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Xcessbio/HIF-C2, HIF-2 Inhibitor -Xcessbio Biosciences Inc/2mg solid/M60121-2s

Details
Product Information
Molecular Weight:308.65
Formula:C12H6ClFN4O3
Purity:≥98%
CAS#:1422955-31-4
Solubility:DMSO up to 50 mM
Chemical Name:N-(3-chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine
Storage:Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year.

Biological Activity:

HIF-C2 is a potent and selective allostericinhibitor of hypoxia inducible factor-2 (HIF-2). It binds within the internalcavity of HIF-2α PAS-B (Kd of 81 nM) and disrupts heterodimerizationof the full-length HIF-2 transcription factor. HIF-C2 functions effectively as aHIF-2 inhibitor in living cells, disrupting HIF-2 DNA binding and inhibiting thetranscription of its target genes. Moreover, HIF-C2 is selective for the HIF-2isoform and has no activity to antagonize HIF-1. HIF-C2 provides an opportunityto delineate differences in HIF-1 and HIF-2 biology and serves as an entrypoint for development of HIF-2 inhibitor drugs for treating diseases, includingrenal cell carcinomas.

How to Use:

  • In vitro: HIF-C2 was used at 10 µM final concentration in vitro and in cellular assays.
  • In vivo:n/a

Reference:

  • 1. Scheuermann TH, et al. Allosteric inhibition of hypoxia inducible factor-2 with small molecules. (2013) Nat Chem Biol 9(4):271-6.
  • 2.Rogers JL, et al.Development of Inhibitors of the PAS-B Domain of the HIF-2α TranscriptionFactor. (2013) J Med Chem. 56(4):1739-47.

  • HIF-C2_spec.pdf
  • HIF-C2_MSDS.pdf

Products are for research use only. Not for human use.

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