PF-543 (Sphingosine Kinase I Inhibitor)
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Catalog No.: B-0026 MW: 465.6 Purity: >99% CAS: 1415562-82-1 Description: |
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PF-543 is a potent inhibitor of sphingosine kinase 1 (SK1; IC50 = 2-3.6 nM) that less effectively inhibits SK2 (IC50 = 356 nM).(1) It does not significantly block the activity of other protein and lipid kinases, or bind sphingosine-1-phosphate receptors, when tested at a concentration of 10 µM.1 PF-543 prevents the phosphorylation of sphingosine in cancer cells and in whole blood (EC50 = 8.4 and 27 nM, respectively).1 Through its effects on SK1, PF-543 prevents sickling, hemolysis, and inflammation in sickling cell disease transgenic mice.(2) Unlike inhibitors that are selective for SK2, PF-543 does not impair DNA synthesis in human pulmonary arterial smooth muscle cells.(3) Storage-20C or belowReferences:1) M. E. Schnute, M. D. McReynolds, T. Kasten, et al. “Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1” Biochemistry Journal 2012, 444, 79-88.2) Y. Zhang, V. Berka, A. Song, et al. Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J. Clin. Invest. 2014, 124, 2750-2761. 3) H. S. Byun, S. Pyne, N. Macritchie, et al. Novel sphingosine-containing analogues selectively inhibit sphingosine kinase (SK) isozymes, induce SK1 proteasomal degradation and reduce DNA synthesis in human pulmonary arterial smooth muscle cells. Med. Chem. Comm. 2013, 4, 1-15. |
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Additional Information:
Tech Data Sheet - TDS_B-0026_x |
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