Merck, 259545-10MG, Deoxyhypusine Synthase Inhibitor, GC7 Sulfate

General description
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 µM. 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 µM and 40 µM. In addition, it is shown to significantly impair the growth and invasion of primary HCC cells (HepG2 and Hep3B) in the 10-20 µM range, and against non-tumorigenic CL-48 cells at concentrations as high as 40 µM, with no apparent cytotoxicity. At 25 µM, GC7 treatment is shown to reverse eIF5a-mediated Skeletal Muscle Stem Cell Differentiation.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lee, N.P., et al. 2010. Int J Cancer.4, 968.
Luchessi, A., et al. 2008. J Cell Physiol.3, 480.
Balabanov, S., et al. 2007. Blood.4, 1701.
Jakus, J., et al. 1993. J Biol Chem.18, 13151.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)