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HIF-2alpha-I2 | HIF-2alpha antagonist

HIF-2α-I2 (1422955-31-4) is a potent and selective HIF-2α inhibitor, Kd=81 nM.1 Binds to the HIF-2α PAS-B domain2 and interferes with Hif-2α / ARNT heterodimerization reducing target gene expression in a cellular model1. Highly selective for HIF-2α displaying a >60-fold selectivity over HIF-1α.1,2

References/Citations

1) Scheuermann et al. (2013), Allosteric inhibition of hypoxia inducible factor-2 with small molecules; Nat. Chem. Biol., 9 271
2) Masetti et al. (2014), Protein dynamics of the HIF-2α PAS-B domain upon heterodimerization and ligand binding; PLoS One, 9(4) e94986
3) Rodgers et al. (2013), Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor; J. Med. Chem., 56 1739

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HIF-2alpha-I2 | 1422955-31-4 | Structure | Supplier

Catalog#  10-1508-0005

$70.00
Quantity
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CAS:
1422955-31-4
Catalog Number:
10-1508
Activity:
Hif-2α antagonist
Chemical Name:
N-(3-chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine
Alternate Names:
TC-S 7009
Molecular Weight:
308.65
Molecular Formula:
C12H6ClFN4O3
Solubility:
Soluble in DMSO (up to 30 mg/ml) or in DMF (up to 35 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or DMF may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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