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.

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.

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

ML179 is a potent and selective inverse agonist of liver receptor homolog-1 (LRH1, NR5A2) with IC50 of 320 nM.

(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.

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.

TLX agonist 2 (compound 31) is a TLX agonist with an EC50 of 0.1 μM and a Kd of 0.16 μM. This compound enhances transcriptional activity by binding to TLX, thereby boosting the expression of TLX target genes. TLX agonist 2 is utilized in research on neurodegenerative diseases.

GPR27 agonist-1 (compound I) is a selective agonist for GPR27 with a pEC50 value of 6.34.

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.

PSB-22269 is identified as a GPR17 antagonist with a Ki value of 8.91 nM. It exhibits significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies indicate that the binding site of PSB-22269 includes positively charged arginine residues and a hydrophobic pocket. PSB-22269 promotes myelin regeneration strategies, offering potential for multiple sclerosis research.

LysoPalloT-NH-amide-C3-ph-m-O-C11 is an agonist of the GPR174 receptor with an EC50 value of 34 nM.

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

20-SOLA is the first water-soluble 20-HETE antagonist with oral bioavailability. It significantly improves blood pressure changes and kidney damage associated with the streptozotocin (STZ) diabetic mouse model. Additionally, 20-SOLA acts as a GPR75 receptor blocker. This compound is useful in research related to cardiovascular pathology.

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.

BAN ORL 24 is a highly potent nociceptin/orphan FQ (N/OFQ) receptor (NOP) antagonist that can be used to study neurological diseases.

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

Nobiletin (Hexamethoxyflavone) is a natural polymethoxylated flavone isolated from citrus peels with anti-inflammatory and anti-tumor activities. Nobiletin is practically insoluble (in water) and an extremely weak acidic compound (based on its pKa).

BPK-29 hydrochloride is a specific ligand that disrupts atypical orphan nuclear receptor NR0B1-protein interactions by covalently modifying C274, impairing the anchorage-independent growth of [KEAP1-mutant cancer cells].

TLX agonist 1 is an orphan nuclear receptor tailless (TLX, NR2E1) modulator