CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC50 of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC50 of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models[1].