orphan receptor

RJW100 is a compound that acts as a potent agonist of liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1), exhibiting pEC50 values of 6.6 and 7.5, respectively. Additionally, RJW100 induces robust activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.

(Iso)-RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC 50 s of 6.4 and 7.2, respectively.

LRH-1 Inhibitor-3 is an antagonist that inhibits LRH-1 transcriptional activity, reducing the expression of target genes associated with cell growth and proliferation, such as SHP (small heterodimer partner), cyclin E1 (CCNE1), and G0S2, and inhibiting the proliferation of human pancreatic, colon, and breast adenocarcinoma cells.

ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.

CID 1375606 is a surrogate agonist of the orphan G protein-coupled receptor [GPR27], characterized by a high level of conservation among vertebrates and predominant expression in the central nervous system.

'(Des-Bromo)-Neuropeptide B (1-23) (human)' is an agonist for orphan G-protein-coupled receptors, exhibiting a K i of 1.2 nM for GPR7 (NPBW1) and 341 nM for GPR8 (NPBW2) respectively [1].

7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is an LRH-1 antagonist with an IC50 of 3.1 μM.

N-(3-Chloro-4-morpholinophenyl)-N'-hydroxyformimidamide (TS-011) is a selective 20-Hydroxyeicosatetraenoic acid synthesis inhibitor.

Anticanceragent 258 is an imidazo[1,2-B][1,2,4]triazole derivative that modulates nuclear receptor activity. It exhibits an EC50 of 63 nM for Nurr in N2A cells and an IC50 of 0.1 pM for Nur77 in HEK293 cells. Anticanceragent 258 is applicable in studies related to cancer, metabolic disorders, and neurological diseases.

SJPYT-310 is a selective PXR antagonist, exhibiting no noticeable cytotoxicity.

NR2F6 modulator-2 (Compound I) is an effective NR2F6 modulator that inhibits the recruitment of endogenous NSD1 peptides, with an IC50 equivalent to 2 equivalents of NR2F6. It is applicable in cancer and immunology research.

DLPC is an LRH-1 agonist ligand. DLPC is a phospholipid for biological study[1][2].

BI 6015 is an antagonist of HNF4α. HNF4α is a nuclear receptor that regulates gene expression in the intestine cells, liver cells, and pancreas-β cells.

SID 7969543 is a selective SF-1 inhibitor with potential anticancer activity, inhibits SF-1-triggered luciferase expression and can be used for cancer research.

BMH-9 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

Ethoxyquin dimer is an antioxidant and metabolite of ethoxyquin .1 It prevents oxidation of polyunsaturated fatty acids in fish meal and fish oil. Dietary administration of ethoxyquin dimer (0.1, 0.3, and 0.5% w/w) induces microvesicular steatosis and hepatocyte necrosis, as well as increases liver levels of oxidized glutathione and total lipids in mice.2

SS-RJW100 is an enantiomer of RJW100, known as a racemic agonist that targets two nuclear receptors: liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). In vitro experiments reveal that SS-RJW100 promotes the recruitment of coregulator protein fragments and enhances the interaction with the transcriptional intermediary factor 2 (Tif2) coactivator specifically for LRH-1. Additionally, SS-RJW100 disrupts the allosteric activation networks of LRH-1, displaying suboptimal thermal stability [1] [2].

SID7970631 is an isoquinolinone analog and a potent, selective submicromolar SF-1 (Steroidogenic Factor-1, NR5A1) inhibitor/inverse agonist with an IC50 of 255 nM. It inhibits SF-1-mediated transcriptional activity and exhibits significant cytotoxic effects on SF-1-dependent cancer cell lines. SID7970631 is widely utilized in research exploring therapeutic mechanisms for cancers such as adrenocortical carcinoma.

LRH-1 modulator-1 is a potent modulator/agonist of LRH-1 (liver receptor homolog-1). LRH-1 modulator-1 induces the anti-inflammatory cytokine IL-10 and exhibits inhibition of the inflammatory cytokines IL-1b and TNFa. LRH-1 modulator-1 has anti-inflammatory activity in intestinal-like organs.

CIA-1 inhibits the nuclear receptor COUP-TFII, with IC50s ranging from 1.2 μM to 7.6 μM in prostate cancer cell lines.CIA-1 inhibits the growth of a variety of prostate cancer cell lines in vitro and inhibits COUP-TFII activity to regulate its target genes.CIA-1 in vivo exhibits tumor growth inhibitory effects in a mouse model of prostate cancer xenografts. inhibitory effect on tumor growth in a xenograft mouse model of prostate cancer in vivo.

CIA-1 (Free base) is a nuclear receptor COUP-TFII inhibitor with IC50 values ranging from 1.2 μM to 7.6 μM in prostate cancer cell lines. CIA-1 (Free base) inhibits tumor growth in a mouse model of prostate cancer xenografts.

NR2F1 agonist 1, a specific nuclear receptor NR2F1 activator, initiates dormancy programs in cancer cells by upregulating NR2F1 and its target genes controlling dormancy. This compound promotes neural crest-like features and suppresses growth in head and neck squamous cell carcinoma (HNSCC) through NR2F1 activation. Moreover, NR2F1 agonist 1 demonstrates tumor growth inhibition in a mouse primary tumor model.

RR-RJW100, an enantiomer of RJW100, functions as an agonist for both nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). Among its two synthesized enantiomers, RR-RJW100 and SS-RJW100, the former exhibits greater potency as an LRH-1 agonist. This compound plays a crucial role in regulating metabolic homeostasis and is utilized in researching diabetes, liver disease, and inflammatory bowel disease.

Prolactin-Releasing Peptide (12-31), rat, a fragment of PrRP, exhibits high affinity for GPR10 receptors and stimulates calcium mobilization in CHOK1 cells transfected with the PrRP receptor [1][2].