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Description

A cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition against FAK kinase activity in cell-free assays (IC50 = 0.64 and 2.2 microM, respectively, with 60 or 5 min FAK-inhibitor preincubation before substrate poly-GT and 0.5 microM ATP addition) and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 microM with 30 min inhibitor preincubation before 2 h stimulation by plating cells on fibronectin-coated surface), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38&alpha,, Pyk2, or Src even at concentrations as high as 10 microM., A cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition in kinase assays and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 microM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38&alpha,, Pyk2, or Src even at concentrations as high as 10 microM.