Name | K145 |
Synonyms | K145 3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione 2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]- |
CAS | 1309444-75-4 |
Molecular Formula | C18H24N2O3S |
Molar Mass | 348.46 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
biological activity | K145 is a selective, substrate-competitive and orally active SphK2 inhibitor, IC50 was 4.3 μm and Ki was 6.4 μm. K145 had no activity on SphK1 and other protein kinases. K145 can induce apoptosis and has strong anti-tumor activity. |
Target | IC50: 4.3 µm (SphK2) Ki: 6.4 µm (SphK2) |
Cell Line: | U937 cells U937 cells U937 cells |
Concentration: | 0 µM, 4 µM, 6 µM, 8 µM, 10 µM 10 µM 4 µM, 8 µM |
Incubation Time: | 24 hours, 48 hours, 72 hours 24 hours 3 hours |
Result: | Significantly inhibited the growth of U937 cells in a concentration-dependent manner. Significantly induced apoptosis in U937 cells. Phosphorylated ERK and Akt were decreased. Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed. |
Animal Model: | BALB/c-nu mice injected with U937 cells |
Dosage: | 50 mg/kg |
Administration: | Oral gavage; daily; for 15 days |