脱氧苏氨酸合成酶抑制剂，GC7-CAS 150333-69-0-Calbiochem

C ₈H ₂₂N ₄O ₄S

270.35

A cell-permeable inhibitor that targets the spermidine-binding site of Deoxyhypusine Synthase (K _i= 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 ?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 ?M and 40 ?M. In addition, it is shown to significantly impair the growth and invasion of primary HCC cells (HepG2 and Hep3B) in the 10-20 ?M range, and against non-tumorigenic CL-48 cells at concentrations as high as 40 ?M, with no apparent cytotoxicity. At 25 ?M, GC7 treatment is shown to reverse eIF5a-mediated Skeletal Muscle Stem Cell Differentiation.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

>95% (NMR)

powder

Calbiochem ^?

OK to freeze
desiccated (hygroscopic)

white

water: 25 mg/mL, clear, colorless

ambient

?20℃

10 mg in Glass bottle

11 - Combustible Solids

WGK 1