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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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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CAL-101 (Idelalisib, GS-1101) 是p110δ选择性抑制剂，IC50为2.5 nM，比对p110α/β/γ的抑制性高40到300倍，比对C2β，hVPS34，DNA-PK和mTOR的抑制。
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NVP-BKM120(BKM120)是PI3K抑制剂，对于p110α、β、δ、γ的IC50分别为52 nM、166 nM、116 nM、262 nM。而对于VPS34、mTOR、DNAPK则抑制性较小，对于PI4Kβ则几乎无抑制性。
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