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)

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

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(120166-69-0)Related Product Information

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• N-(2-Aminoethyl)piperidine
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• 4,4'-Difluorodiphenylmethane
• 1-Fluoro-4-(1-methylethenyl)benzene
• 1-BENZOYL-2-THIOUREA
• 4-(DIPHENYLMETHYLENE)PIPERIDINE
• 1-Methyl-4-methylene-piperidine
• 3-ETHYL-2-THIOXO-1,2,3,4-TETRAHYDROQUINAZOLIN-4-ONE
• 2-AMINO-N,N-DIMETHYL-BENZAMIDE
• N-ETHYL-2-PIPERIDIN-1-YLETHANAMINE
• N-BENZYL-N-METHYLTHIOUREA
• METHYL-(2-PIPERIDIN-1-YL-ETHYL)-AMINE
• N,N-DIETHYLTHIOUREA
• 1-(2-PIPERIDINOETHYL)-2-THIOUREA
• 1,1-BIS(4-FLUOROPHENYL)-1-BUTENE
• DIACYLGLYCEROL KINASE INHIBITOR II
• N-METHYL-N-(2-METHYLAMINO-ETHYL)-BENZAMIDE