[CAS NO. 1627710-50-2] LJH685
PRODUCTS SPECIFICATIONS [1627710-50-2]
DESCRIPTION [1627710-50-2]
Overview
| MDL | MFCD29924738 |
|---|---|
| Molecular Weight | 381.42 |
| Molecular Formula | C22H21F2N3O |
| SMILES | OC1=C(F)C=C(C2=C(C3=CC=C(N4CCN(C)CC4)C=C3)C=CN=C2)C=C1F |
2 Publications Citing Use of MCE
Summary
IC50 & Target
IC50: 6 nM (RSK1), 5 nM (RSK1), 4 nM (RSK1) [1]
In Vitro
LJH685 (0.01-100 μM; 72 hours) efficiently inhibits the growth of MDA-MB-231 and H358 cells in soft agar with EC
50
s of 0.73 and 0.79 μM, respectively
[1]
.
LJH685 (0.1-10 μM; 4 hours) efficiently reduces phosphorylation of YB1 at submicromolar concentrations and causes nearly complete inhibition at higher concentrations
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | MDA-MB-231, H358 cells |
| Concentration: | 0.01, 0.1, 1, 10, 100 μM |
| Incubation Time: | 72 hours |
| Result: | The growth in soft agar was efficiently inhibited with EC 50 values of 0.73 and 0.79 μM in MDA-MB-231 and H358, respectively. |
Western Blot Analysis [1]
| Cell Line: | MDA-MB-231, H358 cells |
| Concentration: | 0.1, 0.3, 1, 3, 10 μM |
| Incubation Time: | 4 hours |
| Result: | Efficiently reduced phosphorylation of YB1 at submicromolar concentrations and caused nearly complete inhibition at higher concentrations. |
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 : ≥ 31 mg/mL ( 81.28 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6218 mL | 13.1089 mL | 26.2178 mL |
| 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL |
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] Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7.
- [3] Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.
- [4] My-My Huynh, et al. RSK2: a promising therapeutic target for the treatment of triple-negative breast cancer. Expert Opin Ther Targets. 2020 Jan;24(1):1-5.