PIP4K-IN-a131 is a selective inhibitor of PIP4K lipid kinases, demonstrating IC50 values of 1.9 μM for PIP4K2A and 0.6 μM for PIP4Ks. It exhibits cancer-selective lethality by simultaneously blocking the lipid kinase PIP4Ks and mitotic pathways.

PIP4Ks:0.6 µM (IC50), PIP4K2A:1.9 µM (IC50)

PIP4K-IN-a131 (0-100 μM; 72?hours) is a potent antiproliferative agent with a clear selectivity toward cancer cells killing[1]. PIP4K-IN-a131 eliminates cancer cells via a dual-inhibitory mechanism[1]. PIP4K-IN-a131 causes inhibition of the PI3K/Akt/mTOR pathway only in normal BJ cells, but not in transformed counterparts[1]. 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[1]. Cell Proliferation Assay[1]Cell Line: Normal and transformed BJ cells Concentration: 0-100 μM (MTT assay) Incubation Time: 72?hours Result: Selective killed cancer cells. RT-PCR[1]Cell Line: BJ cells Concentration: 5?μM Incubation Time: 24?hours Result: Induced the upregulation of PIK3IP1 mRNA levels.