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

Properties

• Quality Level: 100
• 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

Description

General description

A cell-permeable thiophene-benzimidazole compound that acts as a potent and reversible inhibitor against polo-like kinases (K_i 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

Warning

Toxicity: Irritant (B)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3