(5Z,2E)-CU-3 is an inhibitor of diacylglycerol kinase α (DGK-α; IC50 = 0.6 ?M for the porcine enzyme).1 It is selective for DGK-α over other type I DGKs, as well as type II, type III, type IV, and type V DGKs (IC50s = 7-36 ?M). (5Z,2E)-CU-3 (5 ?M) induces apoptosis in HeLa cervical and HepG2 liver cancer cells and enhances increases in IL2 mRNA expression in Jurkat T cells induced with concanavalin A .
1.Liu, K., Kunii, N., Sakuma, M., et al.A novel diacylglycerol kinase α-selective inhibitor, CU-3, induces cancer cell apoptosis and enhances immune responseJ. Lipid Res.57(3)368-379(2016)