货号 | 16090-10mg |
描述 | Signal transducer and activator of transcription 3 (STAT3) is a cytokine-inducible transcription factor with roles in inflammation and cancer.1,2 5,15-DPP is a cell-permeable porphyrin derivative that selectively binds STAT3 (Kd = 880 nM).3 This inhibits STAT3 dimerization via Src homology 2 (Sh2) domains (IC50 = 280 nM), preventing nuclear translocation and DNA binding.3 5,15-DPP poorly inhibits STAT1 (IC50 = 10 µM) and does not affect Grb2.3 It reduces IL-6-dependent STAT3 activation and consequent c-myc expression in MDA-MB-468 cells and blocks TRAIL-induced migration and invasion in A549 cells.3,4 Furthermore, inhibition of JAK/STAT signaling in satellite cells via 5,15-DPP and the JAK2 inhibitor AG-490 (Item No. 10010311) has been used to stimulate muscle regeneration in a model of aging skeletal muscle deterioration.5 |
别名 | 5,15-Diphenylporphyrin;STAT3 Inhibitor VIII; |
供应商 | Cayman |
应用文献 | |
1.Poli, V. The role of C/EBP isoforms in the control of inflammatory and native immunity functions. The Journal of Biological Chemisty 273, 29279-29282 (1998). 2.Yu, H. and Jove, R. The stats of cancer - new molecular targets come of age. Nature Reviews.Cancer 4, 97-105 (2004). 3.Uehara, Y.,Mochizuki, M.,Matsuno, K., et al. Novel high-throughput screening system for identifying STAT3-SH2 antagonists. Biochemical and Biophysical Research Communications 380(3), 627-631 (2009). 4.Azijli, K.,Yuvaraj, S.,Peppelenbosch, M.P., et al. Kinome profiling of non-canonical TRAIL signaling reveals RIP1-Src-STAT3-dependent invasion in resistant non-small cell lung cancer cells. Journal of Cell Science 125(Pt 19), 4651-4661 (2012). 5.Price, F.D.,von Maltzahn, J.,Bentzinger, C.F., et al. Inhibition of JAK-STAT signaling stimulates adult satellite cell function. Nature Medicine 20(10), 1174-1181 (2014). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 462.6 |
分子式 | C32H22N4 |
CAS号 | 22112-89-6 |
稳定性 | ≥ 2 years |
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