TPCVIP(LA)1 is a direct dual inhibitor for both IKKβ (IKK-2) and STAT3. It inhibits STAT3 phosphorylation, DNA binding, and transactivation in vivo. Synergistic treatment of TPCVIP(LA)1 with tyrosine kinase inhibitors (TKIs) can potentially be a more effective method for treating cancers.