PF-543 478 Toh et al (2015) A

Toh et al (2015) A strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor of N6-methyladenosine demethylase FTO

CAS Number: 612487-72-6

H2O4S/c1-7-13(26-9-2-8(3-27)14(33)18(37)15(9)34)17(36)20(39)24(41-7)44-23-12(6-30)42-25(21(40)19(23)38)43-22(11(32)5-29)16(35)10(31)4-28

8(8):e72641

InChi: InChI=1S/C27H29NO3/c1-5-31-26(30)23-17(2)28-21-15-27(3

PF-543 478 Toh et al (2015) APF 543 is a novel selective SK 1 inhibitor which inhibited SK 1 activity in a competitive manner with sphingosine. PF 543 inhibits SphK1 with a K(i) of 3. 6 nM, is sphingosine competitive and is more than 100 fold selective for SphK1 over the SphK2 isoform. PF 543 was effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. PF 543 is the most