LJI308
Based on 5 publication(s) in Google Scholar
LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation.
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- 純度: 99.07%
- CAS 番号: 1627709-94-7
- 分子式: C21H18F2N2O2
- 分子量:368.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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溶剤 & 溶解度
- 純度とドキュメンテーション
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生物活性
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RSK1 |
RSK2 |
RSK3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | EC50 |
19.1 μM
Compound: 3; LJI308
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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] |
| MOLM-13 | EC50 |
23.38 μM
Compound: 3; LJI308
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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] |
LJI308 inhibits S6K1 with an IC50 of 0.8 μM[1].
LJI308 inhibits YB-1 phosphorylation in CRC cells at concentrations of 5 to 25 μM. In a dose kinetics experiment, LJI308, starting at 2.5 μM, inhibits YB-1 phosphorylation in the KRAS mutated TNBC cell line MDA-MB-231 by approximately 86%. LJI308 effectively blocks RSK and YB-1 phosphorylation after EGF stimulation and after irradiation in KRAS wild-type HBL-100 cells[2].
LJI308 (1-10 μM; 96 hours) decreases cell viability by up to 90%[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HTRY-LT cell lines
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Concentration:1-10 μM
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Incubation Time:96 hours
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Result:Decreased cell viability by up to 90%.
化学情報
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CAS 番号 1627709-94-7
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性状 Solid
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分子量 368.38
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分子式 C21H18F2N2O2
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Color Light yellow to yellow
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SMILES
OC1=C(C=C(C=C1F)C2=C(C=CN=C2)C3=CC=C(C=C3)N4CCOCC4)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Circulation
Cannabinoid Receptor 2-Centric Molecular Feedback Loop Drives Necroptosis in Diabetic Heart Injuries. [Abstract]2023 Jan 10;147(2):158-174. PMID: 36448459
LJI308 purchased from MedChemExpress. Usage Cited in: Circulation. 2023 Jan 10;147(2):158-174. [Abstract]
Unlike HG (high glucose; 30 mM), which maintained the cytoplasm location of BACH2, LJI308 (1 μM), a specific inhibitor of S6K activity, shifts BACH2 to the nucleus location when cotreated with HG.
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Exp Hematol Oncol
Upregulated PARP1 confers breast cancer resistance to CDK4/6 inhibitors via YB-1 phosphorylation. [Abstract]2023 Nov 30;12(1):100. PMID: 38037159 -
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 -
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Oncotarget
Involvement of Polo-like kinase 1 (Plk1) in quiescence regulation of cancer stem-like cells of the gastric cancer cell lines. [Abstract]2017 Jun 6;8(23):37633-37645. PMID: 28430578
LJI308 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 6;8(23):37633-37645. [Abstract]
Western blot analysis of Plk1 and RSK1 activation in CSC-like cells after treatment with LJI308 for 72 hours. α-Tubulin served as a loading control (bottom panel).
溶剤 & 溶解度
DMSO : 25 mg/mL (67.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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データシート (279 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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]. Lettau K, et al. Simultaneous Targeting of RSK and AKT Efficiently Inhibits YB-1-Mediated Repair of Ionizing Radiation-Induced DNA Double-Strand Breaks in Breast Cancer Cells. Int J Radiat Oncol Biol Phys. 2021;109(2):567-580. [Content Brief]
[3]. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015;6(24):20570-20577. [Content Brief]
[4]. 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]
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 | 2.7146 mL | 13.5729 mL | 27.1459 mL | 67.8647 mL |
| 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL | 13.5729 mL | |
| 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL | 6.7865 mL | |
| 15 mM | 0.1810 mL | 0.9049 mL | 1.8097 mL | 4.5243 mL | |
| 20 mM | 0.1357 mL | 0.6786 mL | 1.3573 mL | 3.3932 mL | |
| 25 mM | 0.1086 mL | 0.5429 mL | 1.0858 mL | 2.7146 mL | |
| 30 mM | 0.0905 mL | 0.4524 mL | 0.9049 mL | 2.2622 mL | |
| 40 mM | 0.0679 mL | 0.3393 mL | 0.6786 mL | 1.6966 mL | |
| 50 mM | 0.0543 mL | 0.2715 mL | 0.5429 mL | 1.3573 mL | |
| 60 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1311 mL |
LJI308 関連分類
HY-19713 関連分類
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