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.
-
PIK-90是PI3Kα，γ和δ抑制剂，IC50分别为11 nM，18 nM和58 nM，对PI3Kβ的IC50为350 nM。
More
-
VS-5584是PI3K/mTOR双重抑制剂，对mTOR和PI3Kα/β/δ/γ的IC50分别为3.4 nM和2.6-21 nM。
More
-
AZD6482是一种PI3Kβ抑制剂，IC50为10 nM，作用于PI3Kβ比作用于PI3Kδ， PI3Kα和PI3Kγ选择性分别高8，87和109倍。
More
-
GSK2126458是PI3K抑制剂，对p110α，β，δ，γ，mTORC1和mTORC2的IC50分别为0.019 nM，0.13 nM，0.024 nM，0.06 nM，0.18 nM和0.3 nM。
More
-
AS-252424是PI3Kγ抑制剂，IC50为33 nM，比对PI3Kα的抑制性高10倍以上。
More
