TC-S 7009

• CAT Number: R030399
• CAS Number: 1422955-31-4
• Molecular Formula: C12H6ClFN4O3
• Molecular Weight: 308.65
• Purity: ≥95%
• Synonyms: N-(3-chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine
• InChI: InChI=1S/C12H6ClFN4O3/c13-6-3-7(14)5-8(4-6)15-10-2-1-9-11(17-21-16-9)12(10)18(19)20/h1-5,15H
• InChIKey: CDQUJZKBRAFWNG-UHFFFAOYSA-N
• SMILES: C1=CC2=NON=C2C(=C1NC3=CC(=CC(=C3)Cl)F)[N+](=O)[O-]

TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression[1][2].
TC-S 7009 (0-100 μM; 72 hours; HPF cells) treatment shows greater inhibition of cell proliferation in hypoxic conditions than that in normoxic conditions[2].
TC-S 7009 (50 μM) treatment almost completely inhibits the hypoxia-induced NFATc2 nuclear translocation[2].

Reference

[1]. Scheuermann TH, et al. Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat Chem Biol. 2013 Apr;9(4):271-6.
 [Content Brief]

[2]. Senavirathna LK, et al. Hypoxia induces pulmonary fibroblast proliferation through NFAT signaling. Sci Rep. 2018 Feb 9;8(1):2709.
 [Content Brief]