| Description | R 59-022 hydrochloride (DKGI-I hydrochloride) is a 5-HT Receptor antagonist that activates protein kinase C (PKC).R 59-022 hydrochloride is a DGK inhibitor (IC50:2.8 µM) that inhibits the phosphorylation of OAG to OAPA.R 59-022 enhances thrombin-induced triglyceride production in platelets and inhibits the production of phosphatidic acid in neutrophils. R 59-022 enhances thrombin-induced diglyceride production in platelets and inhibits phosphatidic acid production in neutrophils. |
| In vitro | R 59-022 (10 μM; 1 min) Hydrochloride enhances platelet aggregation.[1]R 59-022 (30 μM; 0-60 min) Hydrochloride increases the release of norepinephrine in chromaffin cells.[2]R 59-022 (40 μM; 30 min) Hydrochloride activates PKC in HeLa and U87 cells.[3]R 59-022 (0-10 μM; 4 h) Hydrochloride blocks the entry of EBOV GP into Vero cells.[4] |
| In vivo | R 59-022 (2 mg/kg; i.p.; 12 days) significantly increased the median survival of SCID mice implanted with U87 GBM cells.[6] |
| Target activity | DGK:2.8 µM |
| Synonyms | DKGI-I hydrochloride, Diacylglycerol kinase inhibitor I hydrochloride, DKGI-I hydrochloride ; Diacylglycerol kinase inhibitor I hydrochloride |
| molecular weight | 496.04 |
| Molecular formula | C27H27ClFN3OS |
| CAS | 93076-98-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (110.88 mM) |
| References | 1. Nunn DL, et al. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem J. 1987;243(3):809-813. 2. Jones JA, et al. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenaline release and phosphoinositide hydrolysis in chromaffin cells. Br J Pharmacol. 1990;101(3):521-526. 3. Boroda S, et al. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017;123:29-39. 4. Stewart CM, et al. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells. Viruses. 2019;11(3):206. 5. 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;260(29):15762-15770. 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;3(7):782-797. |