R59949

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].

Product Specifications

CAS Number

[120166-69-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

PKC

Type

Reference compound

Related Pathways

Epigenetics; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/r59949.html

Concentration

10mM

Purity

99.08

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C28H25F2N3OS

Molecular Weight

489.58

Precautions

H302, H315, H319

References & Citations

[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.