R-59-949 (Synonyms: Diacylglycerol Kinase Inhibitor II, DKGI-II) |
| Katalog-Nr.GC18246 |
R-59-949 ist ein Pan-Diacylglycerolkinase (DGK)-Inhibitor mit einem IC50 von 300 nM. R-59-949 hemmt stark die Aktivität von Typ I DGK α und γ und schwächt die Aktivität von Typ II DGK θ und κ moderat ab. R-59-949 aktiviert die Proteinkinase C (PKC), indem es die Spiegel des endogenen Liganden Diacylglycerin erhöht.
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Cas No.: 120166-69-0
Sample solution is provided at 25 µL, 10mM.
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R-59-949 is an inhibitor of diacylglycerol kinase α (DGK-α) with an IC50 value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate. DGK-α inhibition with R-59-949 increases diacylglycerol-dependent PKC activity, serotonin secretion, and aggregation of thrombin-stimulated platelets. R-59-949 inhibits DGK-α activity induced by platelet-derived growth factor (PDGF) in intact vascular smooth muscle cells (VSMCs). It inhibits high K+- and glucose-induced insulin secretion in MIN6 pancreatic β-cells in a dose-dependent manner. In vivo, administration of R-59-949 prevents retinal neovascularization in a mouse model of oxygen-induced retinopathy.
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