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.
NR2F1 agonist 1 (compound C26) (0.5 μM, 1 μM; 18 h) significantly induces luciferase expression in D-HEp3 cells[1].NR2F1 agonist 1 (0.5 μM; 7 d) significantly down-regulates the phosphoinositide 3-kinase (PI3K) signaling pathway[1].NR2F1 agonist 1 (0.5 μM; 7 d) significantly up-regulates mRNA levels of SOX9, RARβ, and p27[1].NR2F1 agonist 1 (0.5 μM; 48 h) induces cell cycle arrest at G0/G1 in D-HEp3 cells[1].
NR2F1 agonist 1 (0.5 mg/kg/day; i.p.; 3 weeks) inhibits inhibits primary tumor growth and metastatic growth in lungs in mouse models[1].
References:
[1]. Khalil BD, et al. An NR2F1-specific agonist suppresses metastasis by inducing cancer cell dormancy. J Exp Med. 2022 Jan 3;219(1):e20210836.