Catalog Number: 3706
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
  • M.Wt:
    327.34
  • Formula:
    C18H13N7
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    865362-74-9
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.
Background References
  1. Signaling to Extracellular Signal-regulated Kinase from ErbB1 Kinase and Protein Kinase C.
    Perrett et al.
    J Biol Chem., 2013;19:288
  2. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex.
    Ohori et al.
    Biochem.Biophys.Res.Comm., 2005;336:357
Citations:

The citations listed below are publications that use Tocris products. Selected citations for FR 180204 include:

8 Citations: Showing 1 - 8
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  1. Neurogenin 3 is regulated by neurotrophic tyrosine kinase receptor type 2 (TRKB) signaling in the adult human exocrine pancreas
    Authors: Shamblott Et al.
    Cell Communication and Signaling 2016;14:23
  2. Neurogenin 3 is regulated by neurotrophic tyrosine kinase receptor type 2(TRKB) signaling in the adult human exocrine pancreas.
    Authors: Shamblott Et al.
    Cell Communication and Signaling 2016;14:23
  3. Inhibition of ERK1/2 down-regulates the Hippo/YAP signaling pathway in human NSCLC cells.
    Authors: You Et al.
    Oncotarget 2015;6:4357
  4. Terminal epidermal differentiation is regulated by the interaction of Fra-2/AP-1 with Ezh2 and ERK1/2.
    Authors: Wurm Et al.
    PLoS Biol 2015;29:144
  5. A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells.
    Authors: López-Cotarelo Et al.
    Proc Natl Acad Sci U S A 2015;290:827
  6. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    Microvasc Res 2014;171:5417
  7. HIF1A reduces acute lung injury by optimizing carbohydrate metabolism in the alveolar epithelium.
    Authors: Eckle Et al.
    J Biol Chem 2013;11:e1001665
  8. Post-transcriptional regulation of placenta growth factor mRNA by hydrogen peroxide.
    Authors: Shaw and Lloyd
    Genes Dev 2012;84:155

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