| Bioactivity | 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]. | ||||||||||||
| Target | Kd: 81 nM (HIF-2α) | ||||||||||||
| Invitro | 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]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| Name | TC-S 7009 | ||||||||||||
| CAS | 1422955-31-4 | ||||||||||||
| Formula | C12H6ClFN4O3 | ||||||||||||
| Molar Mass | 308.65 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. [2]. Senavirathna LK, et al. Hypoxia induces pulmonary fibroblast proliferation through NFAT signaling. Sci Rep. 2018 Feb 9;8(1):2709. |
TC-S 7009
CAS: 1422955-31-4 F: C12H6ClFN4O3 W: 308.65
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 H
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