1. Signaling Pathways
  2. Vitamin D Related/Nuclear Receptor
  3. Orphan Nuclear Receptor
  4. Orphan Nuclear Receptor Inhibitor

Orphan Nuclear Receptor Inhibitor

Orphan Nuclear Receptor Inhibitors (8):

Cat. No. Product Name Effect Purity
  • HY-115613
    ML-180
    Inhibitor 99.96%
    ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 μM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 μM). ML-180 has the potential for LRH-1-dependent cancers.
  • HY-156190A
    NR2F2-IN-1 free base
    Inhibitor 99.34%
    NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation.
  • HY-176847
    HNF4A-IN-1
    Inhibitor
    HNF4A-IN-1 (Compound 17) is a Hepatocyte nuclear factor 4 alpha (HNF4A) inhibitor. HNF4A-IN-1 has potent anticancer activity against human head and neck squamous cells (SCC131 cells) and with no toxicity to normal cells. HNF4A-IN-1 significantly inhibits SCC131 cells growth with an IC50 of 1.75 μM, and induces apoptosis and G2/M cell cycle arrest. HNF4A-IN-1 promotes tumor regression in SCC131 tumor xenografts mouse models.
  • HY-107404
    SID 7969543
    Inhibitor 99.42%
    SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily.
  • HY-128207
    SID7970631
    Inhibitor 98.30%
    SID7970631, as an isoquinolinone analog, is a potent and selective submicromolar SF-1 inhibitor (IC50=255 nM). SID7970631 can be used for the research of cancer.
  • HY-156190
    NR2F2-IN-1
    Inhibitor
    NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation.
  • HY-118054
    LRH-1 Inhibitor-3
    Inhibitor
    LRH-1 Inhibitor-3 is a small molecule that inhibits LRH-1 transcriptional activity, thereby decreasing the expression of target genes associated with cell growth and proliferation. LRH-1 Inhibitor-3 has shown potential in reducing cancer cell proliferation in human pancreatic, colon, and breast adenocarcinoma cell lines. LRH-1 Inhibitor-3 serves as a molecular probe for investigating the role of LRH-1 in various malignancies.
  • HY-155168
    Iso-RJW100
    Inhibitor
    Iso-RJW100 (compound 24-endo) is a dual-liver receptor homologue-1 (LRH-1) and steroidogenic factor-1 (SF-1) agonist with pEC50 of 6.4 and 7.2, respectively.