GSK2126458 is a potent inhibitor of common activating mutants of p110α (E542K, E545K, and H1047R), with Ki values of 8 pM, 8 pM and 9 pM, respectively. GSK2126458 causes a significant reduction in the levels of pAkt-S473 in T47D and BT474 cells with an IC50 of 0.41 nM and 0.18 nM, respectively. GSK2126458 leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively.
GSK2126458 is an inhibitor of mTOR, PI 3-kinase p110 α, PI 3-kinase p110 β, PI 3-kinase p110 δ and PI 3-kinase p110 γ.
Soluble in DMSO (100 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).
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