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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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 308.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.24 mL||16.2 mL||32.4 mL|
|5 mM||0.65 mL||3.24 mL||6.48 mL|
|10 mM||0.32 mL||1.62 mL||3.24 mL|
|50 mM||0.06 mL||0.32 mL||0.65 mL|
References are publications that support the biological activity of the product.
Scheuermann et al (2013) Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat.Chem.Biol. 9 271 PMID: 23434853
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
Wu et al (2019) Bidirectional modulation of HIF-2 activity through chemical ligands. Nat.Chem.Biol. 15 367 PMID: 30804532
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Keywords: TC-S 7009, TC-S 7009 supplier, TC-S7009, high, affinity, inhibits, inhibitors, HIF2α, HIF2a, HIF2alpha, PASB, hypoxia-inducible, factors, OX3, 0X3, Hypoxia, Inducible, Factors, 5243, Tocris Bioscience
1 Citation for TC-S 7009
Citations are publications that use Tocris products. Selected citations for TC-S 7009 include:
Sasagawa et al (2018) HIF-2α, but not HIF-1α, mediates hypoxia-induced up-regulation of Flt-1 gene expression in placental trophoblasts. Sci Rep 8 17375 PMID: 30478339
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