N,N-Dimethylsphingosine

N,N-Dimethylsphingosine is a sphingosine kinase inhibitor. N,N-Dimethylsphingosine binds competitively to sphingosine kinase and blocks the conversion of sphingosine to sphingosine-1-phosphate. N,N-Dimethylsphingosine inhibits sphingosine-1-phosphate release and aggregation of platelets, and also exerts pro-apoptotic effects by resetting ceramide/sphingosine-1-phosphate homeostasis. N,N-Dimethylsphingosine can be used in cancer-related research^[1][2][3]. In Vitro:N,N-Dimethylsphingosine (0.2-50 µM; 5 min) inhibits sphingosine kinase activity in human platelets, with an IC₅₀ of approximately 10 µM^[1].
N,N-Dimethylsphingosine (0.2-50 µM; 1 h) inhibits sphingosine kinase activity in cell-free cytosolic fractions of human platelets, with an IC₅₀ of approximately 5 µM^[1].
N,N-Dimethylsphingosine (25 µM; 1 min pretreatment) inhibits TPA (HY-18739)-induced sphingosine-1-phosphate release in human platelets^[1].
N,N-Dimethylsphingosine (5-50 µM; 30 min) is a potent competitive inhibitor of sphingosine kinase, with K_i values of 3.1 µM, 2.3 µM, and 6.8 µM in cytoplasmic extracts of U937, Swiss 3T3, and PC12 cells, respectively^[2].
N,N-Dimethylsphingosine (10-20 μM; 4-6 h) induces apoptosis in human leukemia cell lines CMK-7, HL60 and U937^[3].
N,N-Dimethylsphingosine (5-20 μM; 6-12 h) induces apoptosis in human cancer cell lines A431, MKN74, HT29, HRT18 and COLO205^[3].