Download Files:
R59949
$50 – $1,045
Products Details
Product Description
– R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol[1][2][3].
Web ID
– HY-108355
Storage Temperature
– -20°C (Powder, stored under nitrogen)
Shipping
– Blue Ice
Applications
– Cancer-Kinase/protease
Molecular Formula
– C28H25F2N3OS
References
– [1]de Chaffoy de Courcelles D, et al. 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 Biol Chem. 1989;264(6):3274-3285.|[2]Day P, et al. Inhibitors of DAG metabolism suppress CCR2 signalling in human monocytes. Br J Pharmacol. 2019;176(15):2736-2749.|[3]Shimomura T, et al. R59949, a diacylglycerol kinase inhibitor, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. Naunyn Schmiedebergs Arch Pharmacol. 2017;390(2):207-214.|[4]Meinhardt G, et al. Effect of novel modulators of protein kinase C activity upon chemotherapy-induced differentiation and apoptosis in myeloid leukemic cells. Anticancer Drugs. 2002;13(7):725-733.
CAS Number
– 120166-69-0
Molecular Weight
– 489.58
Compound Purity
– 99.08
SMILES
– O=C1N(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)C(NC5=C1C=CC=C5)=S
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 100 mg/mL (ultrasonic)
Target
– PKC
Pathway
– Epigenetics;TGF-beta/Smad
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
