FR 180204

Cat. No. 3706

FR 180204 C18H13N7 [865362-74-9]

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Chemical Name: 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine

Biological Activity

Selective ERK inhibitor (IC50 values are 0.14 and 0.31 μM for ERK2 and ERK1 respectively). Displays 30-fold selectivity for ERK over p38α (IC50 = 10 μM); displays no activity against human recombinant MEK1, MKK4, IKKα, PKCα, Src, Syc and PDGFα at concentrations less than 30 μM. Also inhibits TGFβ-induced AP-1 activation in Mv1Lu cells (IC50 = 3.1 μM).

Technical Data

Soluble to 100 mM in DMSO
>98 %
Store at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Perrett et al (2013) Signaling to Extracellular Signal-regulated Kinase from ErbB1 Kinase and Protein Kinase C. J Biol Chem. 19 288. PMID: 23754287.

Ohori et al (2005) Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem.Biophys.Res.Comm. 336 357. PMID: 16139248.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for FR 180204 include:

Shamblott et al (2016) Neurogenin 3 is regulated by neurotrophic tyrosine kinase receptor type 2 (TRKB) signaling in the adult human exocrine pancreas Cell Communication and Signaling 14 23. PMID: 27659207.

López-Cotarelo et al (2015) A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells. Proc Natl Acad Sci U S A 290 827. PMID: 25425646.

Wurm et al (2015) Terminal epidermal differentiation is regulated by the interaction of Fra-2/AP-1 with Ezh2 and ERK1/2. PLoS Biol 29 144. PMID: 25547114.

You et al (2015) Inhibition of ERK1/2 down-regulates the Hippo/YAP signaling pathway in human NSCLC cells. Oncotarget 6 4357. PMID: 25738359.

Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Microvasc Res 171 5417. PMID: 25052197.

Eckle et al (2013) HIF1A reduces acute lung injury by optimizing carbohydrate metabolism in the alveolar epithelium. J Biol Chem 11 e1001665. PMID: 24086109.

Shaw and Lloyd (2012) Post-transcriptional regulation of placenta growth factor mRNA by hydrogen peroxide. Genes Dev 84 155. PMID: 22683469.

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Keywords: FR 180204, supplier, selective, ERK, inhibitors, inhibits, MAPK, signalling, signaling, ERK1, ERK2, FR180204, Tocris Bioscience, ERK Inhibitor products

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