Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
AR Antagonist
AR Antagonist 11 is a selective androgen receptor (AR) antagonist with an IC50 of 0.019 μM. It also demonstrates efficacy against the ARF877L/T878A mutant with an IC50 of 1.03 μM. AR Antagonist 11 effectively inhibits LNCaP cell proliferation and reduces PSA protein expression, with an IC50 of 0.54 μM. This compound is suitable for research into prostate cancer (PCa) biology and therapeutic strategies. -
Androgen Receptor Modulator
NEP28 is a selective androgen receptor modulator with a reported EC50 of 2.90 nM in 22RV1 cells. It enhances the activity of the Aβ-degrading enzyme neprilysin, demonstrating potential therapeutic benefits in muscle and brain tissue while mitigating adverse effects in the prostate as observed in rat models. This compound is suitable for research applications targeting osteoporosis, sarcopenia, and Alzheimer's disease. -
Estrogen Receptor/ERR Inhibitor
BHPI is a selective inhibitor of the estrogen receptor ERα, regulating downstream signaling pathways by activating phospholipase C gamma (PLCγ) and inducing the unfolded protein response (UPR). This compound exhibits significant antitumor activity, making it relevant for research in breast, endometrial, and ovarian cancers. Its ability to modulate estrogen-related signaling pathways positions BHPI as a valuable tool in the study of hormone-driven malignancies and therapeutic interventions. -
angiotensin-converting enzyme Inhibitor, renin Inhibitor
Lyciumin D functions as both an angiotensin-converting enzyme inhibitor and a renin inhibitor. This compound demonstrates significant potential in the modulation of the renin-angiotensin system, making it a valuable tool for research into hypertension and related cardiovascular conditions. Its multimodal mechanism can facilitate studies aimed at understanding blood pressure regulation and developing therapeutic strategies for hypertension management. -
Renin Inhibitor
Imarikiren hydrochloride is a potent renin inhibitor that disrupts the renin-angiotensin (RA) system. This compound demonstrates significant biological activity in the context of cardiovascular and renal diseases, making it valuable for research related to hypertension, heart failure, and diabetic nephropathy. Its mechanism of action provides insights into the modulation of blood pressure and kidney function, facilitating the exploration of therapeutic strategies for these conditions. -
Renin Inhibitor
SQ 33800 is a highly potent inhibitor of human renin, exhibiting an IC50 value of 0.35 nM. This compound is instrumental in the study of cardiovascular diseases, providing insights into the regulation of blood pressure and fluid balance. Researchers can utilize SQ 33800 to explore the implications of renin inhibition in various cardiovascular-related conditions. -
Direct Renin Inhibitor
SPH3127 is a highly potent and orally active direct renin inhibitor, demonstrating an IC50 of 0.4 nM against recombinant human renin and 0.45 nM for human plasma renin activity. This compound exhibits significant antihypertensive properties, making it a valuable tool for research focused on essential hypertension and related cardiovascular studies. Its mechanism of action as a direct renin inhibitor allows for detailed investigation into the renin-angiotensin-aldosterone system and its implications in hypertension management. -
Renin Inhibitor
Zankiren is a selective renin inhibitor that reduces the formation of angiotensin II, leading to its renal vasodilator effects. This compound is valuable for research focused on hypertension and cardiovascular diseases, as it specifically modulates renal hemodynamics without interfering with other vasodilatory pathways. Its ability to target renin makes Zankiren an important tool for studying the renin-angiotensin system and its implications in various pathological conditions. -
Renin Inhibitor
SQ 32970 is a tripeptidic inhibitor targeting renin, a key enzyme in the regulation of blood pressure. This compound exhibits potent inhibition of endothia protease activity, making it valuable for studies related to hypertension and cardiovascular research. SQ 32970 serves as a useful tool for investigating the physiological and pathological roles of the renin-angiotensin system. -
Renin Inhibitor
