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1309444-75-4

中文名称 1309444-75-4
英文名称 K145
CAS 1309444-75-4
分子式 C18H24N2O3S
分子量 348.46
MOL 文件 1309444-75-4.mol
1309444-75-4 结构式 1309444-75-4 结构式

基本信息

英文别名
K145
3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-
所属类别
生物化工:激动剂抑制剂

物理化学性质

溶解度溶于二甲基亚砜
形态粉末

常见问题列表

生物活性
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,Ki 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。
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: Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
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