528283
Polo-like Kinase Inhibitor II, BTO-1
5-Cyano-7-nitro-2-(benzothiazolo-N-oxide)-carboxamide
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
01 June 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | Beige solid | ||
| Molar mass | 264.2 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C9H4N4O4S | ||
| CAS number | 40647-02-7 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Harmful |
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| Safety information | |||
|---|---|---|---|
| S Phrase |
S: 26-36/37 In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves. |
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| R Phrase |
R: 20/21/22-36/37/38 Harmful by inhalation, in contact with skin and if swallowed. Irritating to eyes, respiratory system and skin. |
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