生物活性 | |||
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描述 | The signal transducer and activator of transcription 3 (STAT3) is a transcription factor associated with liver injury, inflammation, and regeneration. SC-1 (which is STAT3-IN-7), an aryl sulfonamide azetidine compound, is an orally active STAT3 inhibitor. It is a derivative of the multiple tyrosine kinase inhibitor sorafenib, blocks STAT3 phosphorylation and activation, and induces apoptosis in hepatocellular carcinoma cell lines, and has anticancer activities. SC-1 had dose- and time-dependent effects against cell viability on HSC-T6, LX2, and mouse primary hepatic stellate cells (HSCs). Further, SC-1 down-regulated p-STAT3 and suppressed Mcl-1 and cyclin D1 in both HSC-T6 and LX2 cell lines in a dose-dependent manner. Moreover, SC-1–induced apoptosis was abolished in STAT3-overexpressing HSC cells. In hepatotoxic and cholestatic models, hepatic fibrosis significantly reduced after SC-1 treatment in terms of Metavir fibrosis score and collagen-positive area[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.32mL 0.46mL 0.23mL |
11.58mL 2.32mL 1.16mL |
23.16mL 4.63mL 2.32mL |
参考文献 |
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