528283

Polo-like Kinase Inhibitor II, BTO-1

The Polo-like Kinase Inhibitor II, BTO-1, also referenced under CAS 40647-02-7, 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 II, BTO-1, 5-Cyano-7-nitro-2-(benzothiazolo-N-oxide)-carboxamide
• Empirical Formula (Hill Notation): C₉H₄N₄O₄S
• CAS Number: 40647-02-7
• Molecular Weight: 264.22
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD11045282
• Assay: ≥97% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: beige to brown
• solubility: DMSO: 1 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [s]1c2c([n+](c1C(=O)N)[O-])cc(cc2[N+](=O)[O-])C#N
• InChI: 1S/C9H4N4O4S/c10-3-4-1-5-7(6(2-4)13(16)17)18-9(8(11)14)12(5)15/h1-2H,(H2,11,14)
• InChI key: FKRBAXZAJBBIAJ-UHFFFAOYSA-N

Description

General description

A cell-permeable benzothiazolo-N-oxide compound that targets the ATP-binding pocket of polo-like kinase and is shown to inhibit Plk1 kinase activity in cell-free kinase assays (IC₅₀ = 8.0 µM) and suppress the phosphorylation of cellular Plk1 substrate Cdc25C in rat kangaroo kidney-derived PTK cells (75% inhibition at 6.3 µM). BTO-1 treatment of cultured cells results in mitosis defects consistent with loss-of-Plk1 phenotypes seen in Plk1 RNAi-treated U20S cells, including the appearance of monopolar spindles and the reduction of γ-tubulin at the centrosomes. Plk1 inhibition by BTO-1 in HeLa cells results in a blockage of Rho and Rho-GEF recruitment, which is essential for the assembly of a functional contractile ring.

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

Brennan, I.M., et al. 2007. PloS ONE2, e409.
Peters, U., et al. 2006. Nat. Chem. Biol.2, 618.
McInnes, C., et al. 2006. Nat. Chem. Biol.2, 608.

Legal Information

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

Disclaimer

Toxicity: Harmful (C)

Safety Information

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