Table 2. Ki and cLogP Values for SphK2-Selective Inhibitorsa.
Inhibitory constants for recombinant enzymes were obtained by kinetic analysis of S1P production using variable concentration of sphingosine and a fixed concentration of ATP in the presence or absence of compounds as described previously.30 Selectivity for each compound was determined by dividing the KM for SphK2 by the KM for SphK1. hSphK2 selectivity for each compound was determined by dividing Ki for hSphK1 by the Ki for hSphK2.
Ki for mouse SphK2 is 110 ± 13 nM and mouse SphK1 is >10 000 nM.