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Submit ReviewR 59-022
Description: Diacylglycerol kinase inhibitor; increases PKC activity
Chemical Name: 6-[2-[4-[(4-Fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
Purity: ≥98% (HPLC)
Biological Activity for R 59-022
R 59-022 is a 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 for R 59-022
| M. Wt | 459.58 |
| Formula | C27H26FN3OS |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 93076-89-2 |
| PubChem ID | 3012 |
| InChI Key | MFVJXLPANKSLLD-UHFFFAOYSA-N |
| Smiles | CC1=C(CCN2CC\C(CC2)=C(/C2=CC=CC=C2)C2=CC=C(F)C=C2)C(=O)N2C=CSC2=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for R 59-022
References for R 59-022
References are publications that support the biological activity of the product.
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
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
Boonen et al (1993) Neutrophil chemotaxis induced by the diacylglycerol kinase inhibitor R59022. Biochim.Biophys.Acta 1178 97 PMID: 8392381
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
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Keywords: R 59-022, R 59-022 supplier, Diacylglycerol, kinase, inhibitors, inhibits, increases, PKC, activity, DGK, DAG, Kinase, Kinases, Lipid, Metabolism, R59022, 2194, Tocris Bioscience
1 Citation for R 59-022
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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