K145

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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，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。

K145

K145 Chemical Structure

CAS No. : 1309444-75-4

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K145 的其他形式现货产品:

K145 hydrochloride

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Apoptosis Analysis[1]

Cell Line: U937 cells
Concentration: 10 µM
Incubation Time: 24 hours
Result: Significantly induced apoptosis in U937 cells.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 4 µM, 8 µM
Incubation Time: 3 hours
Result: Phosphorylated ERK and Akt were decreased.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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