PF-543 478 RI-1 is an irreversible inhibitor
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PF-543 478 RI-1 is an irreversible inhibitorPF 543 is a novel selective SK 1 inhibitor which inhibited SK 1 activity in a competitive manner with sphingosine. PF 543 inhibits SphK1 with a K(i) of 3. 6 nM, is sphingosine competitive and is more than 100 fold selective for SphK1 over the SphK2 isoform. PF 543 was effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. PF 543 is the most
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