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Submit ReviewTC-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.
TC-S 7009 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
M. Wt | 308.65 |
Formula | C12H6ClFN4O3 |
Storage | Store at RT |
Purity | ≥99% (HPLC) |
CAS Number | 1422955-31-4 |
PubChem ID | 70697712 |
InChI Key | CDQUJZKBRAFWNG-UHFFFAOYSA-N |
Smiles | ClC1=CC(F)=CC(NC3=C([N+]([O-])=O)C2=NON=C2C=C3)=C1 |
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 | |
---|---|---|---|
Solubility | |||
DMSO | 30.86 | 100 |
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
If you know of a relevant reference for TC-S 7009, please let us know.
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
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
Kyoung Min et al (2020) A system-level approach identifies HIF-2α as a critical regulator of chondrosarcoma progression. Nat Commun 11 5023 PMID: 33024108
Do you know of a great paper that uses TC-S 7009 from Tocris? Please let us know.
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