PF-543

PF-543 is a potent, selective, and sphingosine-competitive small molecule inhibitor of sphingosine kinase 1 (SPHK1), originally developed by Pfizer. It inhibits SPHK1 with an IC50 of 2 nM and a Ki of 3.6 nM, demonstrating over 100-fold selectivity for SPHK1 compared to the SPHK2 isoform. By blocking the conversion of sphingosine to sphingosine 1-phosphate (S1P), PF-543 effectively reduces S1P levels and has been shown to induce apoptosis, necrosis, and autophagy in various cancer cell lines. While primarily utilized as a high-affinity chemical probe in research, PF-543 has been extensively studied in preclinical models for its potential in treating colorectal, breast, and lung cancers, as well as pulmonary arterial hypertension, sepsis-associated acute kidney injury, and various fibrotic or inflammatory conditions.

Other names

PF-543 hydrochloridePF543 hydrochloridePF 543 hydrochloridePF-543 HClPF543 HClPF 543 HCl