(5Z,2E)-CU-3 |
| カタログ番号GC60397 |
(5Z,2E)-CU-3 は、0.6 μM の IC50 値を持つ DGK の α アイソザイムに対する強力かつ選択的な阻害剤であり、0.48 mM の Km 値を持つ ATP に対する DGKα の親和性を競合的に阻害します。 (5Z,2E)-CU-3 は触媒領域を標的としますが、DGKα の調節領域は標的としません。 (5Z,2E)-CU-3 は、抗腫瘍効果と免疫促進効果があり、がん細胞のアポトーシスと T 細胞の活性化を促進します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1815598-71-0
Sample solution is provided at 25 µL, 10mM.
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(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.
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