Description
LY294002 is an inhibitor of PI3K that is used to sensitize cancer cells to other co-administered anticancer chemotherapeutics. In macrophages and monocytes, LY294002 inhibits NF-κB activity and decreases levels of p50 NF-κB; it also inhibits LPS-induced expression of IL-10. LY294002 prevents ruffled border formation in osteoclasts by altering the binding of acidic vacuoles with the intercellular membrane. Additionally, this compound inhibits DNA-dependent protein kinase (DPK) activity and prevents the formation of NO.
References
Avni D, Glucksam Y, Zor T. The phosphatidylinositol 3-kinase (PI3K) inhibitor LY294002 modulates cytokine expression in macrophages via p50 nuclear factor κB inhibition, in a PI3K-independent mechanism. Biochem Pharmacol. 2012 Jan 1;83(1):106-14. PMID: 22005520.
Salh B, Wagey R, Marotta A, et al. Activation of phosphatidylinositol 3-kinase, protein kinase B, and p70 S6 kinases in lipopolysaccharide-stimulated Raw 264.7 cells: differential effects of rapamycin, Ly294002, and wortmannin on nitric oxide production. J Immunol. 1998 Dec 15;161(12):6947-54. PMID: 9862729.
Nakamura I, Sasaki T, Tanaka S, et al. Phosphatidylinositol-3 kinase is involved in ruffled border formation in osteoclasts. J Cell Physiol. 1997 Aug;172(2):230-9. PMID: 9258344.
Rosenzweig KE, Youmell MB, Palayoor ST, et al. Radiosensitization of human tumor cells by the phosphatidylinositol3-kinase inhibitors wortmannin and LY294002 correlates with inhibition of DNA-dependent protein kinase and prolonged G2-M delay. Clin Cancer Res. 1997 Jul;3(7):1149-56. PMID: 9815794.
