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Potent pan-ribosomal S6 protein kinase (RSK) inhibitor (IC50 values are 4 to 13 nM). Displays selectivity for RSK isoforms over other kinases. Inhibits RSK-dependent Y-box binding protein 1 (YB-1) phosphorylation in vitro. Suppresses growth of triple negative breast cancer cell lines.
|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|
Preparing Stock Solutions
The following data is based on the product molecular weight 368.38. 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|
|0.5 mM||5.43 mL||27.15 mL||54.29 mL|
|2.5 mM||1.09 mL||5.43 mL||10.86 mL|
|5 mM||0.54 mL||2.71 mL||5.43 mL|
|25 mM||0.11 mL||0.54 mL||1.09 mL|
References are publications that support the biological activity of the product.
Jain et al (2015) Discovery of potent and selective RSK inhibitors as biological probes. J.Med.Chem. 58 6766 PMID: 26270416
Aronchik et al (2014) Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol.Cancer Res. 12 803 PMID: 24554780
Davies et al (2015) Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 6 20570 PMID: 26011941
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