2. Anti-infection MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. Dengue virus Flavivirus ERK Apoptosis
  4. FR 180204

FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively.

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

FR 180204 Chemical Structure

FR 180204 Chemical Structure

CAS No. : 865362-74-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 129 In-stock
Solution
10 mM * 1 mL in DMSO USD 129 In-stock
Solid
5 mg USD 117 In-stock
10 mg USD 187 In-stock
50 mg USD 720 In-stock
100 mg USD 1150 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 18 publication(s) in Google Scholar

FR 180204 Related Antibodies

Top Publications Citing Use of Products

    FR 180204 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2019 Mar;26(3):426-442.  [Abstract]

    Chicken breast muscles are injected with FR180204 or control, and the protein levels of the ERK1 and p-ERK are analysed.

    FR 180204 purchased from MedChemExpress. Usage Cited in: Inflammation. 2018 Jun;41(3):751-759.  [Abstract]

    ERK1/2-specific inhibitor (FR 180204) is responsible for the inhibition of FGF21-induced IL-10 expression without affecting the viability of the THP-1 cells.

    View All ERK Isoform Specific Products:

    View All Isoforms
    ERK ERK1 ERK2 ERK5 ERK8

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively[1].

    IC50 & Target[1]

    ERK2

    0.14 μM (Ki)

    ERK1

    0.31 μM (Ki)

    ERK2

    0.33 μM (IC50)

    ERK1

    0.51 μM (IC50)

    In Vitro

    In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC50 of 3.1 μM[1].?FR 180204 inhibits spontaneous mesothelioma cell growth[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    FR 180204 Related Antibodies
    In Vivo

    FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss in collagen-induced arthritis mice[2].?In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves clinical parameters[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    327.34

    Formula

    C18H13N7
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21
    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 : ≥ 50 mg/mL (152.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0549 mL 15.2746 mL 30.5493 mL
    5 mM 0.6110 mL 3.0549 mL 6.1099 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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: 99.64%

    COA (257 KB) HNMR (270 KB) LCMS (268 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Nunc-Immuno MaxiSorp plates are coated with 20 μg/mL MBP solution in phosphate-buffered saline (PBS). After washing with PBS containing 0.05% Tween 20 (T-PBS), blocking buffer (T-PBS containing 3% BSA) is added to each well and the plates are incubated for 10 min at room temperature. After washing with T-PBS, chemical compounds, ATP and recombinant ERK2 diluted in assay dilution buffer (20 mM Mops, pH 7.2, 25 mM β-glycerol phosphate, 5 mM EGTA, 1 mM sodium orthovanadate, 1 mM dithiothreitol, and 50 μg/mL BSA) and are added to each well. Vehicle groups (containing 0.1% DMSO) and kinase-withdrawal groups are used for the control and basal determinations. After incubation for 1 h at room temperature, plates are washed twice with T-PBS. Anti-phospho MBP antibody (0.2 μg/mL) is added to each well, and the plates are incubated for 1 h at room temperature. After washing, anti-mouse HRP-conjugated polyclonal antibodies are added and the plates are incubated for 30 min.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    In brief, mice are randomized and grouped by body weight immediately before treatment. Bovine CII is dissolved in 0.1mol/Lacetic acid at the concentration of 10 mg/mL and then emulsified in an equal volume of Freund’s complete adjuvant H37Rv. Apart from a naive group, each mouse is immunized with 25 μL of the CII emulsion into the tail base, followed by a boost injection 3 weeks after primary injection (day 0). FR180204 and methylprednisolone are ground and suspended in 0.1% methylcellulose solution to a volume of 5 mL/kg. Drugs are given by twice daily intraperitoneal injection from days 0 to 12 in accordance with pharmacokinetic studies with superior area under the curve and Cmax values of i.p. versus s.c. or p.o. administration. The initial administration is 30 min before the boost CII injection. The clinical score of arthritis is obtained by summing the visual severity grade of each limb, scored as follows: 0, no arthritis; 1, one swollen digit; 2, two or more swollen digits or swelling of the entire paw without ankylosis; 3, gross swelling with ankylosis of the paw. Body weight is measured on day 12.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 3.0549 mL 15.2746 mL 30.5493 mL 76.3732 mL
    5 mM 0.6110 mL 3.0549 mL 6.1099 mL 15.2746 mL
    10 mM 0.3055 mL 1.5275 mL 3.0549 mL 7.6373 mL
    15 mM 0.2037 mL 1.0183 mL 2.0366 mL 5.0915 mL
    20 mM 0.1527 mL 0.7637 mL 1.5275 mL 3.8187 mL
    25 mM 0.1222 mL 0.6110 mL 1.2220 mL 3.0549 mL
    30 mM 0.1018 mL 0.5092 mL 1.0183 mL 2.5458 mL
    40 mM 0.0764 mL 0.3819 mL 0.7637 mL 1.9093 mL
    50 mM 0.0611 mL 0.3055 mL 0.6110 mL 1.5275 mL
    60 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2729 mL
    80 mM 0.0382 mL 0.1909 mL 0.3819 mL 0.9547 mL
    100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
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    FR 180204 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:

    FR 180204865362-74-9FR180204FR-180204Dengue virusFlavivirusERKApoptosisDENVExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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