In Vitro: PP2A Cancerous-IN-1 (2.5 and 5 μM; 24 hours; SK-Hep-1 cells) reduces CIP2A expression and cell viability with a dose dependent manner and is more potent in its action than erlotinib. PP2A Cancerous-IN-1 (5 μM; 24 hours; SK-Hep-1 cells) induces cell apoptosis. PP2A Cancerous-IN-1 shows CIP2A inhibitory activity, reduces p-Akt level, induces PARP cleavage. PP2A Cancerous-IN-1 exhibits high potency with low IC50 values of 2.8 μM against HCC cells.