BAY-091 (BAY091) is a potent and highly selective inhibitor of PIP4K2A with IC50 of 16 nM in the high ATP (2 mM) HTRF assay.
BAY-091 showed excellent kinase selectivity profile a commercial kinase panel (Millipore, 373 kinases) at 1 uM, none of the potential off-target kinases was inhibited >60%.
BAY-091 displayed drug-like physicochemical properties with favorable lipophilicity (log D), TPSA, and aqueous solubility and exhibited high metabolic stability in human and rat liver microsomes as well as in rat hepatocytes.
BAY-091did not increase the levels of p-AKT (Ser473 and Thr308) in THP-1 cells up to a concentration of 50 uM, also was unable to induce changes in the p-PP2A (Tyr307) protein levels.
BAY-091 is a valuable chemical probe to study PIP4K2A signaling and its involvement in pathophysiological conditions such as cancer.
