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.
Compound Libraries
R 59-022 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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(CCN2CCC(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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 22.98 | 50 | |
| ethanol | 9.19 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 459.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.18 mL | 10.88 mL | 21.76 mL |
| 5 mM | 0.44 mL | 2.18 mL | 4.35 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.18 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: R 59-022, supplier, Diacylglycerol, kinase, inhibitors, inhibits, increases, PKC, activity, DGK, DAG, Kinase, Kinases, Lipid, Metabolism, R59022, Diacylglycerol, Kinase, Diacylglycerol, Kinase, Tocris Bioscience
