Bruton's tyrosine kinase (abbreviated Btk or BTK) also known as tyrosine-protein kinase BTK is an enzyme that in humans is encoded by the BTK gene. BTK plays a crucial role in B cell maturation as well as mast cell activation through the high-affinity IgE receptor.
Btk contains a PH domain that binds phosphatidylinositol (3,4,5)-trisphosphate (PIP3). PIP3 binding induces Btk to phosphorylate phospholipase C, which in turn hydrolyzes PIP2, a phosphatidylinositol, into two second messengers, inositol triphosphate (IP3) and diacylglycerol (DAG), which then go on to modulate the activity of downstream proteins during B-cell signalling.
  • DH 97 EI0970

    DH 97是MT2 受体拮抗剂。

  • PF 06465469 EI2123

    PF 06465469是活性的 ITK 抑制剂, 也是抑制 BTK。

  • PCI 29732 EI2066

    PCI 29732是活性的 BTK 抑制剂。

  • LFM-A13 EI1540

    LFM-A13是活性选择性 BTK 抑制剂。

  • Ibrutinib EY0004

    Ibrutinib (PCI-32765)是一种有效的,高选择性的Btk抑制剂,IC50为0.5 nM,能稍许微抑制Bmx, CSK, FGR, BRK及HCK,但对EGFR, Yes, ErbB2, JAK3等作用效果稍弱。

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