SBE13 hydrochloride

CAS No. : 1052532-15-6

SBE13 hydrochloride,1052532-15-6
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000284
Synonyms:N-(4-((6-chloropyridin-3-yl)methoxy)-3-methoxybenzyl)-2-(3,4-dimethoxyphenyl)ethanamine hydrochloride
Molecular Formula:C₂₄H₂₇ClN₂O₄.HCl
Molecular Weight:479.4
IC50:0.2 nM [1]
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Appearance:white solid powder
Purity: > 98%
Cat No:I000284
Cas No:1052532-15-6
Product-Name:SBE13 hydrochloride
MDL No:MFCD20036266

SBE13 Hcl is a potent and selective PLK1 with IC50 of 0.2 nM; no inhibition om Aurora A kinase, Plk2 and Plk3.
IC50 value: 0.2 nM [1]
Target: PLK1 inhibitor
in vitro: To test the selectivity of SBE13 for Plk1 we probed its inhibitory effect on aurora A kinase, Plk2, and Plk3. No decrease in aurora A kinase activity was observed, and only marginally decreased Plk2 (IC50>66μm) or Plk3 (IC50=875 nm) kinase activity was detected after 13 h release in the presence of SBE13 (p>0.05) [1]. Plk1 inhibition using SBE13 enhances the effects of Enzastaurin in cancer cells. HCT116(p53wt) and HCT116(p53-/-) cells confirmed the p53-dependence of different effects after Plk1 and PKCβ inhibition observed in HeLa and MCF-7 cells. Obviously, p53 protects cells from the cytotoxicity of Enzastaurin in combination with SBE13 [2].

[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]. Lange L, et al. Combinatorial inhibition of Plk1 and PKCβ in cancer cells with different p53 status. Oncotarget. 2014 Apr 30;5(8):2263-75.
[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.

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