货号 | 14336-5mg |
描述 | 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 vitromodel.4 |
别名 | NSC 74859; |
供应商 | Cayman |
应用文献 | |
1.Schust, J.,Sperl, B.,Hollis, A., et al. Stattic: A small-molecule inhibitor of STAT3 activation and dimerization. Chemistry & Biology 13(11), 1235-1242 (2006). 2.Johnson, A.W.,Kinzenbaw, D.A.,Modrick, M.L., et al. Small-molecule inhibitors of signal transducer and activator of transcription 3 protect against angiotensin II-induced vascular dysfunction and hypertension. Hypertension 61(2), 437-442 (2013). 3.Zhang, S.,Zheng, M.,Kibe, R., et al. Trp53 negatively regulates autoimmunity via the STAT3-Th17 axis. The FASEB Journal 25(7), 2387-2398 (2011). 4.Mir, S.A.,Chatterjee, A.,Mitra, A., et al. Inhibition of signal transducer and activator of transcription 3 (STAT3) attenuates interleukin-6 (IL-6)-induced collagen synthesis and resultant hypertrophy in rat heart. The Journal of Biological Chemisty 287(4), 2666-2677 (2012). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 365.4 |
分子式 | C16H15NO7S |
CAS号 | 501919-59-1 |
稳定性 | ≥ 2 years |
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