K145 是一种选择性的，具有底物竞争性和口服活性的 Sph

K145  

K145 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，K_i 为 6.4 µM。K145 对 SphK1 和其他蛋白激酶没有活性。K145 可诱导细胞凋亡，并具有强大的抗肿瘤活性。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

生物活性    
K145 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 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity[1].

IC50 & Target    
IC50: 4.3 µM (SphK2)[1]
Ki: 6.4 µM (SphK2)[1]

体外研究(In Vitro)    
K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner[1].
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells[1].
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt[1].
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels[1].

Cell Viability Assay[1]

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.

体内研究(In Vivo)    
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[1].

Animal Model:    BALB/c-nu mice injected with U937 cells[1]
Dosage:    50 mg/kg
Administration:    Oral gavage; daily; for 15 days
Result:    Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.

分子量    
348.46

Formula    
C18H24N2O3S

CAS 号    
1309444-75-4

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Please store the product under the recommended conditions in the Certificate of Analysis.
 

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.  [Content Brief]

•