TC-S 7009

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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% (HPLC)
Citations (2)
Literature (2)

Biological Activity for TC-S 7009

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.

Compound Libraries for TC-S 7009

TC-S 7009 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for TC-S 7009

M. Wt 308.65
Formula C12H6ClFN4O3
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 1422955-31-4
PubChem ID 70697712
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.

Solubility Data for TC-S 7009

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 30.86 100

Preparing Stock Solutions for TC-S 7009

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for TC-S 7009

Certificate of Analysis / Product Datasheet
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References for TC-S 7009

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.

View Related Products by Product Action

View all Hypoxia Inducible Factor (HIF) Inhibitors

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

2 Citations for TC-S 7009

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

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

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

Do you know of a great paper that uses TC-S 7009 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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