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OTSSP167
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
OTSSP167图片
CAS NO:1431697-89-0
规格:98%
分子量:487.42
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
MELK inhibitor
CAS:1431697-89-0
分子式:C25H28Cl2N4O2
分子量:487.42
纯度:98%
存储:Store at -20°C

Background:

OTSSP167 is an inhibitor of maternal embryonic leucine zipper kinase (MELK) with IC50 value of 0.41nM [1].


MELK is a member of the AMPK serine/threonine kinase family and is involved in the mammalian embryonic development. It plays roles in cancer cell growth and formation or maintenance of cancer stem cells. OTSSP167 is a small-molecule inhibitor and can inhibit MELK’s activity effectively and selectively. OTSSP167 inhibits cell proliferation of a variety of cancer cell lines including A549, T47D, DU4475 and 22Rv1. The IC50 values are 6.7nM, 4.3nM, 2.3nM and 6nM, respectively. In mice bearing MDA-MB-231 xenograft, administration of OTSSP167 inhibits 70% tumor growth at dose of 20 mg/kg. Besides that, OTSSP167 is also found to have effects on PSMA1 and DBNL which are the novel substrates of MELK. It inhibits the phosphorylation of PSMA1 and DBNL causes the subsequent suppression of mammosphere formation [1].


参考文献:
[1] Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget, 2012, 3(12): 1629.