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Beschreibung

A cell-permeable inhibitor that targets the spermidine-binding site of Deoxyhypusine Synthase (Ki = 9.7 nM), an enzyme which is responsible for the first step hypunisation of eukaryotic initiation factor 5A (eIF5A). In vivo, it demonstrates almost complete cessation of hypusine formation in CHO cells at >= 1 µ,M. Several studies indicate this compound as a useful tool for the down-regulation of eIF5A, a protein essential for cell proliferation. For example, it exhibits an anti-proliferative effect on both BCR-ABL -positive and -negative leukemia cell lines (K562 and HL-60) dose-dependently, at concentrations between 5 µ,M and 40 µ,M. In addition, it is shown to significantly impair the growth and invasion of primary HCC cells (HepG2 and Hep3B) in the 10-20 µ,M range, and against non-tumorigenic CL-48 cells at concentrations as high as 40 µ,M, with no apparent cytotoxicity. At 25 µ,M, GC7 treatment is shown to reverse eIF5a-mediated Skeletal Muscle Stem Cell Differentiation.