PI3K?/HDAC6-IN-1

Description

PI3K?/HDAC6-IN-1 Compound 22E is an orally active and dual inhibitor of PI3K? and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3K?/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma NHL cells and possesses in vivo antitumor activity without significant toxicity. PI3K?/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3K?/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of ?-tubulin and histone H3.