Identification | Back Directory | [Name]
DIACYLGLYCEROL KINASE INHIBITOR II | [CAS]
120166-69-0 | [Synonyms]
R59949 DAG Kinase Inhibitor DAG Kinase Inhibitor II DIACYLGLYCEROL KINASE INHIBITOR II Diacylglycerol Kinase Inhibitor II solid DIACYLGLYCEROL KINASE INHIBITOR I (R59 949) DIACYLGLYCEROL KINASE INHIBITOR II (R 59 949) Diacylglycerol Kinase Inhibitor II - CAS 120166-69-0 - Calbiochem 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 3-[2-(4-[BIS(4-FLUOROPHENYL)-METHYLENE)-1-PIPERIDINYL)ETHYL]-2,3-DIHYDRO-2-THIOXO-4[1H]-QUINAZOLINONE 4(1H)-Quinazolinone, 3-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo- 3-[2-[4-(bis(4-Fluorophenyl)Methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone, R59949 R59949, 3-[2-[4-(bis(4-Fluorophenyl)methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone | [Molecular Formula]
C28H25F2N3OS | [MDL Number]
MFCD00069258 | [MOL File]
120166-69-0.mol | [Molecular Weight]
489.58 |
Chemical Properties | Back Directory | [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 Information | Back Directory | [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. |
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