| Description | LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. |
| In vitro | 在MDA-MB-231和H358细胞中，LJI308以EC50为0.2-0.3 μM阻断RSK的细胞抑制及其对YB1 Ser102的磷酸化，从而抑制细胞生长。[1] 在TNBC HTRY-LT细胞中，LJI308也通过抑制YB-1来抑制细胞生长。[2] |
| Cell experiments | Cell growth under attached conditions is assessed by plating 1000 cells per well on 96-well tissue culture-treated plates in cell growth medium. Appropriate dilutions of compound are 4 added medium above cells and cell growth was assessed after 72 hrs by addition of CellTiter Glo reagent according to manufacturer’s directions. (Only for Reference) |
| Target activity | RSK3:13 nM, RSK2:4 nM, RSK1:6 nM |
| molecular weight | 368.38 |
| Molecular formula | C21H18F2N2O2 |
| CAS | 1627709-94-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: Insoluble DMSO: 50 mg/mL (135.73 mM), Heating is recommended. |
| References | 1. Aronchik I, et al. Mol Cancer Res. 2014, 12(5), 803-812. 2. Davies AH, et al. Oncotarget. 2015, 6(24), 20570-205777. |