R-59-022

R-59-022

CAT N°: 16772
Price:

From 55.00 46.75

Diacylglycerol (DAG) kinases (DGKs) phosphorylate DAG to give phosphatidic acid (PA), reducing signaling through DAG and increasing signaling through PA.{7274} R-59-022 is an inhibitor of DGK (IC50 = 2.8 µM).{27715} This results in increased DAG-dependent PKC activity and potentiates aggregation of thrombin-stimulated platelets.{27715,27713} R-59-022 also blocks vascular contraction induced by the thromboxane analog U-46619 (Item No. 16450).{27712} At 10 µM, R-59-022 induces apoptosis in glioblastoma cells without being toxic to non-cancerous cells.{27710} It inhibits DGK-? in vitro at concentrations below 1 µM and blocks DGK-? activity in vivo.{27714} R-59-022 also inhibits A. thaliana DGK2 (IC50 = 50 µM) and suppresses root growth but does not affect DGK7 at 50 µM.{27711}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 6-[2-[4-[(4-fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
  • Correlated keywords
    • 93076-98-3 biochemical inhibitor kinase cancer intracellular signaling diacylglycerol DAG-dependent DKG inhibit R59022 PKC activity aggregation thrombin-stimulated platelet block vascular contraction thromboxane TX analog U-46619 U46619 apoptosis programmed cell death glioblastoma DGK-? in vitro vivo Arabidopsis thaliana DGK2 suppress root growth DKGI-I DKGII
  • Product Overview:
    Diacylglycerol (DAG) kinases (DGKs) phosphorylate DAG to give phosphatidic acid (PA), reducing signaling through DAG and increasing signaling through PA.{7274} R-59-022 is an inhibitor of DGK (IC50 = 2.8 µM).{27715} This results in increased DAG-dependent PKC activity and potentiates aggregation of thrombin-stimulated platelets.{27715,27713} R-59-022 also blocks vascular contraction induced by the thromboxane analog U-46619 (Item No. 16450).{27712} At 10 µM, R-59-022 induces apoptosis in glioblastoma cells without being toxic to non-cancerous cells.{27710} It inhibits DGK-? in vitro at concentrations below 1 µM and blocks DGK-? activity in vivo.{27714} R-59-022 also inhibits A. thaliana DGK2 (IC50 = 50 µM) and suppresses root growth but does not affect DGK7 at 50 µM.{27711}

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