Ro 106-9920
货号:
15373-1mg 基本售价:
546.0 元 规格:
1 mg
产品信息
概述货号 | 15373-1mg |
描述 | Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50< 1 µM in human peripheral blood mononuclear cells).1 It selectively inhibits the ubiquitination of activated IκBα with an IC50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.1 In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.1 |
性能供应商 | Cayman |
应用文献 |
1.Swinney, D.C.,Xu, Y.Z.,Scarafia, L.E., et al. A small molecule ubiquitination inhibitor blocks NF-κB-dependent cytokine expression in cells and rats. The Journal of Biological Chemisty 277(26), 23573-23581 (2002).
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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 | 245.3 |
分子式 | C10H7N5OS |
CAS号 | 62645-28-7 |
稳定性 | ≥ 2 years |
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