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Merck

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.

Synonym(s):

Polo-like Kinase Inhibitor III, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-((2-(trifluoromethyl)-benzyl)oxy)thiophene-2-carboxamide, Plk Inhibitor III

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About This Item

Empirical Formula (Hill Notation):
C22H18F3N3O4S
CAS Number:
660868-91-7
Molecular Weight:
477.46
UNSPSC Code:
12352200
MDL number:
MFCD09971143

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Product Name

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.

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

storage temp.

2-8°C

Quality Level

100

Disclaimer

Toxicity: Irritant (B)

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.

Other Notes

Johnson, E.F., et al. 2007. Biochemistry46, 9551.
Lansing, T.J., et al. 2007. Mol. Cancer Ther.6, 450.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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