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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TGX-221, a novel, potent, isoform-specific, and cell-permeable small molecule inhibitor of PI3Kβ, is critical for cell growth, proliferation, and tumorigenesis of PTEN-deficient tumor cells. TGX-221是可通透细胞的PI3K p110β选择性抑制剂。
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A66
EY0337
A66是一种有效的，特异性的p110α抑制剂，IC50为32 nM，作用于p110α比作用于其他I型PI3K亚型选择性高100倍以上。
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HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
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Voxtalisib (SAR245409, XL765) Analogue是作用于mTOR/PI3K的双重抑制剂，对p110γ作用最强，IC50为9 nM；也可抑制DNA-PK和mTOR。
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TG100713是一种pan-PI3K抑制剂，作用于PI3Kγ， PI3Kδ， PI3Kα和PI3Kβ，IC50分别为50 nM， 24 nM， 165 nM和215 nM。
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