Skp2 inhibitor; thought to prevent assembly of Skp2-Skp1 complexes. Selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the activity of other SCF complexes. Also inhibits Skp2-mediated p27 and Akt ubiquitination in vivo
and in vitro
. Suppresses the survival of cancer cells and cancer stem cells by triggering cell senescence and inhibiting glycolysis. Exhibits antitumor effects in multiple animal models and cancer cell lines.
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Pharmacological inactivation of Skp2 SCF ubiquitin ligase restricts cancer stem cell traits and cancer progression.
Chan et al.