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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ETP 45658是活性的 PI 3-激酶 抑制剂， 也抑制 DNA-PK，mTOR。
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BAG 956是双效的 PI 3-激酶，PDK1 抑制剂。
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AZD8186是一种特异性的PI3K抑制剂, 有效抑制PI3Kβ (IC50=4 nM) 和PI3Kδ (IC50=12 nM),选择性比PI3Kα (IC50=35 nM) 和PI3Kγ (IC50=675 nM) 高。
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PI 828是PI 3-激酶抑制剂， 抑制活性胜过LY 294002 。
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PF 05212384是活性的，选择性双效的PI 3-K/mTOR 抑制剂。
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