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. 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. 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. 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. 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 beta-myosin heavy chain in an in vitro model.Formal Name: 2-hydroxy-4-[[2-[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]-benzoic acid. CAS Number: 501919-59-1. Synonyms: NSC 74859. Molecular Formula: C16H15NO7S. Formula Weight: 365.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12.5 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 16 mg/ml. lambdamax: 219, 268, 309 nm. SMILES: OC(C1=C(O)C=C(NC(COS(C2=CC=C(C)C=C2)(=O)=O)=O)C=C1)=O. InChi Code: InChI=1S/C16H15NO7S/c1-10-2-5-12(6-3-10)25(22,23)24-9-15(19)17-11-4-7-13(16(20)21)14(18)8-11/h2-8,18H,9H2,1H3,(H,17,19)(H,20,21). InChi Key: HWNUSGNZBAISFM-UHFFFAOYSA-N.