1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

FR 180204 

Cat. No.: HY-12275 Purity: 99.60%
Handling Instructions

FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 and ERK2, 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
10 mM * 1 mL in DMSO USD 117 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 106 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 186 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 874 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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    FR 180204 purchased from MCE. Usage Cited in: Inflammation. 2018 Feb 9.

    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.

    FR 180204 purchased from MCE. Usage Cited in: Cell Death Differ. 2018 May 21.

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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 and ERK2, respectively.

    IC50 & Target[1]

    ERK2

    0.14 μM (Ki)

    ERK1

    0.31 μM (Ki)

    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]

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.3055 mL 1.5275 mL 3.0549 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]

    FR180204 is ground and suspended in 0.1% methylcellulose solution to a volume of 5 mL/kg.

    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
    Molecular Weight

    327.34

    Formula

    C₁₈H₁₃N₇

    CAS No.

    865362-74-9

    SMILES

    NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 50 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    FR 180204
    Cat. No.:
    HY-12275
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