Home MAPK ERK inhibitor FR 180204

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FR 180204 ERK inhibitor

Cat.No.S7524

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.
FR 180204 ERK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 327.34

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Quality Control

Batch: S752401 DMSO]65 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 100.00%
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  • NMR
  • HPLC
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100.00

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (198.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 327.34 Formula

C18 H13 N7

 Storage (From the date of receipt)
CAS No. 865362-74-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C=C1)C2=NN3C=CC=CC3=C2C4=CC5=C(NN=C5N=N4)N

Mechanism of Action

Features
ERK1/ERK2-selective inhibitor
Targets/IC50/Ki
ERK2
(Cell-free assay)
0.14 μM(Ki)
ERK1
( Cell-free assay)
0.31 μM(Ki)
In vitro
In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC50 of 3.1 μM. FR 180204 inhibits spontaneous mesothelioma cell growth.
Kinase Assay
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.
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. In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves Clinical parameters.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/24704674/

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