R-59-949 (Synonyms: Diacylglycerol Kinase Inhibitor II, DKGI-II) |
| Catalog No.GC18246 |
R-59-949는 IC50이 300nM인 판 디아실글리세롤 키나제(DGK) 억제제입니다. R-59-949는 유형 I DGK α 및 γ의 활성을 강력하게 억제하고 유형 II DGK θ 및 κ의 활성을 적당히 약화시킵니다. R-59-949는 내인성 리간드 디아실 글리세롤의 수준을 향상시켜 단백질 키나제 C(PKC)를 활성화합니다.
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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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