| 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: 4oC 3 month; -20oC 1 year. |
Biological Activity:
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.
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 Transcription Factor. (2013) J Med Chem. 56(4):1739-47.
Products are for research use only. Not for human use.
