A potent inhibitor of SPHK1 (IC50 = 2 nM); inhibits S1P binding to human recombinant SPHK1 (Ki = 3.6 nM); selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at 10 µM; inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM

PF-543 – 10 mg

Brand:
Cayman
CAS:
1415562-82-1
Storage:
-20
UN-No:
De Minimis - 3077 / 9

PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).{27977} It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.{27978}  

 

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Description

A potent inhibitor of SPHK1 (IC50 = 2 nM); inhibits S1P binding to human recombinant SPHK1 (Ki = 3.6 nM); selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at 10 µM; inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively); prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease

Formal name: 1-[[4-[[3-methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2R-pyrrolidinemethanol

Synonyms: 

Molecular weight: 465.6

CAS: 1415562-82-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Lipid Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Sphingolipid Turnover||Research Area|Cardiovascular System|Blood|Erythrocytes & Hemoglobin

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