Definition

An orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3), with potential antineoplastic activity. Upon oral administration, STAT3 inhibitor VVD-130850 targets and binds to an allosteric pocket of STAT3. This prevents STAT3 binding to responsive gene promoters, STAT3-mediated signaling and the expression of STAT3 target genes, thereby inhibiting the proliferation of STAT3-overexpressing tumor cells. STAT3 regulates the transcription of genes involved in several cellular functions. STAT3 is constitutively activated in a variety of human cancers and plays a key role in neoplastic transformation, uncontrolled tumor cell proliferation, resistance to apoptosis, metastasis, immune evasion, tumor angiogenesis, epithelial-mesenchymal transition (EMT) and the Warburg effect.