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SBE13 Sale

目录号 : GC37601

A potent Plk1 inhibitor

SBE13 Chemical Structure

Cas No.:775294-82-1

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Sample solution is provided at 25 µL, 10mM.

Description

SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme 1,2. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 ?M) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 ?M), and induces apoptosis in a broad range of human cancer cell lines.2,3

1.Keppner, S., Proschak, E., Schneider, G., et al.Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1Chem. Med. Chem.4(11)1806-1809(2009) 2.Keppner, S., Proschak, E., Kaufmann, M.T., et al.Biological impact of freezing Plk1 in its inactive conformation in cancer cellsCell Cycle9(4)761-773(2010) 3.Keppner, S., Proschak, E., Schneider, A., et al.Fate of primary cells at the G1/S boundary after polo-like kinase 1 inhibition by SBE13Cell Cycle10(4)708-720(2011)

实验参考方法

Kinase experiment:

To assay Plk1 kinase activity, cells are lysed after 13?h release in the presence of SBE13 after double thymidine block and kinase is immunoprecipitated from lysates using antibodies. In brief, for each immunoprecipitation 800?μg of total protein are incubated with Plk1 antibody cocktail (1.5?μg) for 2?h at 4°C on a rotator. Immunoprecipitated protein is collected using Protein A/G Agarose beads. Plk1 immunoprecipitates are incubated with casein (1?μg) and with [γ-32P]ATP (1?μCi) for 30?min at 37°C in kinase buffer. Products from the kinase assays are fractionated on 10?% bis-tris-polyacrylamide gels, and phosphorylated substrate is visualized by autoradiography after an exposure of 12-36?h. Equal amounts of immunoprecipitates are subjected to Western blot analysis to confirm equal loading of Plk1 protein in kinase reactions[1].

References:

[1]. Keppner S, et al. Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009 Nov;4(11):1806-9.
[2]. Keppner S, et al. Fate of primary cells at the G /S boundary after polo-like kinase 1 inhibition by SBE13. Cell Cycle. 2011 Feb 15;10(4):708-20. Epub 2011 Feb 15.
[3]. Keppner S, et al. Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73. Epub 2010 Feb 16.

化学性质

Cas No. 775294-82-1 SDF
Canonical SMILES COC1=CC=C(CCNCC2=CC=C(OCC3=CC=C(Cl)N=C3)C(OC)=C2)C=C1OC
分子式 C24H27ClN2O4 分子量 442.94
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 2.2576 mL 11.2882 mL 22.5764 mL
5 mM 0.4515 mL 2.2576 mL 4.5153 mL
10 mM 0.2258 mL 1.1288 mL 2.2576 mL
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