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TC-S 7009

Catalog #: 5243
2 Citations Datasheet / COA / SDS
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5243/5
TC-S 7009 | CAS No. 1422955-31-4 | HIF Inhibitors
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Description: High affinity and selective HIF-2α inhibitor

Chemical Name: N-(3-Chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine

Purity: ≥99%

Product Details
Citations (2)
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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

TC-S 7009 is a high affinity and selective HIF-2α inhibitor (Kd = 81 nM). Binds to the HIF-2α PAS-B domain; disrupts HIF-2α-ARNT heterodimerization. Exhibits >60-fold selectivity for HIF-2α over HIF-1α. Decreases HIF-2α DNA-binding and attenuates expression of HIF-2α target genes in vitro.

Technical Data

M.Wt:
308.65
Formula:
C12H6ClFN4O3
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
1422955-31-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Allosteric inhibition of hypoxia inducible factor-2 with small molecules.
    Scheuermann TH, Li Q, Ma HW et al.
    Nat Chem Biol
  2. Hypoxia induces pulmonary fibroblast proliferation through NFAT signaling
    LK Senavirath, C Huang, X Yang, MC Munteanu, R Sathiaseel, D Xu, CA Henke, L Liu
    Sci Rep, 2018;8(1):2709.
  3. Bidirectional modulation of HIF-2 activity through chemical ligands.
    Wu et al.
    Nat.Chem.Biol., 2019;15:367
  4. Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor.
    Rogers et al.
    J.Med.Chem., 2013;56:1739

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Citations for TC-S 7009

The citations listed below are publications that use Tocris products. Selected citations for TC-S 7009 include:

2 Citations: Showing 1 - 2

  1. A system-level approach identifies HIF-2α as a critical regulator of chondrosarcoma progression.
    Authors: Kyoung Min Et al.
    Nat Commun  2020;11:5023
  2. HIF-2α, but not HIF-1α, mediates hypoxia-induced up-regulation of Flt-1 gene expression in placental trophoblasts.
    Authors: Sasagawa Et al.
    Sci Rep  2018;8:17375

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