PF-543 (PF543, Sphingosine Kinase 1 Inhibitor II)是一种可逆的SPHK1选择性抑制剂，IC₅₀为2 nM，K_i为3.6 nM，选择性是SPHK2的100倍以上，与鞘氨醇具有竞争性，但不具有ATP竞争性。PF-543还可以抑制内源性1-磷酸鞘氨醇(S1P)水平，S1P可以由SPHK1磷酸化鞘氨醇得到。此外，PF-543能促进LC3累积，诱导LC3-I向LC3-II的转化，提高自噬水平。

参考文献

[1].Schnute ME, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88.

[2].MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55.

[3].Hamada M, et al. Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells. Cell Death Discov. 2017 Aug 14;3:17047.

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