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FR 180204

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Purity:99.8%

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COA HNMR HPLC

FR 180204

Catalog No. T1956Cas No. 865362-74-9

FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.

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Pack Size	Price	Availability
1 mg	$36	In Stock
2 mg	$50	In Stock
5 mg	$78	In Stock
10 mg	$140	In Stock
25 mg	$233	In Stock
50 mg	$349	In Stock
100 mg	$523	In Stock
1 mL x 10 mM (in DMSO)	$86	In Stock

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Product Introduction

Bioactivity

Description	FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.
In vitro	In a mouse model of Dengue virus (DENV) infection, FR180204 was observed to restrict hepatocyte apoptosis, reduce DENV-induced liver damage, and enhance clinical parameters. Additionally, in mice with collagen-induced arthritis, FR180204 (100 mg/kg, i.p., b.i.d.) significantly mitigated the severity of symptoms and weight loss.
In vivo	FR 180204 inhibits the spontaneous growth of mesothelioma cells. In AP-1 transfected cells, FR180204 dose-dependently suppresses AP-1 transactivation, with an IC50 of 3.1 μM.
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.
Cell Research	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)
Alias	FR180204

Chemical Properties

Molecular Weight	327.34
Formula	C18H13N7
Cas No.	865362-74-9

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32.7 mg/mL (100 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0549 mL	15.2746 mL	30.5493 mL	152.7464 mL
5 mM	0.6110 mL	3.0549 mL	6.1099 mL	30.5493 mL
10 mM	0.3055 mL	1.5275 mL	3.0549 mL	15.2746 mL
20 mM	0.1527 mL	0.7637 mL	1.5275 mL	7.6373 mL
50 mM	0.0611 mL	0.3055 mL	0.6110 mL	3.0549 mL
100 mM	0.0305 mL	0.1527 mL	0.3055 mL	1.5275 mL

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