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Poloxin
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。
Poloxin图片
CAS NO:321688-88-4
规格:98%
分子量:297.35
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
PLK1 inhibitor
CAS:321688-88-4
分子式:C18H19NO3
分子量:297.35
纯度:98%
存储:Store at -20°C

Background:

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
Poloxin (25 μM) induces defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells[1]. Poloxin inhibits proliferation in both cell lines with a comparable efficiency through 72 h period[2]. Poloxin inhibits the polo-box domain (PBD) interaction with an apparent IC50 of ~4.8 μM. Poloxin exhibits a loose Plk1 PBD specificity with 4-10 times higher IC50 values for Plk2 and Plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains[3].
Poloxin (40 mg/kg) decreases the proliferation of MDA-MB-231 cells, and surpresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231[1].
Reference:
[1]. Yuan J, et al. Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo. Am J Pathol. 2011 Oct;179(4):2091-9.
[2]. Sanhaji M, et al. p53 is not directly relevant to the response of Polo-like kinase 1 inhibitors. Cell Cycle. 2012 Feb 1;11(3):543-53.
[3]. Lee KS, et al. Pinning down the polo-box domain. Chem Biol. 2008 May;15(5):415-6.
[4]. Reindl W, et al. Inhibition of polo-like kinase 1 by blocking polo-box domain-dependent protein-protein interactions. Chem Biol. 2008 May;15(5):459-66.