DIACYLGLYCEROL KINASE INHIBITOR II
Synonym(s):3-[2-[4-(bis(4-Fluorophenyl)methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone;Diacylglycerol Kinase Inhibitor II - CAS 120166-69-0 - Calbiochem;R59949;R59949, 3-{2-[4-[ bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II;R59949, 3-{2-[4-[bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II
- CAS NO.:120166-69-0
- Empirical Formula: C28H25F2N3OS
- Molecular Weight: 489.58
- MDL number: MFCD00069258
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-18 21:14:07
What is DIACYLGLYCEROL KINASE INHIBITOR II?
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.
The Uses of DIACYLGLYCEROL KINASE INHIBITOR II
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.
What are the applications of Application
DAG Kinase Inhibitor II is an inhibitor of DGK
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.
Properties of DIACYLGLYCEROL KINASE INHIBITOR II
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 |
Safety information for DIACYLGLYCEROL KINASE INHIBITOR II
Computed Descriptors for DIACYLGLYCEROL KINASE INHIBITOR II
New Products
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