PF-543 HCl
Sphingosine kinase-1 inhibitor / PF-543 (1706522-79-3) is a potent (IC50 = 2.0 nM) and selective (>100-fold over SphK2) reversible inhibitor of sphingosine kinase-1 (SphK1).1 It induced autophagy in head and neck squamous cell carcinoma cells.2 PF-543 mitigated pulmonary fibrosis via reducing lung epithelial cell mitochondrial DNA damage and monocyte recruitment.3 It also alleviated sepsis-induced lung injury in an acute ethanol intoxication model in mice.4 PF-543 inhibited cell cycle and tumor growth in a xenograft model of non-small cell lung cancer.5
Biochemicals & reagents
1706522-79-3
1 Schnute et al. (2012), Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1; Biochem. J. 444 79 2 Hamada et al. (2017); Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells, Cell Death Discov. 3 17047 3 Cheresh et al. (2020); The Sphingosine Kinase 1 Inhibitor, PF543, Mitigates Pulmonary Fibrosis by Reducing Lung Epithelial Cell mtDNA Damage and Recruitment of Fibrogenic Monocytes, Int. J. Mol. Sci. 21 5595 4 Chen et al. (2021); Blocking SphK1/S1P/S1PR1 Signaling Pathway Alleviates Lung Injury Caused by Sepsis in Acute Ethanol Intoxication in Mice, Inflammation 44 2170 5 Lin et al. (2022); Targeting SPHK1/PBX1 Axis Induced Cell Cycle Arrest in Non-Small Cell Lung Cancer, Int. J. Mol. Sci. 23 12741
-20°C
TARGET: Kinase -- PATHWAY: Sphingolipid metabolism; Autophagy; Necrosis -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer