Table 4.
KI values for head group modifications.
Compound | Structure | KI (μM)a | SphK1 Selectivityb | |
---|---|---|---|---|
SphK1 | SphK2 | |||
1 |
![]() |
0.2 | 0.5 | 5 |
33 |
![]() |
1.6 | 5 | 6.3 |
36a |
![]() |
0.13 | 1.5 | 24 |
36b |
![]() |
16 | 5 | 0.6 |
38 |
![]() |
0.075 | 3 | 80 |
47 |
![]() |
0.099 | 5.3 | 110 |
40 |
![]() |
0.13 | 8 | 130 |
KI = [I]/(K’M/KM - 1); KM of Sphingosine at SphK1 = 10 μM; KM of Sphingosine at SphK2 = 5 μM
Selectivity = (KI/KM)SphK2/(KI/KM)SphK1