LJH685
Based on 6 publication(s) in Google Scholar
LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.64%
- CAS No.: 1627710-50-2
- 화학식: C22H21F2N3O
- 분자량:381.42
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) LJH685
More
Biological Activity
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RSK1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | EC50 |
22 μM
Compound: 2; LJH685
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Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTox green assay
Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTox green assay
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[PMID: 31982240] |
| MOLM-13 | EC50 |
9.71 μM
Compound: 2; LJH685
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Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 31982240] |
LJH685 (0.01-100 μM; 72 hours) efficiently inhibits the growth of MDA-MB-231 and H358 cells in soft agar with EC50s 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, H358 cells
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Concentration:0.01, 0.1, 1, 10, 100 μM
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Incubation Time:72 hours
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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.
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Cell Line:MDA-MB-231, H358 cells
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Concentration:0.1, 0.3, 1, 3, 10 μM
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Incubation Time:4 hours
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Result:Efficiently reduced phosphorylation of YB1 at submicromolar concentrations and caused nearly complete inhibition at higher concentrations.
Chemical Information
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CAS No. 1627710-50-2
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Appearance Solid
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분자량 381.42
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화학식 C22H21F2N3O
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Color White to off-white
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SMILES
OC1=C(F)C=C(C2=C(C3=CC=C(N4CCN(C)CC4)C=C3)C=CN=C2)C=C1F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Discovery, delineation, and therapeutic targeting of a hyper-translation pathway driving cytokine release syndrome. [Abstract]2025 Dec 30:102531. PMID: 41475340 -
Cell Death Differ
2022 Jun;29(6):1283-1295. PMID: 35022570 -
Cell Commun Signal
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. [Abstract]2024 Oct 3;22(1):473. PMID: 39363344 -
Br J Cancer
Inhibition of YB-1 phosphorylation enhances cisplatin activity and disrupts cell division in pleural mesothelioma. [Abstract]2025 Sep 4. PMID: 40908296 -
J Invest Dermatol
Inhibition of the Extracellular Signal-Regulated Kinase/Ribosomal S6 Kinase Cascade Limits Chlamydia trachomatis Infection. [Abstract]2021 Apr;141(4):852-862.e6. PMID: 32918951 -
J Proteomics
2025 Jan 16:311:105355. PMID: 39547397
용액&용해도
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.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.62 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.62 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6218 mL | 13.1089 mL | 26.2178 mL | 65.5445 mL |
| 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | 13.1089 mL | |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL | 6.5545 mL | |
| 15 mM | 0.1748 mL | 0.8739 mL | 1.7479 mL | 4.3696 mL | |
| 20 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2772 mL | |
| 25 mM | 0.1049 mL | 0.5244 mL | 1.0487 mL | 2.6218 mL | |
| 30 mM | 0.0874 mL | 0.4370 mL | 0.8739 mL | 2.1848 mL | |
| 40 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6386 mL | |
| 50 mM | 0.0524 mL | 0.2622 mL | 0.5244 mL | 1.3109 mL | |
| 60 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0924 mL | |
| 80 mM | 0.0328 mL | 0.1639 mL | 0.3277 mL | 0.8193 mL |
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