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FR 180204

Catalog No. T1956 CAS 865362-74-9

Synonyms: FR180204

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

FR 180204, CAS 865362-74-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 78.00
10 mg	In stock	$ 140.00
25 mg	In stock	$ 233.00
50 mg	In stock	$ 349.00
100 mg	In stock	$ 523.00
1 mL * 10 mM (in DMSO)	In stock	$ 86.00

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Purity: 99.8%

Purity: 99.49%

Purity: 98%

Biological Description

Chemical Properties

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Description	FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.
Targets&IC50	ERK2:0.14 μM(Ki), ERK1:0.31 μM(Ki)
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)

Synonyms	FR180204
Molecular Weight	327.34
Formula	C18H13N7
CAS No.	865362-74-9

Storage

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

Solubility Information

DMSO: 32.7 mg/mL (100 mM)

References and Literature

1. Ohori M, et al. Biochem Biophys Res Commun. 2005, 336(1), 357-363. 2. Ohori M, et al. Naunyn Schmiedebergs Arch Pharmacol. 2007, 374(4), 311-316. 3. Honda M, et al. Cell Physiol Biochem. 2012, 29(5-6), 667-674. 4. Sreekanth GP, et al. Virus Res. 2014, 188, 15-26. 5. Lv, Jiawen, Junchao Zeng, Wen Zhao, Yuanxiong Cheng, Lin Zhang, Shaoxi Cai, Guodong Hu, and Yinghua Chen. Cdc42 regulates LPS-induced proliferation of primary pulmonary microvascular endothelial cells via ERK pathway [J]. Microvascular research . 2017 Jan;109:45-53 6. Lin H, Lu P, Zhou M, et al. Purification of recombinant human fibroblast growth factor 13 in E. coli and its molecular mechanism of mitogenesis[J]. Applied microbiology and biotechnology. 2019: 1-11.

Citations

1. Lin H, Lu P, Zhou M, et al. Purification of recombinant human fibroblast growth factor 13 in E. coli and its molecular mechanism of mitogenesis. Applied Microbiology and Biotechnology. 2019: 1-11

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Immunology/Inflammation Compound Library Apoptosis Compound Library Anti-Cancer Compound Library MAPK Inhibitor Library Anti-Aging Compound Library Bioactive Compound Library Anti-Liver Cancer Compound Library Autophagy Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

FR 180204 865362-74-9 Apoptosis MAPK ERK Extracellular signal regulated kinases FR-180204 FR180204 Inhibitor inhibit inhibitor

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