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Submit ReviewLJI308
Description: Potent pan-RSK inhibitor
Chemical Name: 2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]phenol
Purity: ≥98% (HPLC)
Biological Activity for LJI308
LJI308 is a 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.
Compound Libraries for LJI308
LJI308 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LJI308
| 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 for LJI308
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.42 | 50 |
Preparing Stock Solutions for LJI308
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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Product Datasheets for LJI308
References for LJI308
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
If you know of a relevant reference for LJI308, please let us know.
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Citations for LJI308
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