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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:
Molecular Weight:
477.46
UNSPSC Code:
12352200
MDL number:
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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Quality Level

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

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

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.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)


Storage Class

11 - Combustible Solids

wgk

WGK 3



Certificates of Analysis (COA)

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