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[1].
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
[1]. Mayumi Kitagawa, et al. Dual Blockade of the Lipid Kinase PIP4Ks and Mitotic Pathways Leads to Cancer-Selective Lethality. Nat Commun. 2017 Dec 19;8(1):2200.