Orphan Nuclear Receptor

BI-6015 is an antagonist of hepatocyte nuclear factor 4α (HNF4α), effectively inhibiting the expression of HNF4α target genes. By repressing insulin promoter activity, it serves as a valuable tool for studying the regulatory mechanisms governed by HNF4α. BI-6015 is applicable in research focused on cancer and diabetes, providing insights into metabolic and oncogenic pathways.

NR2F2-IN-1 free base is a selective inhibitor targeting the orphan nuclear receptor COUP-TFII (NR2F2). This compound effectively suppresses COUP-TFII-driven expression of the NGFIA reporter by binding to the ligand-binding domain of COUP-TFII, interfering with its interactions with transcriptional regulators such as FOXA1. NR2F2-IN-1 is suitable for research applications focused on elucidating the role of COUP-TFII in gene regulation and its implications in various biological processes.

NR2F1 agonist 1 is a selective agonist of the nuclear receptor NR2F1, designed to activate dormancy programs in malignant cells. This compound up-regulates NR2F1 and its downstream target genes, leading to neural crest-like differentiation and growth suppression in head and neck squamous cell carcinoma (HNSCC). Additionally, NR2F1 agonist 1 has demonstrated the ability to inhibit tumor growth in preclinical mouse models, making it a valuable tool for research into cancer dormancy and therapeutic strategies.

RJW103 is an acid-stable agonist of SF-1 (NR5A1) and LRH-1, demonstrating pEC50 values of 6.5 and 5.9, respectively. This compound effectively activates SF-1- and LRH-1-mediated transcription of endogenous target genes. Research applications include investigations in cancer biology, endocrinology, and metabolic diseases, particularly in the context of adrenocortical tumors.

GSK8470 is a potent LRH-1 and SF-1 agonist, with EC50 values of 0.43 μM and 0.054 μM, respectively. This compound enhances the expression of small heterodimer chaperones (SHPs), a critical target gene regulated by LRH-1, in hepatocytes. GSK8470 is valuable for research applications involving the modulation of nuclear hormone receptor signaling pathways and related metabolic processes.

SID 7969543 is a selective inhibitor of steroidogenic factor 1 (SF-1, NR5A1) with an IC50 value of 760 nM. This compound effectively inhibits SF-1-mediated luciferase expression with an impressive IC50 of 30 nM. SF-1 plays a crucial role as a transcription factor within the nuclear receptor superfamily, making SID 7969543 valuable for research involving steroidogenesis and related pathways.

7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is an LRH-1 antagonist, exhibiting an IC50 of 3.1 μM. This compound is valuable for studying the role of LRH-1 in various biological processes, including lipid metabolism and endocrine signaling. Its pharmacological properties make it a suitable tool for investigating potential therapeutic targets in metabolic diseases and hormone-related conditions.

TLX Agonist 1 acts as a modulator for the orphan nuclear receptor TLX (NR2E1), exhibiting an EC50 of 1 μM and a Kd of 650 nM. This compound enhances the transcriptional repressive activity of TLX, making it a valuable tool for research into gene regulation and neurogenesis. Its unique mechanism supports investigations into the role of TLX in various biological processes and potential therapeutic applications.

NR2E3 Agonist 1 is a small molecule specifically designed to activate the photoreceptor-specific nuclear receptor NR2E3, demonstrating an EC50 value of less than 200 nM. This compound plays a critical role in research focused on retinal diseases, particularly retinitis pigmentosa, by modulating NR2E3 activity to explore its effects on photoreceptor development and function.

SID7970631 is a selective inhibitor of Steroidogenic Factor-1 (SF-1), exhibiting potent activity with an IC50 of 255 nM. This isoquinolinone analog is primarily utilized in cancer research, facilitating the investigation of SF-1's role in tumorigenesis and potential therapeutic strategies. Its specificity and efficacy make SID7970631 a valuable tool for studying pathways associated with steroidogenesis and related malignancies.

LysoPalloT-NH-amide-C3-ph-m-O-C11 is a potent agonist of GPR174, exhibiting an EC50 of 34 nM. This compound is utilized in research to elucidate the role of GPR174 in various biological processes, including immune modulation and potential therapeutic applications in autoimmune diseases. It serves as a valuable tool for studying GPR174 signaling pathways and their impact on cellular responses.

