LJI308

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Cat.No. 6754 - LJI308 | C21H18F2N2O2 | CAS No. 1627709-94-7
Description: Potent pan-RSK inhibitor
Chemical Name: 2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]phenol
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

M. Wt 368.38
Formula C21H18F2N2O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1627709-94-7
PubChem ID 118704762
InChI Key YUYJEQHNWKQNBT-UHFFFAOYSA-N
Smiles OC1=C(C=C(C2=CN=CC=C2C3=CC=C(N4CCOCC4)C=C3)C=C1F)F

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.42 50

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

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References

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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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