FR 180204

Catalog No.S7524

FR 180204 Chemical Structure

Molecular Weight(MW): 327.34

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

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1 Customer Review

  • ERK1/2 inhibition reverse EMT in H1299- EML4-ALK cells. H1299-EML4-ALK cells were treated with FR180204 (10 μM), crizotinib (10 nM) and S3I-201(20 μM) for 24 h, cell extracts were analyzed by immunoblotting.

    Biochem Biophys Res Commun, 2015, 459(3): 398-404. FR 180204 purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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.
Features ERK1/ERK2-selective inhibitor
Targets
ERK2 [1] ERK1 [1]
0.14 μM(Ki) 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 In collagen-induced arthritis mice, FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss. [2] In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves Clinical parameters. [4]

Protocol

Kinase Assay:[1]
+ Expand

ERK assay:

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 were incubated for 30 min. SuperSignal chemiluminescent substrate is used for the measurement of HRP activity according to the manufacturer’s instructions. Prism 4.0 software is used for the Lineweaver–Burk plot analysis, IC50 and Ki determinations.
Cell Research:[3]
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  • Cell lines: Met5A, MSTO-211H, NCI-H28, NCI-H2052, and NCIH2452 cell lines
  • Concentrations: 10 μM
  • Incubation Time: 48 hours
  • Method: Cell viability is assayed by the method using MTT. MTT-reactive cells are quantified at an absorbance of 570 nm using a micro-plate reader.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Collagen-induced arthritis mouse model
  • Formulation: Suspended in 0.1% methylcellulose solution
  • Dosages: 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 65 mg/mL (198.57 mM)
Ethanol 2 mg/mL warmed (6.1 mM)
Water <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 327.34
Formula

C18 H13 N7

CAS No. 865362-74-9
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID