[CAS NO. 1627709-94-7] LJI308
PRODUCTS SPECIFICATIONS [1627709-94-7]
DESCRIPTION [1627709-94-7]
Overview
| MDL | MFCD29905461 |
|---|---|
| Molecular Weight | 368.38 |
| Molecular Formula | C21H18F2N2O2 |
| SMILES | OC1=C(F)C=C(C2=C(C3=CC=C(N4CCOCC4)C=C3)C=CN=C2)C=C1F |
3 Publications Citing Use of MCE
Summary
LJI308 is a potent pan- ribosomal S6 kinase (RSK) inhibitor, with IC 50 s of 6 nM, 4 nM, and 13 nM for RSK1 , RSK2 , and RSK3 , respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF , and in cells expressing a KRAS mutation [1] [2] .
In Vitro
LJI308 inhibits S6K1 with an IC
50
of 0.8 μM
[1]
.
LJI308 inhibits YB-1 phosphorylation in CRC cells at concentrations of 5 to 25 μM. In a dose kinetics experiment, LJI308, starting at 2.5 μM, inhibits YB-1 phosphorylation in the KRAS mutated TNBC cell line MDA-MB-231 by approximately 86%. LJI308 effectively blocks RSK and YB-1 phosphorylation after EGF stimulation and after irradiation in KRAS wild-type HBL-100 cells
[2]
.
LJI308 (1-10 μM; 96 hours) decreases cell viability by up to 90%
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [3]
| Cell Line: | HTRY-LT cell lines |
| Concentration: | 1-10 μM |
| Incubation Time: | 96 hours |
| Result: | Decreased cell viability by up to 90%. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 67.86 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7146 mL | 13.5729 mL | 27.1459 mL |
| 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL |
| 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution
References
- [1] Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12.
- [2] Lettau K, et al. Simultaneous Targeting of RSK and AKT Efficiently Inhibits YB-1-Mediated Repair of Ionizing Radiation-Induced DNA Double-Strand Breaks in Breast Cancer Cells. Int J Radiat Oncol Biol Phys. 2021;109(2):567-580.
- [3] Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015;6(24):20570-20577.
- [4] Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.