| Bioactivity | R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4]. | |||||||||
| Invitro | R 59-022 (10 μM，1 分钟) 增强血小板聚集[2]。R 59-022 (30 uM，0-60 分钟) 增加嗜铬细胞中去甲肾上腺素的释放[3]。R 59-022 (40 uM，30 分钟) 激活 HeLa 和 U87 细胞中的 PKC[4]。R 59-022 (0-10 uM，4 小时) 阻断 EBOV 进入 Vero 细胞[5]。 Western Blot Analysis[4] Cell Line: | |||||||||
| In Vivo | R 59-022 (2 mg/kg，腹腔注射，12 天) 显着增加植入 U87 GBM 细胞的 SCID 小鼠的中位生存期[6]。 Animal Model: | |||||||||
| Name | R 59-022 | |||||||||
| CAS | 93076-89-2 | |||||||||
| Formula | C27H26FN3OS | |||||||||
| Molar Mass | 459.58 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
|
|||||||||
| Reference | [1]. de Chaffoy de Courcelles DC, et al. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. J Biol Chem. 1985 Dec 15;260(29):15762-70. [2]. Nunn DL, et al. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem J. 1987 May 1;243(3):809-13. [3]. Jones JA, et al. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenalinerelease and phosphoinositide hydrolysis in chromaffin cells. Br J Pharmacol. 1990 Nov;101(3):521-6. [4]. Boroda S, et al. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017 Jan 1;123:29-39. [5]. Stewart CM, et al. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells. Viruses. 2019 Mar 1;11(3). pii: E206. [6]. Dominguez CL, et al. Diacylglycerol kinase α is a critical signaling node and novel therapeutic target in glioblastoma and other cancers. Cancer Discov. 2013 Jul;3(7):782-97. |