S83381 |
K145 (hydrochloride) |
| 源叶(MedMol) | 98% |
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- 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)
- 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
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