivalent androgen receptor (AR) degrader that utilizes the AUTOTAC (AUTOphagy-TArgeting Chimera) technology to promote targeted protein degradation. It facilitates the assembly of an AR/p62 complex, triggering autophagy-mediated lysosomal degradation of the AR, which results in reduced nuclear AR levels and diminished expression of AR and AR-v7 target genes. Additionally, ATC-324 effectively degrades various common AR mutants associated with prostate cancer. This compound consists of the target-binding ligand Enzalutamide and the p62 autophagy-targeting ligand YT 6-2 analog-1, interconnected by a PEG-based linker for enhanced cellular uptake. -
E3 Ligase Ligand-Linker Conjugates
E3 Ligase Ligand-linker Conjugate 197 is an E3 ubiquitin ligase ligand-linker conjugate designed for use in the synthesis of PROTACs. Its primary application is in the development of targeted protein degradation strategies. This compound enables the formation of heterobifunctional degraders, facilitating the selective degradation of proteins such as the androgen receptor, thereby aiding in studies of protein regulation and disease mechanisms. -
PROTAC Linker
Boc-piperazine-benzoic acid acts as a PROTAC linker, facilitating the design and synthesis of proteolysis-targeting chimeras (PROTACs). This compound can be utilized in the development of PROTACs that target specific proteins for degradation, including the androgen receptor (AR) degrader ARD-2128. Its implementation in research enables advanced studies in protein regulation and therapeutic applications in cancer treatment. -
Ligands for E3 Ligase
VHL Ligand 8 is a potent ligand for the von Hippel-Lindau (VHL) E3 ligase. It serves as a key precursor in the synthesis of ARD-266, a highly effective PROTAC degrader targeting the androgen receptor (AR). ARD-266 induces robust degradation of AR protein in various AR-positive prostate cancer cell lines, including LNCaP, VCaP, and 22Rv1, with demonstrated DC50 values ranging from 0.2 to 1 nM. This compound is useful in research focusing on targeted protein degradation therapies for prostate cancer. -
PROTAC Ligand
AR Antagonist 1 Hydrochloride is a potent androgen receptor (AR) antagonist that serves as a crucial component in the synthesis of PROTAC ARD-266. It effectively binds to E3 ligase ligands with weak affinities to the VHL protein, facilitating targeted protein degradation. This compound is valuable for research applications focused on AR modulation and targeted therapeutic strategies in prostate cancer and other androgen-related diseases. -
Intermediate
BWA-522 intermediate-1 serves as a crucial intermediate in the synthesis of PROTAC BWA-522 and functions as a ligand for cereblon E3 ubiquitin ligase. This compound plays a significant role in the development of orally active small molecule protein-targeting chimeras (PROTACs), which exhibit potent degradation activity on androgen receptor full-length (AR-FL) and variant 7 (AR-V7). Its application is essential in research focused on targeted protein degradation and therapeutic strategies for diseases driven by androgen signaling. -
PROTAC Ligand
AR Antagonist 1 is a potent androgen receptor (AR) antagonist that serves as a key PROTAC ligand. It demonstrates significant activity in disrupting AR signaling pathways, making it valuable for research into androgen-related diseases. Additionally, it has weak binding affinities to VHL protein, facilitating the synthesis of PROTAC ARD-266 for studying targeted protein degradation mechanisms in cancer and other therapeutic areas. -
Ligands for E3 Ligase
6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole is a selective ligand for E3 ligases, facilitating targeted protein degradation pathways. This compound plays a crucial role in the synthesis of the PROTAC Androgen Receptor Degrader-1, highlighting its importance in advancing research on androgen receptor-mediated signaling. Its use in drug discovery efforts underscores its potential in addressing diseases associated with dysfunctional protein regulation. -
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. -
ER Degrader
ER Degrader 10 is a selective orally active degrader and antagonist of the estrogen receptor (ER), demonstrating a DC50 of 0.43 nM and an IC50 of 0.56 nM. This compound effectively inhibits the proliferation of ER-positive cancer cells, with IC50 values ranging from 0 to 15 nM. While it shows minimal inhibitory activity against the hERG channel (IC50 > 40 μM), ER Degrader 10 is capable of crossing the blood-brain barrier, with a brain/plasma ratio of 3.05. Additionally, it has demonstrated significant antitumor efficacy in mouse models, making it a valuable tool for cancer research. -
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. -
testosterone 5α-reductase Inhibitor, 5α-dihydrotestosterone receptor Inhibitor
Kushenol Q is an inhibitor of testosterone 5α-reductase and the 5α-dihydrotestosterone receptor. This compound demonstrates significant biological activity in modulating androgen signaling pathways, making it useful in studies related to hormone-related disorders. Additionally, Kushenol Q exhibits antibacterial properties against Gram-positive bacteria, indicating its potential in antimicrobial research applications. -
