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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.

  • U0126-EtOH EY1161

    U0126-EtOH(U-0126)是MEK1和2选择性抑制剂，IC50分别为70nM和60nM，对ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。

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  • PD184352 EY1139

    PD184352 (CI-1040)是一种ATP非竞争性的MEK1/2抑制剂，IC50为17 nM，对MEK1/2的选择性比MEK5高100倍。

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  • PD0325901 EY1046

    PD0325901是一种选择性的，ATP非竞争性的MEK抑制剂，IC50为0.33 nM，对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。

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  • PD98059 EY0820

    PD98059是一种非ATP竞争性的MEK抑制剂，IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。

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  • BIX 02188 EY0802

    BIX 02188是一种选择性的MEK5抑制剂，IC50为4.3 nM，也抑制ERK5催化活性，IC50为810 nM，且不抑制与其密切相关的激酶MEK1， MEK2， ERK2，和JNK2。

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