SQ 31844 is a novel renin inhibitor from the imidazolidinol class, specifically targeting the enzyme renin. This compound demonstrates potent in vitro inhibition of primate renin while showing no significant effects on renin from rat, pig, or dog. In vivo studies in sodium-deprived cynomolgus monkeys reveal a dose-dependent reduction in plasma renin activity (PRA) and arterial blood pressure, particularly at higher intravenous doses. Notably, oral administration of SQ 31844 at 50 μmol/kg leads to an 80% reduction in PRA. SQ 31844 serves as a valuable tool for exploring renin-related cardiovascular research and hypertension studies. -
Renin Inhibitor
Renin IN-2 is a selective inhibitor of human renin, exhibiting an IC50 value of 0.059 μM. This compound demonstrates oral efficacy and is applicable in the study of hypertension. Research utilizing Renin IN-2 can provide insights into renin's role in the regulation of blood pressure and related cardiovascular conditions. -
Renin Antagonist
EMD 55068 is a potent renin antagonist that effectively inhibits the enzyme's activity, thereby modulating the renin-angiotensin-aldosterone system. This compound has demonstrated efficacy in reducing taurocholate uptake, making it a valuable tool for studying renal function and hypertension-related research. EMD 55068 is of interest for investigations into cardiovascular diseases and the physiological implications of renin inhibition. -
Renin Inhibitor
Renin-IN-4 is a potent renin inhibitor that modulates the renin-angiotensin system. This compound is primarily studied for its implications in cardiovascular diseases, as it plays a crucial role in regulating blood pressure and fluid balance. Renin-IN-4 serves as a valuable tool for investigating the pathophysiology of hypertension and related cardiovascular disorders. -
Renin Inhibitor
Ciprokiren is a potent renin inhibitor, exhibiting IC50 values of 0.07 nM in buffer and 0.65 nM in plasma. This compound can be applied transdermally while maintaining hemodynamic effects without reducing plasma renin activity or plasma immunoreactive angiotensin II levels. Ciprokiren demonstrates significant antihypertensive efficacy, making it a valuable tool for hypertension research and the study of renin-angiotensin system modulation. -
Renin Inhibitor
CGP 29287 is a potent inhibitor of renin, the enzyme responsible for the conversion of angiotensinogen to angiotensin I in the renin-angiotensin system. By selectively inhibiting renin activity, CGP 29287 plays a critical role in studying the regulation of blood pressure and cardiovascular function. This compound is useful in research applications focusing on hypertension, heart failure, and related metabolic disorders. -
Renin Inhibitor
CP-85339 is a tetrapeptide compound that functions as a selective renin inhibitor, effectively modulating the renin-angiotensin-aldosterone system. It demonstrates significant biological activity by decreasing plasma renin levels, which can contribute to lowering blood pressure. This reagent is utilized in research applications related to cardiovascular diseases and hypertension studies, providing insights into the therapeutic potential of renin inhibition. -
Renin Inhibitor
SQ 30774 is a selective renin inhibitor that demonstrates potent in vitro activity in primate models. This compound effectively reduces plasma renin activity (PRA) and has been shown to lower arterial blood pressure in vivo. SQ 30774 is valuable for research applications focusing on hypertension and the renin-angiotensin system, providing insights into cardiovascular regulation and potential therapeutic interventions. -
Renin Inhibitor
Terlakiren is an orally active renin inhibitor that effectively modulates blood pressure regulation. With an IC50 value of 0.7 nM against human renin, Terlakiren demonstrates potent inhibition, making it a valuable tool for studying hypertension and related cardiovascular conditions. This compound is useful in research focused on renin-angiotensin system modulation and potential therapeutic interventions for hypertension. -
Renin Inhibitor
L-363564 is a potent renin inhibitor that plays a critical role in the modulation of the renin-angiotensin-aldosterone system (RAAS). This compound is primarily utilized in cardiovascular disease research, aiding in the investigation of hypertension and related conditions. Its ability to effectively inhibit renin activity makes it a valuable tool for exploring therapeutic strategies in this area. -
Renin Inhibitor
CGP 44099 is a selective renin inhibitor that plays a critical role in the modulation of the renin-angiotensin system. This compound is particularly valuable for research on ischemic injury and the mechanisms underlying reperfusion arrhythmias in rat heart models, providing insights into cardiovascular pathophysiology and potential therapeutic interventions.
