1449240-68-9
1449240-68-9 结构式
基本信息
3-(2-氨基乙基)-5-[3-(4-丁氧基苯基)亚丙基]-2,4-噻唑烷二酮盐酸盐
SphK2 inhibitor
K14 (hydrochloride)
K145 (hydrochloride)
K145 hydrochloride >=98% (HPLC)
SPHK2 INHIBITOR
K 145 HYDROCHLORIDE
K-145 HYDROCHLORIDE
3-(2-Amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione hydrochloride
3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione hydrochloride (1:1)
常见问题列表
IC50: 4.3 µM (SphK2)
Ki: 6.4 µM (SphK2)
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 (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. |