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| | DIACYLGLYCEROL KINASE INHIBITOR II Basic information |
| Product Name: | DIACYLGLYCEROL KINASE INHIBITOR II | | Synonyms: | DIACYLGLYCEROL KINASE INHIBITOR I (R59 949);DIACYLGLYCEROL KINASE INHIBITOR II;R59949, 3-[2-[4-(bis(4-Fluorophenyl)methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone;3-[2-[4-Bis(4-fluorophenyl)methylenepiperidino]ethyl]-2,3-dihydro-2-thioxoquinazolin-4(1H)-one;3-[2-[4-(bis(4-Fluorophenyl)Methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone, R59949;DAG Kinase Inhibitor II;DAG Kinase Inhibitor;3-[2-(4-[BIS(4-FLUOROPHENYL)-METHYLENE)-1-PIPERIDINYL)ETHYL]-2,3-DIHYDRO-2-THIOXO-4[1H]-QUINAZOLINONE | | CAS: | 120166-69-0 | | MF: | C28H25F2N3OS | | MW: | 489.58 | | EINECS: | | | Product Categories: | quinazolinone | | Mol File: | 120166-69-0.mol |  |
| | DIACYLGLYCEROL KINASE INHIBITOR II Chemical Properties |
| Melting point | 228-230 °C | | Boiling point | 637.1±65.0 °C(Predicted) | | density | 1.36±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | 0.1 M HCl: slightly soluble | | form | solid | | pka | 11.24±0.20(Predicted) | | color | pale yellow |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 |
| | DIACYLGLYCEROL KINASE INHIBITOR II Usage And Synthesis |
| Description | 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. | | Uses | Diacylglycerol Kinase Inhibitor II has been used to determine tumor-induced inhibition with genetically modified cytotoxic T cells expressing chimeric antigen receptors (CAR). It has also been used to induce pAkt and PKR-like extracellular signal-regulated kinase (pErk) signals in T-cell acute lymphoblastic leukemia (T-ALL) cells. | | Definition | ChEBI: 3-[2-[4-[bis(4-fluorophenyl)methylidene]-1-piperidinyl]ethyl]-2-sulfanylidene-1H-quinazolin-4-one is a diarylmethane. | | Biochem/physiol Actions | Diacylglycerol kinase inhibitor. Inhibits formation of [38P]1-Oleoyl-2-acetylglyceryl-3-phosphoric acid (OAPA) in red blood cell membranes: IC50 = 3.3 μM. |
| | DIACYLGLYCEROL KINASE INHIBITOR II Preparation Products And Raw materials |
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