PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9?μM and 0.6?μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.IC50 & Target: IC50: 1.9?μM (PIP4K2A), 0.6?μM (PIP4Ks)In Vitro: PIP4K-IN-a131 (0-100 μM; 72?hours) is a potent antiproliferative agent with a clear selectivity toward cancer cells killing.
PIP4K-IN-a131 eliminates cancer cells via a dual-inhibitory mechanism.
PIP4K-IN-a131 causes inhibition of the PI3K/Akt/mTOR pathway only in normal BJ cells, but not in transformed counterparts.
Inhibition of PIP4Ks by PIP4K-IN-a131 arrests normal cells at the G1/S phase of the cell cycle by suppressing the PI3K/Akt/mTOR signaling pathway via transcriptional upregulation of PIK3IP1.