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R-59949

Chemical Structure : R-59949

CAS No.: 120166-69-0

R-59949 (R59949;R 59949)

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

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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets; 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; 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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