Ro 106-<wbr/>9920

Ro 106-9920

CAT N°: 15373
Price:

From 74.00 62.90

Transcriptional activation by NF-?B is limited by I?B? binding, which masks the NF-?B nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target I?B? for degradation, enabling NF-?B to promote gene expression. Because NF-?B 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-?B-dependent expression of TNF-?, interleukin-1?, and interleukin-6 (IC50 50 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.{25615} 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.{25615}

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