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.
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CZC24832是PI3Kγ选择性抑制剂，在PI3Kγ依赖的fMLP诱导的中性粒细胞迁移实验中IC50为1.0 μM，且对其它多种蛋白的脱靶效应极有限。
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AS-604850是一种选择性的，ATP竞争性的PI3Kγ抑制剂，IC50为250 nM，作用于PI3Kγ比作用于PI3Kδ/β选择性高80倍以上，作用于PI3Kγ比作用于PI3Kα选择性高18倍。
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PIK-294是p110δ高选择性抑制剂，IC50值为10nM,对PI3Kα/β/γ作用弱。
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PIK-90是PI3Kα，γ和δ抑制剂，IC50分别为11 nM，18 nM和58 nM，对PI3Kβ的IC50为350 nM。
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VS-5584是PI3K/mTOR双重抑制剂，对mTOR和PI3Kα/β/δ/γ的IC50分别为3.4 nM和2.6-21 nM。
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