(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。
| Cas No. | 1815598-71-0 |
| Canonical SMILES | O=S(C1=CC=CC=C1)(NN(C/2=O)C(SC2=C/C=C/C3=CC=CO3)=S)=O |
| 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℃); Water:< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | (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. |
