(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。
货号:ajcx29800
CAS:1815598-71-0
分子式:C16H12N2O4S3
分子量：392.47
溶解度:DMSO: 20 mg/mL (50.96 mM; ultrasonic and warming and heat to 60°C); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(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.