R 59-022

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Cat.No. 2194 - R 59-022 | C27H26FN3OS | CAS No. 93076-89-2
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)
Datasheet
Citations (1)
Literature

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(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.

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

Safety Datasheet

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


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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

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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