STAT3 Dual Phosphorylation Site Inhibitor YY201

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable inhibitor of signal transducer and activator of transcription 3 (STAT3), with potential antineoplastic activity. Upon oral administration, STAT3 dual phosphorylation site inhibitor YY201 targets, binds to and inhibits Tyr705 and Ser727 double-site phosphorylation of STAT3, thereby inhibiting the function of STAT3. This prevents STAT3 binding to responsive gene promoters, STAT3-mediated signaling and the expression of STAT3 target genes. This inhibits 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.

**Synonyms:** - STAT3 Inhibitor YY201 - YY 201 - YY-201 - YY201