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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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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PF-04691502是ATP竞争性PI3K(α/β/δ/γ)和mTOR抑制剂，Ki分别为1.8 nM/2.1 nM/1.6 nM/1.9 nM和16 nM，对Vps34，AKT，PDK1，p70S6K，MEK，ERK，p38和JNK几乎无活性。
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GDC-0941是一种有效的PI3Kα/δ抑制剂，IC50为3 nM，比对p110β(10倍)和p110γ的作用强25倍。
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LY294002是第一个人工合成的PI3Kα/δ/β的抑制剂，IC50分别为0.5 μM/0.57 μM/0.97 μM，也能够抑制自噬体的形成。
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