| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H18F2N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50 values of 6 nM, 4 nM and 13 nM against RSK1, RSK2 and RSK3, respectively. It blocks phosphorylation of RSK at T359/S363 and of YB-1 at S102 following irradiation, EGF treatment, and in cells carrying a KRAS mutation[1][2]. It is supplied as a light yellow to yellow solid (C21H18F2N2O2, MW 368.38) at 99.07% purity.
Physical & Chemical Properties
| CAS Number | 1627709-94-7 |
|---|---|
| Molecular Formula | C21H18F2N2O2 |
| Molecular Weight | 368.38 g/mol |
| Purity | 99.07% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | OC1=C(C=C(C=C1F)C2=C(C=CN=C2)C3=CC=C(C=C3)N4CCOCC4)F |
| Target | RSK1, RSK2, RSK3 |
| Signaling Pathway | MAPK/ERK Pathway; Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 25 mg/mL (67.86 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (67.86 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (6.79 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
S6K1 is inhibited by LJI308, with an IC50 of 0.8 μM[1]. In CRC cells, LJI308 at 5 to 25 μM suppresses YB-1 phosphorylation. A dose kinetics experiment shows that, starting at 2.5 μM, LJI308 reduces YB-1 phosphorylation by approximately 86% in MDA-MB-231, a KRAS mutated TNBC cell line. In KRAS wild-type HBL-100 cells, LJI308 effectively blocks RSK and YB-1 phosphorylation following EGF stimulation and following irradiation[2]. LJI308 (1-10 μM; 96 hours) reduces cell viability by up to 90%[3].
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%. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Cannabinoid Receptor 2-Centric Molecular Feedback Loop Drives Necroptosis in Diabetic Heart Injuries. Circulation 2023 Jan 10;147(2):158-174. PMID: 36448459
Upregulated PARP1 confers breast cancer resistance to CDK4/6 inhibitors via YB-1 phosphorylation. Exp Hematol Oncol 2023 Nov 30;12(1):100. PMID: 38037159
Inhibition of the Extracellular Signal-Regulated Kinase/Ribosomal S6 Kinase Cascade Limits Chlamydia trachomatis Infection. J Invest Dermatol 2021 Apr;141(4):852-862.e6. PMID: 32918951
Harvard University. 2026.
Involvement of Polo-like kinase 1 (Plk1) in quiescence regulation of cancer stem-like cells of the gastric cancer cell lines. Oncotarget 2017 Jun 6;8(23):37633-37645.
