LY294002是一种有效的、细胞通透性的、选择性的和可逆的I类磷酸肌醇3-激酶（PI3Ks）抑制剂，作用于p110α，p110β和p110δ催化亚基的ATP结合位点[1, 2]。

PI3K家族分为3类：I类、II类和III类。LY294002可以抑制I类PI3K 4个催化亚基中的3个，分别为p110α、β和δ，IC50值分别为500 nM、973 nM和570 nM[3]。尽管LY294002比wortmannin（另一个PI3K抑制剂）的效力低，但是LY294002在溶液中更加稳定。而且，LY294002是一种可逆抑制剂，而wortmannin是不可逆的[2]。

PI3Ks通过Akt激活mTOR，抑制Bad，诱导细胞生长和增殖。在体外和体内，LY294002有效的抑制I类PI3K的催化亚基，诱导细胞凋亡，抑制肿瘤细胞的生长[2, 4]。LY294002也是一种有效的自体吞噬抑制剂，阻断自噬体的形成[5]。定量化学蛋白质组学分析表明，LY294002抑制BET bromodomain蛋白BRD2、BRD3和BRD4，IC50范围介于1-2 μM之间[6]。

参考文献：
[1]Maira et al.  (2009). PI3K inhibitors for cancer treatment: where do we stand?. doi:10.1042/BST0370265.
[2]Vlahos CJ. , et al. (1994). A Specific Inhibitor of Phosphatidylinositol 3-Kinase, 2-(4-Morpholinyl)-8-phenyl-4H-l-benzopyran-4-one (LY294002). Journal of Biological Chemistry 269 (7): 5241–5248.
[3]Chaussade C, et al.  Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J, 2007, 404(3), 449-58.
[4]Hu L, et al.  In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY294002). Clin Cancer Res, 2000, 6(3), 880-6.
[5]Blommaart EF. , et al., (1997). The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. Eur. J. Biochem. 243: 240–246.
[6]Dittmann, A. , et al. (2013). The Commonly Used PI3-Kinase Probe LY294002 is an Inhibitor of BET Bromodomains. ACS Chemical Biology: 131210150813004.