A cell-permeable, phenylbutyrate hydroxamate pan-HDAC inhibitor that is shown to suppress the activities of class I (HDAC1 and HDAC8), class II (HDAC4 and HDAC6), and class IV (HDAC11) HDACs by > ∽90% compared to control, at a concentration of 1μM with a comparable or greater inhibitory effect than SAHA
In vitro , this compound exhibits a broad spectrum of anti-tumor activities in NSCLC cells, holds synergistic effects with cisplatin in the reduction of cell viability, is implicated in the induction of the intrinsic apoptotic pathway, and displays inhibitory effects against mitosis and cytokinesis
This inhibitor is also shown to suppress tumor growth in mice genograft models by 62%, 78% and 90% at 7.5, 15 and 30mg/kg respectively without adversely affect in body weight and detectable toxicity.