NR2F1 agonist 1

• CAT Number: I041744
• CAS Number: 374101-64-1
• Molecular Formula: C28H30N4OS
• Molecular Weight: 470.63
• Purity: ≥95%
• Synonyms: 16-ethylsulfanyl-12-(2-phenylethyl)spiro[12,14,15,17-tetrazatetracyclo[8.7.0.02,7.013,17]heptadeca-1(10),2,4,6,13,15-hexaene-9,1′-cyclohexane]-11-one
• InChI: InChI=1S/C28H30N4OS/c1-2-34-27-30-29-26-31(18-15-20-11-5-3-6-12-20)25(33)23-24(32(26)27)22-14-8-7-13-21(22)19-28(23)16-9-4-10-17-28/h3,5-8,11-14H,2,4,9-10,15-19H2,1H3
• InChIKey: YMOYEJYEEJZQCT-UHFFFAOYSA-N
• SMILES: CCSC1=NN=C2N1C3=C(C(=O)N2CCC4=CC=CC=C4)C5(CCCCC5)CC6=CC=CC=C63

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[1].
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].

Reference

[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.
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