PI3K


PI3K (Phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. Many of these functions relate to the ability of class I PI 3-kinases to activate protein kinase B (PKB, aka Akt) as in the PI3K/AKT/mTOR pathway. The p110δ and p110γ isoforms regulate different aspects of immune responses. PI 3-kinases are also a key component of the insulin signaling pathway. The pathway, with oncogene PIK3CA and tumor suppressor PTEN, is implicated in insensitivity of cancer tumors to insulin and IGF1, and in calorie restriction. PI3K family is divided into four different classes: Class I, Class II, Class III, and Class IV. The classifications are based on primary structure, regulation, and in vitro lipid substrate specificity.
  • PIK-293 EY0385

    PIK-293是 一种PI3K抑制剂,最有效作用于PI3Kδ,IC50为0.24 μM,作用于PI3Kα/β/γ效果分别低500,100和50倍。

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  • CH5132799 EY0315

    CH5132799抑制I型PI3Ks,尤其是PI3Kα,IC50为14 nM;对PI3Kβδγ作用效果稍弱,对PIK3CA突变型细胞系敏感。

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