2. MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Ribosomal S6 Kinase (RSK) YB-1
  4. LJI308

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.

For research use only. We do not sell to patients.

LJI308 Chemical Structure

LJI308 Chemical Structure

CAS No. : 1627709-94-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 198 In-stock
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 180 In-stock
10 mg USD 300 In-stock
25 mg USD 660 In-stock
50 mg USD 1188 In-stock
100 mg USD 1980 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

LJI308 Related Antibodies

Top Publications Citing Use of Products

    LJI308 purchased from MedChemExpress. Usage Cited in: Circulation. 2022 Nov 30.  [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.

    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).

    View All Ribosomal S6 Kinase (RSK) Isoform Specific Products:

    View All Isoforms
    p70S6K RSK1 RSK2 RSK3 RSK4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2].

    IC50 & Target

    RSK1

     

    RSK2

     

    RSK3

     

    In Vitro

    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.

    LJI308 Related Antibodies

    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%.
    Molecular Weight

    368.38

    Formula

    C21H18F2N2O2
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7146 mL 13.5729 mL 27.1459 mL
    5 mM 0.5429 mL 2.7146 mL 5.4292 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.07%

    COA (252 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References

    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
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    LJI308 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    LJI3081627709-94-7LJI 308LJI-308Ribosomal S6 Kinase (RSK)YB-1S6KY box binding protein 1mutationphosphorylationviabilitystimulationcancerdouble-strandbreaksInhibitorinhibitorinhibit

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