R 59-022

Cat. No. 2194

R 59-022 C27H26FN3OS [93076-89-2]

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

Biological Activity

Diacylglycerol (DAG) kinase inhibitor (IC50 = 2.8 μM); increases protein kinase C activity. Potentiates thrombin-induced platelet aggregation and induces neutrophil chemotaxis. Inhibits U46619-induced contractions in mouse aorta and porcine coronary artery.

Technical Data

M.Wt:
459.58
Formula:
C27H26FN3OS
Solubility:
Soluble to 20 mM in ethanol and to 50 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
93076-89-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Nobe et al (2004) Novel diacylglycerol kinase inhibitor selectively suppressed an U46619-induced enhancement of mouse portal vein contraction under high glucose conditions. Br.J.Pharmacol. 143 166. PMID: 15289283.

Boonen et al (1993) Neutrophil chemotaxis induced by the diacylglycerol kinase inhibitor R59022. Biochim.Biophys.Acta 1178 97. PMID: 8392381.

Nunn and Watson (1987) A diacylglyerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem.J. 243 809. PMID: 2821994.

de Chaffoy de Courcelles et al (1985) R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. J.Biol.Chem. 260 15762. PMID: 2999135.

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Citations are publications that use Tocris products. Selected citations for R 59-022 include:

Conley et al (2015) Evaluation of AaDOP2 receptor antagonists reveals antidepressants and antipsychotics as novel lead molecules for control of the yellow fever mosquito, Aedes aegypti. Nature 352 53. PMID: 25332454.

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Keywords: R 59-022, supplier, Diacylglycerol, kinase, inhibitors, inhibits, increases, PKC, activity, DGK, DAG, Kinase, Kinases, Lipid, Metabolism, R59022, Tocris Bioscience, Diacylglycerol Kinase Inhibitor products

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