5 alpha Reductase Inhibitor
12-O-Methylcarnosic acid is a potent inhibitor of 5 alpha reductase, exhibiting an IC50 value of 61.7 μM. Isolated from the acetone extract of Salvia microphylla, this diterpene demonstrates significant anti-proliferative effects in LNCaP prostate cancer cells. In addition to its role in cancer research, 12-O-Methylcarnosic acid also possesses antioxidant and antimicrobial properties, making it a valuable reagent for various biological studies. -
5α-Reductase Inhibitor
Lapisteride is a potent 5α-reductase inhibitor, demonstrating efficacy in the modulation of androgen metabolism. This compound effectively inhibits 5α-reductase activity within hair follicles, making it a valuable tool for investigating prostatic hyperplasia and androgenic alopecia. Its applications extend to research aimed at understanding androgen-related disorders and developing targeted therapies. -
5-Alpha Reductase Inhibitor
CGP-53153 is a steroidal inhibitor of 5-alpha reductase, exhibiting IC50 values of 36 nM in rat prostatic tissue and 262 nM in human prostatic tissue. This compound is primarily utilized in research to investigate the inhibition of 5-alpha reductase, which plays a crucial role in androgen metabolism. Its biological activity makes it a valuable tool for studying conditions related to androgen levels, such as benign prostatic hyperplasia and prostate cancer. -
5α-Reductase Inhibitor
Izonsteride is a potent inhibitor of 5α-reductase, demonstrating IC50 values of 11.6 nM for type I and 7.37 nM for type II isoforms. By hindering the enzyme responsible for converting testosterone to dihydrotestosterone, Izonsteride effectively reduces androgenic activity. This compound has been shown to significantly inhibit the growth of LNCaP tumors in thymic mice, indicating its potential as a therapeutic agent in prostate cancer research, with minimal host toxicity observed. -
5 alpha Reductase Inhibitor
MK 386 is a selective inhibitor of 5-alpha reductase type I, which plays a critical role in the metabolism of testosterone into dihydrotestosterone (DHT). By inhibiting this enzyme, MK 386 is utilized in research focused on prostate cancer treatment and hormone-related disorders. Its specificity for 5-alpha reductase I makes it a valuable tool for studying the effects of DHT modulation on cellular and molecular pathways associated with prostate cancer progression. -
Steroid 5α-Reductase Inhibitor
8,11-Eicosadiynoic acid is a steroid 5α-reductase inhibitor that exhibits potent biological activity in the modulation of androgen metabolism. This unsaturated fatty acid is primarily utilized in research related to acne and other androgen-mediated conditions. Its ability to inhibit 5α-reductase makes it a valuable tool for investigating pathways involved in sebaceous gland function and acne pathology. -
5α-reductase Inhibitor
Bexlosteride is a benzoquinolinone that acts as a specific inhibitor of human type I 5α-reductase. It exhibits significant metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. This compound is valuable for research focused on prostate cancer, providing insights into the modulation of androgen pathways and potential therapeutic interventions. -
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. -
5alpha-reductase 1 Inhibitor
AS-601811 is a potent inhibitor of 5α-reductase 1, demonstrating an IC50 of 20 nM. This compound is valuable for investigating conditions such as alopecia and hirsutism by modulating androgen metabolism. Its specificity for 5α-reductase 1 makes it an essential tool for research into related endocrine and dermatological disorders. -
5 alpha Reductase Inhibitor
ONO-3805 is a non-steroidal 5α-reductase inhibitor that selectively targets the enzyme responsible for converting testosterone to dihydrotestosterone. It exhibits potential therapeutic benefits in the management of benign prostatic hyperplasia and may contribute to the reduction of associated symptoms. This compound is primarily utilized in endocrine-related research and studies focusing on androgen modulation in prostatic disorders. -
Human Type I 5α-Reductase Inhibitor
LY191704 is a selective, nonsteroidal inhibitor of human type I 5α-reductase, exhibiting noncompetitive inhibition. This compound, a racemic mixture of LY300502 and LY300503, demonstrates potent activity in modulating the enzymatic conversion of testosterone to dihydrotestosterone (DHT). LY191704 is valuable for investigating human endocrine disorders linked to elevated DHT levels, offering insights into potential therapeutic approaches for conditions such as androgenetic alopecia and benign prostatic hyperplasia. -
5 alpha Reductase Inhibitor
L-751788 is a selective inhibitor of type I 5α-reductase, a key enzyme involved in steroid metabolism. This compound demonstrates significant potential in reducing dihydrotestosterone levels without adversely affecting fetal external genitalia, as evidenced by studies conducted in pregnant rhesus monkeys. L-751788 is valuable for research applications investigating disorders of androgen metabolism and related therapeutic interventions.
