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TC-S 7009

Names

[ CAS No. ]:
1422955-31-4

[ Name ]:
TC-S 7009

[Synonym ]:
HIF2α-IN-2

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C12H6ClFN4O3

[ Molecular Weight ]:
308.65200

[ Exact Mass ]:
308.01100

[ PSA ]:
96.77000

[ LogP ]:
4.26330

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H413

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds