SL 0101-1

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Cat.No. 2250 - SL 0101-1 | C25H24O12 | CAS No. 77307-50-7
Description: Selective ribosomal S6 kinase (RSK) inhibitor
Chemical Name: 3-[(3,4-Di-O-acetyl-6-deoxy-α-L-mannopyranosyl)oxy]-5,7-dihydro-2-(4-hydroxyphenyl)-4H-1benzopyran-4-one
Purity: ≥95% (HPLC)
Datasheet
Citations (7)
Reviews
Literature

Biological Activity

Selective 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.

Technical Data

M. Wt 516.46
Formula C25H24O12
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 77307-50-7
PubChem ID 14825856
InChI Key SXOZSDJHGMAEGZ-UHFFFAOYSA-N
Smiles O=C1C3=C(C=C(O)C=C3O)OC(C4=CC=C(O)C=C4)=C1OC2C(O)C(OC(C)=O)C(OC(C)=O)C(C)O2

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
ethanol 10.33 20
DMSO 5.16 10

Preparing Stock Solutions

The following data is based on the product molecular weight 516.46. 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 1.94 mL 9.68 mL 19.36 mL
5 mM 0.39 mL 1.94 mL 3.87 mL
10 mM 0.19 mL 0.97 mL 1.94 mL
50 mM 0.04 mL 0.19 mL 0.39 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

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

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

Saha et al (2012) RSK phosphorylates SOS1 creating 14-3-3-docking sites and negatively regulating MAPK activation. Biochem.J. 447 159 PMID: 22827337


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Keywords: SL 0101-1, SL 0101-1 supplier, Selective, p90, ribosomal, S6, kinases, RSK, inhibitors, inhibits, SL0101-1, 2250, Tocris Bioscience

7 Citations for SL 0101-1

Citations are publications that use Tocris products. Selected citations for SL 0101-1 include:

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

Gawecka et al (2012) RSK2 protein suppresses integrin activation and fibronectin matrix assembly and promotes cell migration. J Biol Chem 287 43424 PMID: 23118220

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

Gawecka et al (2012) PEA15 impairs cell migration and correlates with clinical features predicting good prognosis in neuroblastoma. Int J Cancer 131 1556 PMID: 22213050

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

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


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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases