Androgen Receptors

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.

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.

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-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.

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.

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-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.

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.

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.

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.

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 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.

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.

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.

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.

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.

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.

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.

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.

BWA-522 intermediate-3 is a key intermediate in the synthesis of BWA-522, a small molecule protein-targeting chimera (PROTAC). This compound exhibits potent degradation of androgen receptor full-length (AR-FL) and its variant AR-V7. BWA-522 is primarily used in research applications focusing on hormone-resistant prostate cancer and mechanisms of selective protein degradation.

AH3960 is a selective agonist of the parathyroid hormone receptor 1 (PTHR1). It has demonstrated significant biological activity through its ability to activate PTHR1, contributing to studies in bone metabolism and calcium homeostasis. Additionally, AH3960 exhibits inhibitory effects on androgen receptors, specifically targeting both wild-type and the T877 mutant variant, with an IC50 value of 0.82 μM. This dual functionality makes AH3960 a valuable tool for research in endocrine signaling and related pathways.

Dehydroisoandrosterone 3-acetate is an androgen receptor agonist that serves as a key precursor to testosterone and estrogen. It plays a significant role in modulating vertebrate aggression and has been utilized in research to explore its effects on hormonal pathways and behavioral responses. This compound is particularly useful for studies investigating androgenic activity and its implications in various physiological and psychological processes.

11β,17β-Dihydroxy-5α-androstan-3-one is a C11-oxy C19 steroid that functions as a potent androgen. This compound exhibits significant biological activity in androgen receptor modulation, making it an important tool for exploring prostate cancer mechanisms. Researchers can utilize 11OHDHT to investigate its effects on androgen signaling pathways and develop potential therapeutic strategies in prostate cancer treatment.

p,p'-DDE (4,4'-DDE) serves as a potent androgen receptor antagonist, exhibiting an IC50 value of 5 μM and a Ki of 3.5 μM. This compound plays a significant role in the disruption of male reproductive system development and function. Furthermore, elevated levels of p,p'-DDE in serum have been associated with an increased risk of type 2 diabetes in women, highlighting its relevance in endocrine disruption studies and metabolic research.