NR2F2-IN-1 is a potent and selective inhibitor of the orphan nuclear receptor COUP-TFII (NR2F2). It significantly inhibits COUP-TFII-driven expression of the NGFIA reporter by directly binding to the ligand-binding domain of COUP-TFII, thereby disrupting its interactions with transcriptional regulators such as FOXA1. This inhibition effectively suppresses COUP-TFII activity on the regulation of target genes, making NR2F2-IN-1 a valuable tool for studying the role of COUP-TFII in various biological processes and diseases.

LRH-1 Inhibitor-3 is a small molecule that specifically inhibits the transcriptional activity of the orphan nuclear receptor LRH-1. By downregulating the expression of genes linked to cell growth and proliferation, this compound has demonstrated potential in reducing proliferation in human pancreatic, colon, and breast adenocarcinoma cell lines. LRH-1 Inhibitor-3 serves as a valuable molecular probe for exploring the role of LRH-1 in various cancer types and may provide insights into targeted cancer therapies.

Photoregulin1 targets orphan nuclear receptors to modulate gene expression in retinal cells. This compound has demonstrated the potential to slow photoreceptor degeneration in mouse models of retinitis pigmentosa, making it valuable for research into retinal diseases and regenerative therapies. Its mechanism of action offers insights into the underlying biology of photoreceptor cell survival and degeneration.

NR2F6 modulator-2 is a selective modulator of the orphan nuclear receptor NR2F6, which plays a crucial role in gene regulation and cellular processes. This compound demonstrates the ability to inhibit the recruitment of the bio-NSD1 peptide, with an IC50 value of 2.0 equivalents of NR2F6. NR2F6 modulator-2 is intended for research applications in the fields of cancer biology and immunology, contributing to the understanding of NR2F6's role in various pathophysiological conditions.

TLX Agonist 3 is a potent and selective agonist of the tailless homolog (TLX, NR2E1) that exhibits an EC50 of 0.25 μM and a Kd of 1.6 μM. This compound demonstrates high specificity for TLX over related nuclear receptors and promotes TLX oligomerization with an EC50 of 5.0 μM. TLX Agonist 3 is utilized in research focused on neurodegenerative diseases, providing insights into the role of TLX in neuronal function and disease mechanisms.

LRH-1 antagonist-1 is a selective antagonist of Liver Receptor Homolog-1 (LRH-1) with a Kd of 1.8 μM. This compound effectively inhibits the transcriptional activity of LRH-1, leading to reduced expression of G0S2 and subsequent inhibition of proliferation in LRH-1-positive cancer cells. It is suitable for research applications in pancreatic, colon, and breast cancer studies, where targeting LRH-1 may provide valuable insights into tumor growth and progression.

SF-1 antagonist-1 is a potent inhibitor of steroidogenic factor 1 (SF-1), demonstrating an EC50 value of less than 200 nM in modulating SF-1 transcriptional activity. This compound effectively inhibits the proliferation of rat Leydig tumor cells, making it a valuable tool in cancer research. SF-1 antagonist-1 provides insights into the role of SF-1 in tumor biology and offers potential for therapeutic exploration in malignancies associated with steroidogenesis.

GPR27 Agonist-1 is a selective agonist of the GPR27 receptor, exhibiting a pEC50 of 6.34. This compound is valuable for investigating the role of GPR27 in various biological processes and its potential implications in metabolic disorders. Its specific activation of GPR27 makes it an essential tool for research in receptor biology and pharmacology.

LRH-1 antagonist-1 dihydrochloride is a selective antagonist of Liver Receptor Homolog-1 (LRH-1), exhibiting a Kd of 1.8 μM. This compound effectively inhibits the transcriptional activity of LRH-1, leading to a decrease in the expression of G0S2. Furthermore, it demonstrates the ability to suppress the proliferation of LRH-1-positive cancer cells, making it a valuable tool for research in pancreatic, colon, and breast cancer.

Iso-RJW100 is a dual agonist of liver receptor homologue-1 (LRH-1) and steroidogenic factor-1 (SF-1), demonstrating pEC50 values of 6.4 and 7.2, respectively. This compound significantly modulates the activity of LRH-1 and SF-1, key regulators in steroidogenesis and metabolic processes. Iso-RJW100 is valuable for research in endocrine signaling, metabolic regulation, and associated disease models.

Benfluorex is an activator of hepatic nuclear factor 4 alpha (HNF4α), a key transcription factor involved in regulating glucose and lipid metabolism. Its biological activity has been linked to potential applications in the study of metabolic disorders, particularly diabetes and dyslipidemia. Researchers may utilize Benfluorex to investigate its effects on gene expression and metabolic pathways associated with HNF4α activation.