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A cell-permeable benzoxazolone-containing bioisostere of tyrphostin AG 538 (Cat. No. 658403) that acts as a potent, substrate-competitive, but not ATP-competitive, inhibitor of insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R). It is selective towards IR and IGF-1R (IC50 = 0.4 and 0.43 µM, respectively) and inhibits Src and PKB only at much higher concentrations (IC50 = 2.2 and 55 µM, respectively) in kinase assays. Shown to prevent IGF-1-induced cellular IGF-1R autophosphorylation and down stream signalling. Specifically inhibits IGF-1-induced, but not PDGF-induced, activation of PKB in cells. Effectively blocks the formation of colonies in soft agar by breast and prostate cancer cells. Exhibits improved cellular oxidative stability than AG 538.
|References||Blum, G., et al. 2003. J. Biol. Chem. 278, 40442.|
|Structure formula Image|
|Primary Target IC<sub>50</sub>||0.43 µM|
|Secondary target||IR (IC₅₀ = 0.4 µM) and inhibits Src and PKB at (IC₅₀ = 2.2 and 55 µM, respectively)|
|Purity||≥97% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Blum, G., et al. 2003. J. Biol. Chem. 278, 40442.|