SphK1-IN-5

SphK1-IN-5 (compound 9d) potently and selectively inhibits purified SphK1 with an IC₅₀ of 0.87 μM, while it exhibits only weak activity against SphK2. It also acts as an ATP-competitive inhibitor of purified SphK1 with a K_i value of 1.05 μM, and directly binds to endogenous SphK1 in MC38 cells to enhance its thermal stability^[1].
SphK1-IN-5 exhibits high specificity for SphK1, with no significant inhibitory effect on the other 27 purified kinases tested at a concentration of 10 μM^[1].
SphK1-IN-5 (1-10 μM) increases Sph levels and decreases S1P levels in HepG2 cells in a dose-dependent manner by inhibiting SphK1 activity^[1].
SphK1-IN-5 exhibits antiproliferative activity against HCT-116, MC38, Hepa1-6 and HepG2 tumor cells, but shows no activity against non-tumor NIH-3T3 cells or breast cancer MCF-7 cells^[1].
SphK1-IN-5 (1-10 μM; 48 h) induces apoptosis in MC38 cells in a dose-dependent manner, and its activity at the concentration of 10 μM is superior to that of the reference inhibitor PF-543 (HY-15425)^[1].
SphK1-IN-5 (1-10 μM; 24 h) induces G2/M and S phase cell cycle arrest in MC38 cells^[1].
SphK1-IN-5 (1-10 μM; 12, 24 h) inhibits the migration of MC38 cells in a concentration- and time-dependent manner, and exhibits superior activity to PF-543 (HY-15425) at equivalent concentrations^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.