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Potent and selective centromere associated protein E (CENP-E) allosteric inhibitor (IC50 = 22 nM); does not compete with ATP. Exhibits selectivity over a panel of other kinesins (<25% inhibition at 50 μM). Inhibits tumor cell growth in vitro. Induces mitotic arrest and regression of human tumor xenografts in vivo.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||11.84||20 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 592.13. Batch specific molecular weights may vary from batch to batch due to the degree 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||1.69 mL||8.44 mL||16.89 mL|
|5 mM||0.34 mL||1.69 mL||3.38 mL|
|10 mM||0.17 mL||0.84 mL||1.69 mL|
|50 mM||0.03 mL||0.17 mL||0.34 mL|
References are publications that support the biological activity of the product.
Qian et al (2010) Discovery of the first potent and selective inhibitor of centromere-associated protein E: GSK923295. ACS Med.Chem.Lett. 1 30 PMID: 24900171
Wood et al (2010) Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc.Natl.Acad.Sci.U.S.A. 107 5839 PMID: 20167803
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Keywords: GSK 923295A, GSK 923295A supplier, GSK923295A, ATPase, Potent, selective, centromere, associated, protein, E, CENP-E, allosteric, inhibitors, inhibits, mitotic, kinesin, mitosis, Kinesin, 6837, Tocris Bioscience
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