Biological Activity
Selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). Exhibits no effect on Aurora kinase A activity. Binds and stabilizes the inactive form of PLK1. Delays cell cycle progression, reduces cell proliferation and induces apoptosis in a range of human cancer cell lines. Transiently arrests cells cycle at G0/G1 in primary cells.
Compound Libraries
SBE 13 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 479.4 |
| Formula | C24H27ClN2O4.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1052532-15-6 |
| PubChem ID | 11948807 |
| InChI Key | QBGSVDJLQQXEGG-UHFFFAOYSA-N |
| Smiles | ClC(N=C3)=CC=C3COC1=C(OC)C=C(CNCCC2=CC(OC)=C(OC)C=C2)C=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.94 | 100 | |
| ethanol | 4.79 | 10mM with gentle warming | |
| water | 4.79 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 479.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.09 mL | 10.43 mL | 20.86 mL |
| 5 mM | 0.42 mL | 2.09 mL | 4.17 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.09 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Eckerdt (2010) Freezing Polo in its sleep: targeting the inactive conformation of Polo-like kinase 1 in cancer cells. Cell Cycle 9 862 PMID: 20348843
Keppner et al (2010) Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle 9 761 PMID: 20139717
Liu (2010) SBE13 joins the family of Polo-like kinase 1 (Plk1) inhibitors. Cell Cycle 9 445 PMID: 20130451
Keppner et al (2011) Fate of primary cells at the G1/S boundary after Polo-like kinase 1 inhibition by SBE13. Cell Cycle 10 708 PMID: 21301227
Keppner et al (2009) Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem 4 1806 PMID: 19746360
Keywords: SBE 13 hydrochloride, supplier, SBE13, polo-like, kinases, plk1, plk, selective, potent, Polo-like, Kinase, Mitosis, Polo-like, Kinase, Tocris Bioscience
