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LJI308 efficiently inhibits RSK activity. LJI308 inhibites S6K1 with an IC50 of 0.8 μM, representing a 200-fold lower inhibition than that of RSK2. LJI308 inhibits MEK4 less than 50% at 10 μMand HIP kinase 1 less than 50% at 1 μM. LJI308 inhibits the growth and survival of TNBC. LJI308 also suppresses the growth of HTRY-LT cells in 3-dimensional soft agar cultures. LJI308 is one of the first potent and effective targeted therapies for TNBC that, unlike currently utilized drugs, exhibits efficacy in eliminating the CSC population.
| Cell Experiment | |
|---|---|
| Cell lines | HTRZ and HTRY-LT1 cell lines |
| Preparation method | Viability of HTRZ and HTRY-LT1 cell lines treated with increasing doses of LJI308 (1 - 10 μM) for 96 hours. DMSO treated cells served as a control. |
| Concentrations | 1 - 10 μM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 368.38 |
| Formula | C21H18F2N2O2 |
| CAS Number | 1627709-94-7 |
| Form | Solid |
| Solubility (25°C) | 32 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related S6 Kinase Products |
|---|
| BI-D1870
BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of the p90 RSK (ribosomal S6 kinase) with IC50 values of 31 nM, 24 nM, 18 nM, 15 nM for RSK1, RSK2, RSK3, RSK4, respectively. |
| PF-4708671
PF-4708671 is a novel cell-permeable inhibitor of S6K1 with Ki/IC50 value of 20 nM/160 nM. PF4708671 inhibits MSK1 (IC50 of 0.95 μM) 4-fold more weakly than S6K1. |
| FMK
FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinaseRSK2 (wt) with IC50 of 15 nM, >600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants. |
| SL 0101-1
SL-0101-1 is a selective p90 RSK inhibitor for RSK2 with IC50 of 89 nM. |
| Quercitrin
Quercitrin (Quercitrin) is a natural compound in bitter buckwheat, which has anti-inflammatory effects and has the potential to be used in cardiovascular disease research. |
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