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HomeProduct name listDIACYLGLYCEROL KINASE INHIBITOR II

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

DIACYLGLYCEROL KINASE INHIBITOR II Structural

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

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