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Beschreibung

A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC50 = 600 nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC50 = 1 to 2.5 mM) while sparing normal epithelial cells. Its effect on cancer cells have been attributed to induction of autophagy and apoptosis. Suppresses ILK-mediated phosphorylation of Akt at Ser473 site, thereby down-regulating the downstream targets, such as GSK-3b and myosin light chain. Also causes a transcriptional repression of the transcription factor Y-Box binding protein 1 (YB-1). Exhibits minimum toxicity in mouse model., A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC50 = 600 nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC50 = 1 to 2.5 µ,M) while sparing normal epithelial cells. Its effect on cancer cells have been attributed to induction of autophagy and apoptosis. Suppresses ILK-mediated phosphorylation of Akt at Ser473 site, thereby down-regulating the downstream targets, such as GSK-3b and myosin light chain. Also causes a transcriptional repression of the transcription factor Y-Box binding protein 1 (YB-1). Exhibits minimum toxicity in mouse model.