opb-51602

OPB-51602 is an orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3), developed for its potential antineoplastic activity. It inhibits both tyrosine (Tyr705) and serine (Ser727) phosphorylation sites on STAT3, thereby blocking its activation, nuclear translocation, and regulation of gene expression. In addition to inhibiting the canonical transcriptional activity of STAT3, OPB-51602 disrupts mitochondrial functions by inhibiting complex I activity in a STAT3-dependent manner, leading to increased reactive oxygen species production, mitophagy, actin rearrangements, and cell death in tumor cells. The drug was investigated primarily for relapsed or refractory hematological malignancies but showed limited clinical efficacy with notable toxicities[1][2][4][5][6].

Other names

STAT3 inhibitor OPB-51602STAT-3 inhibitor OPB-51602STAT 3 inhibitor OPB-51602