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SBE 13 HCl
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。
SBE 13 HCl图片
CAS NO:1052532-15-6
规格:98%
分子量:479.4
包装与价格:
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
Inactive Plk1 inhibitor
CAS:1052532-15-6
分子式:C24H28Cl2N2O4
分子量:479.4
纯度:98%
存储:Store at -20°C

Background:

The serine/threonine kinase polo-like kinase 1 (Plk1) attracts great attention in the field of cancer therapy because it exhibits generally elevated activity in cancer cells and is a negative prognostic factor for cancer patients. The importance of Plk1 activity as a measure for the aggressiveness of a tumor results from its important role in mitotic checkpoints. SBE13 is identified as a novel and potent inhibitor of inactive Plk1.


In vitro: To determine its ability to induce cell death in cancer cells, we applied kinase assays, western blot analyses, FACS can analyses, Caspase assays and immunofluorescence studies. We detected decreased cell proliferation, delayed progression through the cell cycle in lower SBE13 concentrations, a G2/M arrest using higher SBE13 concentrations followed by apoptosis, and abnormal mitotic figures. Notably, SBE13 did not influence activity of other kinases (Plk2, Plk3, Aurora A), indicating the selectivity of this type II Plk1 inhibitor [1].


In silico: The docking pose of SBE13 in the homology model suggests an interaction with Arg 95 of Plk1, and thus spans the whole hydrophobic pocket, which is anticipated for a type II inhibitor. Another SBE13’s characteristic feature of type II inhibitors is the interaction with the hinge region and with the Asp in the Asp-Phe-Gly (DFG) motif [2].


Clinical trial: Up to now, SBE13 is still in the preclinical development stage.


Reference:
[1] Keppner S, Proschak E, Kaufmann M, Strebhardt K, Schneider G, Sp?nkuch B.  Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73.
[2] Keppner S, Proschak E, Schneider G, Sp?nkuch B.  Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009 Nov;4(11):1806-9.