PI-273 (PI273) is a potent, specific, substrate-competitive small molecule inhibitor ofPI4KIIα with IC50 of 0.47 uM.
PI-273 reduces PI4P content, cell viability and AKT signaling in wild-type MCF-7 cells but not in PI4KIIα knockout MCF-7 cells.
PI-273 retards cell proliferation by blocking cells in G2/M, inducing cell apoptosis and suppressing colony-forming ability, significantly inhibits MCF-7 cell-induced breast tumor growth without toxicity in a xenograft model (intravenous or intragastrical).
