SLC5111312 is a dual inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2 (Kis = 0.73 and 0.9 μM, respectively, using human recombinant kinases).
CAS：1870811-01-0
分子式：C22H27N5O3.HCl
分子量：445.9
纯度：98%
存储：Store at -20°C

Background:

SLC5111312 is a dual inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2 (Kis = 0.73 and 0.9 µM, respectively, using human recombinant kinases). SLC5111312 binding is selective for Sphk2 over Sphk1 in mice (Kis = 1 and 20 µM, respectively) but not rat (Kis = 1.1 and 0.8 µM, respectively). It decreases cell-associated sphingosine-1-phosphate (S1P) and increases sphingosine in U937 monocytic leukemia cells at concentrations of 0.1 and 0.3 µM. SLC5111312 (10 mg/kg) also decreases S1P in vivo in Sphk1-/- but not in Sphk2-/- mice and in rat, showing a functional selectivity for Sphk2 in mice.