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Beschreibung

A cell-permeable thienylhydrazone compound that suppresses the translation of cellular HIF-2alpha message by enhancing the binding of IRP1 (Iron-Regulatory Protein 1) to the IRE (Iron-Responsive Element) region at the 5' UTR of the HIF-2alpha mRNA, exhibiting otherwise no effects toward the transcription of HIF-2alpha mRNA or the stability of HIF-2alpha mRNA and protein. Shown to reduce cellular protein levels of HIF-2alpha and HIF-2alpha target genes, including Glut-1, IGFBP3, and VEGF, in 786-O cells (5 to 10 µ,M final concentration) that express only the 2alpha isoform of hypoxia-inducible factor., A cell-permeable thienylhydrazone compound that suppresses the translation of cellular HIF-2alpha message by enhancing the binding of IRP1 (Iron-Regulatory Protein 1) to the IRE (Iron-Responsive Element) region at the 5' UTR of the HIF-2alpha mRNA, exhibiting otherwise no effects toward the transcription of HIF-2alpha mRNA or the stability of HIF-2alpha mRNA and protein. Shown to reduce cellular protein levels of HIF-2alpha and HIF-2alpha target genes, including Glut-1, IGFBP3, and VEGF, in 786-O cells (5-10 µ,M final concentration) that express only the 2alpha isoform of hypoxia-inducible factor.