HIF-C2 is a potent and selective allosteric inhibitor of hypoxia inducible factor-2 (HIF-2). It binds within the internal cavity of HIF-2α PAS-B (Kd of 81 nM) and disrupts heterodimerization of the full-length HIF-2 transcription factor. HIF-C2 functions effectively as a HIF-2 inhibitor in living cells, disrupting HIF-2 DNA binding and inhibiting the transcription of its target genes. Moreover, HIF-C2 is selective for the HIF-2 isoform and has no activity to antagonize HIF-1. HIF-C2 provides an opportunity to delineate differences in HIF-1 and HIF-2 biology and serves as an entry point for development of HIF-2 inhibitor drugs for treating diseases, including renal cell carcinomas.
CAS Number: 1422955-31-4
Molecular Weight: 308.65
Chemical Name: N-(3-chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
HIF-C2 was used at 10 µM final concentration in vitro and in cellular assays.
- Scheuermann TH, et al. Allosteric inhibition of hypoxia inducible factor-2 with small molecules. (2013) Nat Chem Biol 9(4):271-6.
- Rogers JL, et al. Development of Inhibitors of the PAS-B Domain of the HIF-2α Transcription Factor. (2013) J Med Chem. 56(4):1739-47.
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