Date published: 2025-9-19

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R 59-022 (CAS 93076-89-2)

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Alternate Names:
Diacylglycerol Kinase Inhibitor I
Application:
R 59-022 is an inhibitor of DGK and serotonin
CAS Number:
93076-89-2
Purity:
≥98%
Molecular Weight:
459.58
Molecular Formula:
C27H26FN3OS
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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R 59-022 potentiates the activity of protein kinase C by inhibiting diacylglycerol metabolism. R 59-022 inhibits DGK (diacylglycerol kinase, IC50 = 2.8 muM) without affecting phosphodiesterase or phosphatidylinositol kinase. R 59-022 is a weak dopamine D2 and histamine H1 antagonist and strong serotonin S2 antagonist.


R 59-022 (CAS 93076-89-2) References

  1. Phosphatidic acid accumulation and catecholamine release in adrenal chromaffin cells: stimulation by high potassium and by nicotine, and effect of a diacylglycerol kinase inhibitor R 59 022.  |  Owen, PJ., et al. 1991. J Neurochem. 57: 769-74. PMID: 1861148
  2. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenaline release and phosphoinositide hydrolysis in chromaffin cells.  |  Jones, JA., et al. 1990. Br J Pharmacol. 101: 521-6. PMID: 1963797
  3. PKC and Pi deprivation modulate differently the ubiquitous Na-dependent Pi uptake in MDCK cells.  |  Escoubet, B., et al. 1991. Am J Physiol. 260: F235-42. PMID: 1996673
  4. Induction of gene expression by IL-1 in NIH 3T3 cells. Possible requirement of protein kinase C activity and independence from arachidonic acid metabolism.  |  Donati, D., et al. 1990. J Immunol. 145: 4115-20. PMID: 2124235
  5. Antagonism by the diacylglycerol kinase inhibitor R59 022 of muscarinic receptor-mediated cyclic GMP formation and binding of [3H]N-methylscopolamine.  |  Lai, WS. and el-Fakahany, EE. 1990. Biochem Pharmacol. 39: 221-2. PMID: 2153379
  6. Regulation of oxytocin secretion by the ovine corpus luteum: effect of activators of protein kinase C.  |  Hirst, JJ., et al. 1990. J Endocrinol. 124: 225-32. PMID: 2155985
  7. A diacylglycerol kinase inhibitor, R 59 022, potentiates superoxide anion production and 46-kDa protein phosphorylation in guinea pig polymorphonuclear leukocytes.  |  Ohtsuka, T., et al. 1990. J Biol Chem. 265: 15418-23. PMID: 2168412
  8. The actions of inhibitors of diacylglycerol kinase and diacylglycerol lipase on histamine release from rat peritoneal mast cells.  |  Cantwell, ME. and Foreman, JC. 1987. Br J Pharmacol. 92: 597-601. PMID: 2447987
  9. [3H]phosphatidic acid formed in response to FMLP is not inhibited by R59 022, a diacylglycerol kinase inhibitor.  |  Mahadevappa, VG. 1988. Biochem Biophys Res Commun. 153: 1097-104. PMID: 2839168
  10. The inhibition of arachidonic acid mobilization in human platelets by R59 022, a diacylglycerol kinase inhibitor.  |  Mahadevappa, VG. and Sicilia, FJ. 1988. Biochim Biophys Acta. 961: 309-15. PMID: 2840967
  11. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet.  |  de Chaffoy de Courcelles, DC., et al. 1985. J Biol Chem. 260: 15762-70. PMID: 2999135
  12. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells.  |  Stewart, CM., et al. 2019. Viruses. 11: PMID: 30832223
  13. Relationship among cellular diacylglycerol, sphingosine formation, protein kinase C activity, and parathyroid hormone secretion from dispersed bovine parathyroid cells.  |  McKay, C. and Miller, A. 1996. Endocrinology. 137: 2473-9. PMID: 8641201

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

R 59-022, 5 mg

sc-203227
5 mg
$122.00