CU-3是(5Z,2E)-CU-3的消旋体。(5Z,2E)-CU-3是一种有效的选择性抗DGKα同工酶抑制剂，IC50值为0.6μM，竞争性抑制DGKα对ATP的亲和力，Km值为0.48mM。(5Z,2E)-CU-3靶向DGKα催化区域，但不靶向调节区域。(5Z,2E)-CU-3具有抗肿瘤和免疫原性作用，增强癌细胞的凋亡和T细胞的活化。
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells[1].
[1]. Liu K, et al. A novel diacylglycerol kinase α-selective inhibitor, CU-3, induces cancer cell apoptosis and enhances immune response. J Lipid Res. 2016 Mar;57(3):368-79.
动态评分
0.0