Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
PROTAC Linkers
Boc-Pip-alkyne-Ph-COOH is a PROTAC linker designed for use in the synthesis of targeted protein degraders. It facilitates the development of PROTACs, including ARD-266, which effectively promotes degradation of the androgen receptor in AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, exhibiting DC50 values of 0.2-1 nM. This compound features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it essential for click chemistry applications in chemical biology research. -
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. -
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.
