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Beschreibung

A cell-permeable, water soluble and specific p53-Snail binding inhibitor that activates p53 in a K-Ras-dependent manner and displays anti-proliferating effect toward K-Ras-MEF (K-Ras-transformed mouse embryonic fibroblast) cells with 20% viability at 10µ,M, but not in N-Ras/Myc-MEF or non-transformed MEF. Snail and p53 expression are elevated in a dose dependent manner after GN25 treatment at 1-10µ,M in K-Ras-mutated human cancer cell lines A549, but not in MKN-45 (wt-K-Ras/wt-p53) cells. Furthermore, it is shown to selectively activate wild-type p53 in p53WT/MT cancer cells, but not Panc-1 cells with single allelic mutant p53. Exhibits anti-tumor effect in a xenograft model in vivo.