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R 59022

Chemical Structure : R 59022

CAS No.: 93076-89-2

R 59022 (R 59-022;R59022)

Catalog No.: PC-70274Not For Human Use, Lab Use Only.

R 59022 is a small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.

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Biological Activity

R 59022 is a small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.
R 59022 concomitantly stimulates PKC activity, selectively suppresses U46619-induced enhancement of mouse portal vein contraction under high glucose conditions.
R 59022 also induces caspase-mediated apoptosis in glioblastoma cells and in other cancers, but lacks toxicity in noncancerous cells.

Physicochemical Properties

M.Wt 459.58
Formula C27H26FN3OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-[2-[4-[(4-Fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one

References

1. Dominguez CL, et al. Cancer Discov. 2013 Jul;3(7):782-97.

2. de Chaffoy de Courcelles DC, et al. J Biol Chem. 1985 Dec 15;260(29):15762-70.

3. Nunn DL, et al. Biochem J. 1987 May 1;243(3):809-13.

4. Nobe K, et al. Br J Pharmacol. 2004 Sep;143(1):166-78.

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