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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CAY10505是AS-252424的羟基化合物，是一种PI3Kγ抑制剂，IC50为30 nM.
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PIK-93是第一个高活性PI4K (PI4KIIIβ)抑制剂，IC50为19 nM，还能抑制PI3Kα，IC50为39 nM。
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GSK1059615是可逆的PI3Kα/β/δ/γ和mTOR双重抑制剂，IC50为0.4 nM/0.6 nM/2 nM/5 nM和12 nM。
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PIK-75是一种p110α抑制剂，IC50为5.8 nM (比作用于p110β效果强200倍)，亚型特异性的突变体在Ser773，也有效抑制DNA-PK，IC50为2 nM。
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YM201636是一种选择性的PIKfyve抑制剂，IC50为33 nM，对p110α作用效果稍弱，对Fabl(酵母同源基因)不敏感。
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