TC-S 7009

Cat. No. 5243

TC-S 7009 C12H6ClFN4O3 [1422955-31-4]

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

Biological Activity

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Rogers et al (2013) Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. J.Med.Chem. 56 1739. PMID: 23363003.

Scheuermann et al (2013) Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat.Chem.Biol. 9 271. PMID: 23434853.

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Keywords: TC-S 7009, supplier, TC-S7009, high, affinity, inhibits, inhibitors, HIF2α, HIF2a, HIF2alpha, PASB, hypoxia-inducible, factors, Tocris Bioscience, Hypoxia Inducible Factor Inhibitor products

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