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R59949

R59949, a diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. R59949 strongly inhibits type I DGK a and γ, and moderately attenuates type II DGK θ and κ.

R59949 Chemical Structure

R59949 Chemical Structure

CAS: 120166-69-0

Purity & Quality Control

Batch: E008201 DMSO] 98 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 99.24%
99.24

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Biological Activity

Description R59949, a diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. R59949 strongly inhibits type I DGK a and γ, and moderately attenuates type II DGK θ and κ.
Targets
DKG [1]
0.3 μM
In vitro
In vitro

R59949 is a pan diacylglycerol kinase (DGK) inhibitor, which inhibits inducible NO production through decreasing transplasmalemmal L-arginine uptake in rat aortic smooth muscle cells (RASMCs).[1]
Cell Research Cell lines rat aortic smooth muscle cells (RASMCs)
Concentrations 10 µM
Incubation Time 30 min
Method

RASMCs are prepared from adult male Wistar rats and cultured in DMEM containing 10% FBS under 5% CO2 at 37 ℃. Cultured cells showing a confluent condition in a 24-well plate are used for experiments. The cells are pretreated with R59949 at 10 μM or cycloheximide at 1 μM at 30 min before stimulation with IL-1β at 10 ng/ml or a vehicle for 24 h. Measurement of NOX is performed in the presence of nitrate reductase using a commercial kit. After incubation with nitrate reductase at room temperature for 2 h, aliquots of the culture medium are mixed with Griess reagent (1% sulphanilamide/0.1% N-(1-naphthyl) ethylenediamine dihydrochloride in 5% phosphoric acid). The mixture is then incubated at room temperature for 10 min, and its absorbance is measured at 540 nm using a photometer.
In Vivo
In vivo

R59949 upregulates the expression of PHD-2, also downregulates HIF-1α and vascular endothelial growth factor (VEGF) in the retina of oxygen-induced retinopathy (OIR) mice, suggesting a potential possibility that R59949 suppresses retinal neovascular pathophysiology via PHD2/HIF-1α/VEGF pathway.[2]
Animal Research Animal Models C57BL/6J mice
Dosages 10 μg/g/day
Administration i.p.

Chemical Information & Solubility

Molecular Weight 489.58 Formula

C28H25F2N3OS
CAS No. 120166-69-0 SDF --
Smiles FC1=CC=C(C=C1)C(=C2CCN(CCN3C(=S)NC4=CC=CC=C4C3=O)CC2)C5=CC=C(F)C=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 98 mg/mL ( (200.17 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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