Cat. No. 2250
Chemical Name: 3-[(3,4-Di-O-acetyl-6-deoxy-α-L-mann
Biological ActivitySelective inhibitor of ribosomal S6 kinase (RSK) (IC50 = 89 nM for RSK2). Does not inhibit upstream kinases such as MEK, Raf and PKC. Inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297. PMID: 17850214.
Godeny and Sayeski (2006) ERK1/2 regulates ANG II-dependent cell proliferation via cytoplasmic activation of RSK2 and nuclear activation of elk1. Am.J.Cell.Physiol. 291 1308.
Smith et al (2005) Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation. Cancer Res. 65 1027. PMID: 15705904.
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Citations are publications that use Tocris products. Selected citations for SL 0101-1 include:
Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. J Biol Chem 5 3145. PMID: 24762669.
Gawecka et al (2012) RSK2 protein suppresses integrin activation and fibronectin matrix assembly and promotes cell migration. J Biol Chem 287 43424. PMID: 23118220.
Li et al (2012) Involvement of polo-like kinase 1 (Plk1) in mitotic arrest by inhibition of mitogen-activated protein kinase-extracellular signal-regulated kinase-ribosomal S6 kinase 1 (MEK-ERK-RSK1) cascade. PLoS One 287 15923. PMID: 22427657.
Kroczynska et al (2011) Regulatory effects of ribosomal S6 kinase 1 (RSK1) in IFNλ signaling. J Biol Chem 286 1147. PMID: 21075852.
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984. PMID: 21143600.
Roselli et al (2009) Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways. PLoS One 4 e6011. PMID: 19547699.
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Keywords: SL 0101-1, supplier, Selective, p90, ribosomal, S6, kinases, RSK, inhibitors, inhibits, SL0101-1, Tocris Bioscience, RSK Inhibitor products
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