Orphan Nuclear Receptor Antagonist

BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.

NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model.

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

PSB-22269 is a GPR17 antagonist with a K_i value of 8.91 nM. PSB-22269 further demonstrated significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies revealed that the binding site of PSB-22269 contains positively charged arginine residues and a hydrophobic pocket. PSB-22269 provides a strategy to promote remyelination and holds promise for research in the field of multiple sclerosis.

LRH-1 antagonist-1 (Compound 3d2) is a LRH-1 antagonist with a K_d of 1.8 μM. LRH-1 antagonist-1 inhibits the transcriptional activity of LRH-1 and reduces the expression of G0S2. LRH-1 antagonist-1 inhibits the proliferation of LRH-1-positive cancer cells. LRH-1 antagonist-1 can be used for research on pancreatic cancer, colon cancer and breast cancer.

SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC₅₀ value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer.

LRH-1 antagonist-1 (Compound 3d2) dihydrochloride is a LRH-1 antagonist with a K_d of 1.8 μM. LRH-1 antagonist-1 dihydrochloride inhibits the transcriptional activity of LRH-1 and reduces the expression of G0S2. LRH-1 antagonist-1 dihydrochloride inhibits the proliferation of LRH-1-positive cancer cells. LRH-1 antagonist-1 dihydrochloride can be used for research on pancreatic cancer, colon cancer and breast cancer.

BI-6015 (Standard) is the analytical standard of BI-6015 (HY-108469). This product is intended for research and analytical applications. BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.