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R59949

Chemical Structure : R59949

CAS No.: 120166-69-0

R59949 (R-59949)

Catalog No.: PC-70275Not For Human Use, Lab Use Only.

R59949 is a small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.

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Biological Activity

R59949 is a small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.
R59949 markedly increases PKC activity in platelets stimulated with vasopressin, produces partial inhibition of formation of phosphatidic acid in human platelets challenged with thrombin, DC8 or OAG.
R59949 also induces caspase-mediated apoptosis in glioblastoma cells and in other cancers, but lacks toxicity in noncancerous cells.

Physicochemical Properties

M.Wt 489.585
Formula C28H25F2N3OS
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

3-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-2-sulfanylidene-1H-quinazolin-4-one

References

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

2. de Chaffoy de Courcelles D, et al. J Biol Chem. 1989 Feb 25;264(6):3274-85.

3. Rodríguez-Liñares B, et al. Biochem Pharmacol. 1991 Mar 1;41(5):835-8.

4. Jiang Y, et al. Biochem Pharmacol. 2000 Apr 1;59(7):763-72.

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