| 产品描述： | K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity |
| 靶点： |
IC50: 4.3 µM (SphK2) Ki: 6.4 µM (SphK2);Apoptosis; S1PReceptor |
| 体外研究： |
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. |
| 体内研究： |
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. |
| 参考文献： |
1. Liu K, et al. Biological characterization of 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) as a selective sphingosine kinase-2 inhibitor and anticancer agent. PLoS One. 2013;8(2):e56471. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.598 ml |
12.99 ml |
25.979 ml |
| 5 mM |
0.52 ml |
2.598 ml |
5.196 ml |
| 10 mM |
0.26 ml |
1.299 ml |
2.598 ml |
| 50 mM |
0.052 ml |
0.26 ml |
0.52 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京