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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GSK2636771是一种口服生物有效的PI3Kβ选择性抑制剂，对PTEN缺失细胞系敏感。
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GDC-0980 (RG7422)是I型PI3K抑制剂，对PI3Kα，β，δ和γ的IC50分别为5 nM，27 nM，7 nM和14 nM，对mTOR的Ki为17 nM。
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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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