PDK1 inhibitor is an potent and selective inhibitor of PDK1 with potential as anticancer agent. GSK 2334470,a inhibitor of PDK1, has IC50 value of 0.00251µM and CHEMBL1172241 with IC50 value of 0.085µM.
BX795, a small molecule with an aminopyrimidine backbone in its chemical structure, is a potent and ATP-competitive inhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1) that binds to the ATP binding pocket of PDK1 and hence potently inhibits the enzymatic activity of PDK1 in a direct kinase assay format with a value of 50% concentration inhibition IC50 of 11 nM.
BX-912 is a potent and selective inhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1) with IC50 value of 26nM . BX-912 has shown 9-fold selectivity for PDK1 relative to PKA and 105-fold selectivity against PKC .