Cayman S3I-201

Signal transducers and activators of transcription (STATs) are a family of latent cytoplasmic transcription factors that convey signals from the cell membrane to the nucleus. In various human tumors, STAT3 is constitutively activated by aberrant upstream tyrosine kinase activities.¹ STAT signaling is also suspected to play a role in vascular disease since it can be activated through angiotensin II type 1 receptors or the inflammatory mediator interleukin (IL)-6.² S3I-201 is an inhibitor of STAT3 transcription factor activation, dimerization, and gene transcription. It can suppress IL-6-induced phosphorylation of STAT3 in T cells with an IC₅₀ value of 38 μM.³ Inhibiting STAT3 activation with 10 μM S3I-201 was demonstrated to be protective against angiotensin II-induced oxidative stress, endothelial dysfunction, and hypertension in two different models of vascular disease.² At 10 μM, S3I-201 has also been used as a means to regress cardiac hypertrophy by inhibiting collagen biosynthesis and decreasing atrial natriuretic factor and β-myosin heavy chain in an in vitro model.⁴

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