HIF-C2,HIF-2Inhibitor
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產品名稱: HIF-C2,HIF-2Inhibitor
產品型號: M60121-2
產品展商: 其它品牌
產品文檔: 無相關文檔
簡單介紹
HIF-C2,HIF-2Inhibitor
HIF-C2,HIF-2Inhibitor
的詳細介紹
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: 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.
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How to Use:?
- In vitro:? HIF-C2 was used at 10 μM final concentration in vitro and in cellular assays.
- In vivo:??n/a
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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.
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Products are for research use only. Not for human use.
