K145

K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC₅₀ of 4.3 µM and a K_i of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity^[1]. IC50 & Target: IC50: 4.3 µM (SphK2)^[1]
Ki: 6.4 µM (SphK2)^[1] In Vitro: K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner^[1].
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells^[1].
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt^[1].
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels^[1]. In Vivo: K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice^[1].