PF-543 is a potent inhibitor of sphingosine kinase 1 (SK1; IC50 = 2-3.6 nM) that less effectively inhibits SK2 (IC50 = 356 nM).(1) It does not significantly block the activity of other protein and lipid kinases, or bind sphingosine-1-phosphate receptors, when tested at a concentration of 10 μM.1 PF-543 prevents the phosphorylation of sphingosine in cancer cells and in whole blood (EC50 = 8.4 and 27 nM, respectively).1 Through its effects on SK1, PF-543 prevents sickling, hemolysis, and inflammation in sickling cell disease transgenic mice.(2) Unlike inhibitors that are selective for SK2, PF-543 does not impair DNA synthesis in human pulmonary arterial smooth muscle cells.(3)
| Categories | Biochemical Reagents |
|---|
| Filter | Inhibitor, Sphingolipid |
|---|
| CAS Number | 1415562-82-1 (free base) |
|---|
| Molecular Formula | C27H32ClNO4S |
|---|
| Molecular Weight (g/mol) | 502.07 |
|---|
| Purity | >98% |
|---|
| Storage | -20 °C or below |
|---|
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