Orphan Nuclear Receptor Inhibitor

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.

NR2F2-IN-1 (COUP-TFII inhibitor) free base is a small-molecule inhibitor targeting the orphan nuclear receptor COUP-TFII (NR2F2). NR2F2-IN-1 free base directly binds to the ligand-binding domain of COUP-TFII (NR2F2) and disrupts its interaction with transcriptional regulators including FOXA1. NR2F2-IN-1 free base induces anti-tumor activity in prostate cancer and can be used for prostate cancer research.

XY25028 is an orally active LRH-1 inhibitor with an IC₅₀ of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer.

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.

DHQZ-17 is a HNF4A inhibitor. DHQZ-17 triggers apoptosis in head and neck squamous cell carcinoma cells. DHQZ-17 can be used for the research of head & neck squamous cell carcinoma.

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.

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.

NR2F2-IN-1 (COUP-TFII inhibitor) is a small-molecule inhibitor targeting the orphan nuclear receptor COUP-TFII (NR2F2). NR2F2-IN-1 directly binds to the ligand-binding domain of COUP-TFII (NR2F2) and disrupts its interaction with transcriptional regulators including FOXA1. NR2F2-IN-1 induces anti-tumor activity in prostate cancer and can be used for prostate cancer research.

XY25026 is an orally active LRH-1 inhibitor with an IC₅₀ of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer.

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.

SID 7969543 (Standard) is the analytical standard of SID 7969543 (HY-107404). This product is intended for research and analytical applications. 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.