IC50: 4.3 µM (SphK2) Ki: 6.4 µM (SphK2)

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. Animal Model: BALB/c-nu mice injected with U937 cells Dosage: 50 mg/kg Administration: Oral gavage; daily; for 15 days Result: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.

K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner. K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells. K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt. Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels. Cell Viability Assay Cell Line: U937 cells Concentration: 0 µM, 4 µM, 6 µM, 8 µM, 10 µM Incubation Time: 24 hours, 48 hours, 72 hours Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner. Apoptosis Analysis Cell Line: U937 cells Concentration: 10 µM Incubation Time: 24 hours Result: Significantly induced apoptosis in U937 cells. Western Blot Analysis Cell Line: U937 cells Concentration: 4 µM, 8 µM Incubation Time: 3 hours Result: Phosphorylated ERK and Akt were decreased.

K145 hydrochloride 是一种选择性的，具有底物竞争性和口服活性的 SphK2 抑制剂，IC50 为 4.3 µM，Ki 为 6.4 µM。K145 hydrochloride 对 SphK1 和其他蛋白激酶没有活性。K145 hydrochloride 可诱导细胞凋亡，并具有强大的抗肿瘤活性。