528284
Polo-like Kinase Inhibitor III
The Polo-like Kinase Inhibitor III, also referenced under CAS 660868-91-7, controls the biological activity of Polo-like Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
Polo-like Kinase Inhibitor III, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-((2-(trifluoromethyl)-benzyl)oxy)thiophene-2-carboxamide, Plk Inhibitor III
InChI
1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29)
InChI key
JSKUWFIZUALZLX-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 10 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable thiophene-benzimidazole compound that acts as a potent and reversible inhibitor against polo-like kinases (Ki against Plk1/2/3/4 = 4.8, 3.8, 8.0, and 163 nM , respectively), while exhibiting little or much reduced activity against 39 other commonly studied kinases. Preferentially inhibits the proliferation of a panel of 11 tumor cell lines (IC50 ≤0.7 µM) over normal human diploid fibroblasts (IC50 = 6.14 µM) in culture and is equally potent against the mdr-1-expressing MES-SA/DX5 and its parent non-drug resistant MES-SA uterine sarcoma cell line.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Johnson, E.F., et al. 2007. Biochemistry46, 9551.
Lansing, T.J., et al. 2007. Mol. Cancer Ther.6, 450.
Lansing, T.J., et al. 2007. Mol. Cancer Ther.6, 450.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
11 - Combustible Solids
wgk
WGK 3
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