FR 180204

Catalog No.S7524 Batch:S752401

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Technical Data

Formula

C18 H13 N7
Molecular Weight 327.34 CAS No. 865362-74-9
Solubility (25°C)* In vitro DMSO 65 mg/mL (198.57 mM)
Ethanol 2 mg/mL (6.1 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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. It is 30-fold less potent against the related kinase p38α and failed to inhibit any kinases(MEK1, MKK4, IKKα, PKCα, Src, Syc, and PDGFα) at less than 30 μM.
Targets
ERK2 [1]
(Cell-free assay)		 ERK1 [1]
( Cell-free assay)
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]
Features ERK1/ERK2-selective inhibitor

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[3]
  • 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.
Animal Study:

[2]
  • Animal Models

    Collagen-induced arthritis mouse model

  • Dosages

    100 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2015, 459(3): 398-404]

Selleck's FR 180204 has been cited by 43 publications

Photobiomodulation inhibits the expression of chondroitin sulfate proteoglycans after spinal cord injury via the Sox9 pathway [ Neural Regen Res, 2024, 19(1):180-189] PubMed: 37488865
HDAC Inhibition Restores Response to HER2-Targeted Therapy in Breast Cancer via PHLDA1 Induction [ Int J Mol Sci, 2023, 24(7)6228] PubMed: 37047202
ERK1/2 inhibitors act as monovalent degraders inducing ubiquitylation and proteasome-dependent turnover of ERK2, but not ERK1 [ Biochem J, 2023, 480(9):587-605] PubMed: 37018014
Mycobacterium tuberculosis resides in lysosome-poor monocyte-derived lung cells during persistent infection [ bioRxiv, 2023, 2023.01.19.524758] PubMed: 36711606
Nuclear FGFR1 promotes pancreatic stellate cell-driven invasion through up-regulation of Neuregulin 1 [ Oncogene, 2022, 10.1038/s41388-022-02513-5] PubMed: 36357571
Reactive Oxygen Species are Essential for Placental Angiogenesis During Early Gestation [ Oxid Med Cell Longev, 2022, 2022:4290922] PubMed: 35693704
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Chicken cathelicidin-2 promotes IL-1β secretion via the NLRP3 inflammasome pathway and serine proteases activity in LPS-primed murine neutrophils [ Dev Comp Immunol, 2022, 131:104377] PubMed: 35189160
Treatment of Retinoblastoma 1-Intact Hepatocellular Carcinoma With Cyclin-Dependent Kinase 4/6 Inhibitor Combination Therapy [ Hepatology, 2021, 74(4):1971-1993] PubMed: 33931882
Combined FGFR and Akt pathway inhibition abrogates growth of FGFR1 overexpressing EGFR-TKI-resistant NSCLC cells [ NPJ Precis Oncol, 2021, 5(1):65] PubMed: 34267282

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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