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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PI-145 (INK1197)是PI3K δ和γ高度选择性抑制剂，Ki和IC50分别为23 pM/243 pM和1 nM/50 nM。
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ZSTK474对I类PI3K亚型，尤其是PI3Kδ有抑制活性，IC50为37 nM。
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IC-87114是一种选择性的PI3Kδ抑制剂，IC50为0.5 μM，作用于PI3Kδ比作用于PI3Kγ和PI3Kα/β选择性分别高58和100倍。
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BEZ235 (NVP-BEZ235, Dactolisib)是一种 ATP竞争性的PI3K和mTOR抑制剂，对p110α/γ/δ/β和mTOR(p70S6K)均有抑制作用，IC50分别为4 nM/5 nM/7 nM/75 nM/6 nM，对ATR也有抑制作用，IC50为21 nM；但对Akt和PDK1抑制作用微弱。
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PI103是PI3K多个亚型抑制剂，对p110alpha，p110beta，p110delta和p110gamma的IC50分别为2 nM，3 nM，3 nM和15 nM，同时对mTOR和DNA-PK的IC50为30 nM和23 nM。
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