Purity: > 98%
|Cas No:||1706522-79-3 (HCl)|
PF-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 potent inhibitor of SphK1 described to date and it will be useful for dissecting specific roles of SphK1-driven S1P signalling.
1: Lynch KR. Building a better sphingosine kinase-1 inhibitor. Biochem J. 2012 May 15;444(1):e1-2. doi: 10.1042/BJ20120567. PubMed PMID: 22533672.