BAY-091 is a potent and highly selective PIP4K2A inhibitor (IC50 = 1.3/2.6 nM with 10/250 μM [ATP] by ADP-Glo, 8.5/16.4 nM with 10 μM/2 mM [ATP] by HTRF) with good cellular permeability (target engagement EC50 = 1.1 μM/intact cells vs 1.8 μM/cell lysate by CETSA) and no significant off-target activity as assessed by a 373-kinase panel (<60% inhibition at 1 μM).
Potent and highly selective PIP4K2A inhibitor with good cellular permeability and no significant off-target activity.
Journal of medicinal chemistry, 64(21), 15883-15911 (2021-10-27)
PIP4K2A is an insufficiently studied type II lipid kinase that catalyzes the conversion of phosphatidylinositol-5-phosphate (PI5P) into phosphatidylinositol 4,5-bisphosphate (PI4,5P2). The involvement of PIP4K2A/B in cancer has been suggested, particularly in the context of p53 mutant/null tumors. PIP4K2A/B depletion has
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