| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H21F2N3O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
LJH685 is a potent, ATP-competitive and selective inhibitor of RSK, blocking the biochemical activities of RSK1, RSK2 and RSK3 with IC50 values of 6 nM, 5 nM and 4 nM, respectively[1]. It is supplied as a white to off-white solid (C22H21F2N3O, MW 381.42) at 99.64% purity.
Physical & Chemical Properties
| CAS Number | 1627710-50-2 |
|---|---|
| Molecular Formula | C22H21F2N3O |
| Molecular Weight | 381.42 g/mol |
| Purity | 99.64% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | OC1=C(F)C=C(C2=C(C3=CC=C(N4CCN(C)CC4)C=C3)C=CN=C2)C=C1F |
| Target | RSK1 |
| Signaling Pathway | MAPK/ERK Pathway; Apoptosis |
| Solubility | In Vitro: DMSO: ≥ 31 mg/mL (81.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| 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 | ≥ 31 mg/mL (81.28 mM) | 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 + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 1 mg/mL (2.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 1 mg/mL (2.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 1 mg/mL (2.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 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 (10.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In soft agar, LJH685 (0.01-100 μM; 72 hours) efficiently suppresses the growth of MDA-MB-231 and H358 cells, (EC50s of 0.73 and 0.79 μM, respectively)[1]. LJH685 (0.1-10 μM; 4 hours) effectively lowers YB1 phosphorylation at submicromolar concentrations and nearly completely inhibits it at higher concentrations[1].
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 EC50 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Discovery, delineation, and therapeutic targeting of a hyper-translation pathway driving cytokine release syndrome. Cell Rep Med 2025 Dec 30:102531. PMID: 41475340
YB-1 is a positive regulator of KLF5 transcription factor in basal-like breast cancer. Cell Death Differ 2022 Jun;29(6):1283-1295. PMID: 35022570
Punicalagin as a novel selective aryl hydrocarbon receptor (AhR) modulator upregulates AhR expression through the PDK1/p90RSK/AP-1 pathway to promote the anti-inflammatory response and bactericidal activity of macrophages. Cell Commun Signal 2024 Oct 3;22(1):473. PMID: 39363344
Inhibition of YB-1 phosphorylation enhances cisplatin activity and disrupts cell division in pleural mesothelioma. Br J Cancer 2025 Sep 4. PMID: 40908296
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
An integrated proteomic and phosphoproteomic landscape of chronic kidney disease. J Proteomics 2025 Jan 16:311:105355. PMID: 39547397
