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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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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BYL719是一种有效的，选择性的PI3Kα抑制剂，IC50为5 nM，对PI3Kβ/γ/δ具有极弱的作用。
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3-Methyladenine是一种选择性PI3K抑制剂，抑制Vps34和PI3Kγ的IC50分别为25 μM和60 μM；永久性抑制I型PI3K，短暂的抑制III型PI3K。
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AS-605240选择性抑制PI3Kγ，IC50为8 nM，作用于PI3Kγ比作用于PI3Kδ/β和PI3Kα选择性分别高30和7.5倍以上。
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