528282

Polo-like Kinase Inhibitor I

The Polo-like Kinase Inhibitor I, also referenced under CAS 916985-21-2, 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 I, 5-(5,6-Dimethoxybenzimidazol-1-yl)-3-(4-methanesulfonyl-benzyloxy)-thiophene-2-carboxamide, Plk Inhibitor I, Plk Inhibitor I, 5-(5,6-Dimethoxybenzimidazol-1-yl)-3-(4-methanesulfonyl-benzyloxy)-thiophene-2-carboxamide
• Empirical Formula (Hill Notation): C₂₂H₂₁N₃O₆S₂
• CAS Number: 916985-21-2
• Molecular Weight: 487.55
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: tan
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C22H21N3O6S2/c1-29-17-8-15-16(9-18(17)30-2)25(12-24-15)20-10-19(21(32-20)22(23)26)31-11-13-4-6-14(7-5-13)33(3,27)28/h4-10,12H,11H2,1-3H3,(H2,23,26)
• InChI key: YYZTVTZCYVZGRB-UHFFFAOYSA-N

Description

General description

A thiophenecarboxamide compound that acts as a potent and ATP-binding site-targeting inhibitor of polo-like kinase 1 (IC₅₀ = 126 nM) with excellent selectivity over IKK-2 and IKK-3 (IC₅₀ >16 µM).

Biochem/physiol Actions

Cell permeable: no

Primary Target
Polo-like Kinase

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 126 nM against polo-like kinase 1

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Bamborough, P., et al. 2006. Bioorg. Med. Chem. Lett.16, 6236.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable