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.
References:
[1]. Leiming Wang, et al. Small-molecule inhibitor targeting orphan nuclear receptor COUP-TFII for prostate cancer treatment. Sci Adv. 2020 Apr 29;6(18):eaaz8031.