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DIACYLGLYCEROL KINASE INHIBITOR II manufacturers
- R59949
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- $35.00
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2026-07-15
- CAS:120166-69-0
- Purity: 98.82%
- Supply Ability: 10g
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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 | | biological source | synthetic (organic) | | InChI | 1S/C28H25F2N3OS/c29-22-9-5-19(6-10-22)26(20-7-11-23(30)12-8-20)21-13-15-32(16-14-21)17-18-33-27(34)24-3-1-2-4-25(24)31-28(33)35/h1-12H,13-18H2,(H,31,35) | | InChIKey | ZCNBZFRECRPCKU-UHFFFAOYSA-N | | SMILES | Fc1ccc(cc1)\C(=C2\CCN(CCN3C(=S)Nc4ccccc4C3=O)CC2)c5ccc(F)cc5 |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | 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. | | References | [1] D DE CHAFFOY DE COURCELLES. The role of endogenously formed diacylglycerol in the propagation and termination of platelet activation. A biochemical and functional analysis using the novel diacylglycerol kinase inhibitor, R 59 949.[J]. The Journal of Biological Chemistry, 1989, 264 6: 3274-3285.
[2] X. DU. Fatty acids inhibit growth-factor-induced diacylglycerol kinase alpha activation in vascular smooth-muscle cells.[J]. The Ukrainian Biochemical Journal, 2001, 1 1: 275-282. DOI: 10.1042/bj3570275
[3] YUKIKO KUROHANE KANEKO. Depression of type I diacylglycerol kinases in pancreatic β-cells from male mice results in impaired insulin secretion.[J]. Endocrinology, 2013, 154 11: 4089-4098. DOI: 10.1210/en.2013-1356
[4] LU YANG. Diacylglycerol Kinase (DGK) Inhibitor II (R59949) Could Suppress Retinal Neovascularization and Protect Retinal Astrocytes in an Oxygen-Induced Retinopathy Model[J]. Journal of Molecular Neuroscience, 2014, 56 1: 78-88. DOI: 10.1007/s12031-014-0469-2 |
| | DIACYLGLYCEROL KINASE INHIBITOR II Preparation Products And Raw materials |
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