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JAK/STAT


The JAK-STAT signaling pathway transmits information from extracellular chemical signals to the nucleus resulting in DNA transcription and expression of genes involved in immunity, proliferation, differentiation, apoptosis and oncogenesis. The JAK-STAT signalling cascade consists of three main components: a cell surface receptor, a Janus kinase (JAK) and two Signal Transducer and Activator of Transcription (STAT) proteins. Disrupted or dysregulated JAK-STAT functionality can result in immune deficiency syndromes and cancers.

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    Trametinib (GSK1120212)是一种高特异性的，有效的MEK1/2抑制剂，IC50为0.92 nM/1.8 nM，对c-Raf， B-Raf， ERK1/2没有抑制活性。

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  • PLX-4720 EY0658

    PLX 4720是B-RafV600E和c-Raf-1Y340D/Y341D的抑制剂，IC50分别为13 nM和6.7 nM。

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    SCH772984是一种新型特异性的ERK1/2抑制剂， IC50分别为4 Nm/1 nM。

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  • Selumetinib EY0454

    Selumetinib (AZD6244)是一种高选择性的MEK1抑制剂，IC50为14 nM，也抑制ERK1/2磷酸化，IC50为10 nM，但对p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等没有抑制作用。

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  • GDC-0623 EY1748

    GDC-0623是一种有效的 ATP 非竞争性MEK1抑制剂，Ki为 0.13 nM。

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