pi 14

PI3K/mTOR Inhibitor-14 (compound Y-2) serves as a dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 171.4 nM and 10.1 nM , respectively, and demonstrates antitumor activities [1].

PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and markedly diminishes mitochondrial membrane potential, resulting in cell cycle arrest at the G1 phase and apoptosis in U87-MG cells. Additionally, it demonstrates significant antiproliferative effects against various tumor cell lines, including PC-3 with an IC50 of 0.28 μM, HCT-116 with an IC50 of 0.57 μM, and U87-MG with an IC50 of 1.37 μM [1].

PI3Kδ-IN-14 (Compound (S)-29), a selective PI3Kδ inhibitor with an IC50 of 0.8 nM and a Kd of 84.8 nM, targets the ATP-binding site within the kinase domain of PI3Kδ. This compound exhibits anti-inflammatory properties by impeding the PI3K/AKT pathway and is noted for alleviating acute lung injury (ALI) [1].

MI-14 is a potent and selective inhibitor of PI 4-K IIIß.