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 |
Echelon-脂类研究的最佳拍档
Echelon是脂质研究和脂质与蛋白质相互作用研究领域的引导者。脂质蛋白相互作用是众多的细胞信号通路钟高级调控必不可少的。异常的细胞信号通路将会导致许多疾病,例如癌症、炎症、糖尿病和心血管疾病等。Echelon一直是脂质研究信息,脂质信号分析的顶级供应商。