BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM).
bx-517 is a potent and selective inhibitor of pdk1 that binds to the atp binding pocketof the protein (ic50 = 6 nm). bx-517 also blocks activation of akt in tumor cells with 10-fold more potent (ic50 = 0.1–1.0 μm) than its analogs tested at the highest dose tested (10 μm). [1] the phosphoinositide-dependent kinase-1 (pdk1) is a ser/thr kinase that is a crucial activator of a range of protein kinases in the agc kinase super-family that play key roles in the progression of cancer and for the activation of akt, s6 kinase, and protein kinase c. [2]
1. islam i, brown g, bryant j et al. indolinone based phosphoinositide-dependentkinase-1 (pdk1) inhibitors. part 2: optimization of bx-517. bioorg med chem lett.2007 jul 15;17(14):3819-25. 2. islam i, bryant j, chou yl etc. indolinone based phosphoinositide-dependent kinase-1 (pdk1)inhibitors. part 1: design, synthesis and biological activity. bioorg med chem lett. 2007 jul 15;17(14):3814-8.
