PF-543 (hydro<wbr/>chloride)

PF-543 (hydrochloride)

CAT N°: 17034
Price:

From 48.00 40.80

PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).{27977} It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.{27978}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 1-[[4-[[3-methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2R-pyrrolidinemethanol, monohydrochloride
  • Correlated keywords
    • 1415562-82-1 1415562-83-2 biochemical inhibitor kinase protein signal transduction intracellular signaling cancer vascular disease inhibit inhibition PF543 PF 543 SK1 SK2 sphingosine lipid receptor phosphorylation cell blood sickle sickling hemolysis inflammation
  • Product Overview:
    PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).{27977} It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.{27978}

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