PF 543 hydrochloride
Chemical Name: (2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride
Biological ActivityPotent and selective SphK1 inhibitor (IC50 = 2 nM; Ki = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. Attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. Suppresses HCT-116 tumor xenograft growth in mice. Also reduces sickling, hemolysis and inflammation in a transgenic mouse model of sickle cell disease.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits
Schnute et al.
Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543.
Ju et al.
Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1.
Schnute et al.
Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression.
Zhang et al.
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