1422955-31-4

1422955-31-4 structure

Name: TC-S 7009
Chemical Name: N-(3-chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine
CAS Number: 1422955-31-4
Molecular Formula: C₁₂H₆ClFN₄O₃
Molecular Weight: 308.65200
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIF/HIF Prolyl-Hydroxylase
Create Date: 2018-05-11 07:01:13
Modify Date: 2024-01-05 14:43:14
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].

Name	N-(3-chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine
Synonyms	HIF2α-IN-2

Description	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].
Related Catalog	Research Areas >> Inflammation/Immunology Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase
Target	Kd: 81 nM (HIF-2α)[1]
In Vitro	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: HPF cells in hypoxic conditions Concentration: 0-100 µM Incubation Time: 72 hours Result: Showed greater inhibition of cell proliferation in hypoxic conditions than that in normoxic conditions.
References	[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.