Home / ERK Inhibitors / FR 180204

FR 180204

Catalog #: 3706
23 Citations Datasheet
Catalog # Availability Size / Price Qty
3706/10
3706/50
FR 180204 | CAS No. 865362-74-9 | ERK Inhibitors
1 Image
Description: Selective ERK inhibitor

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

Purity: ≥98%

Product Details
Citations (23)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

FR 180204 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Amyloid beta (Abeta) peptide directly activates amylin-3 receptor subtype by triggering multiple intracellular signaling pathways.
    Fu W, Ruangkittisakul A, MacTavish D, Shi JY, Ballanyi K, Jhamandas JH
    J. Biol. Chem., 2012;287(22):18820-30.
  2. RSPO-LGR4 functions via IQGAP1 to potentiate Wnt signaling.
    Carmon K, Gong X, Yi J, Thomas A, Liu Q
    Proc Natl Acad Sci U S A, 2014;111(13):E1221-9.
  3. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex.
    Ohori et al.
    Biochem.Biophys.Res.Comm., 2005;336:357
  4. Signaling to Extracellular Signal-regulated Kinase from ErbB1 Kinase and Protein Kinase C.
    Perrett et al.
    J Biol Chem., 2013;19:288

Product Datasheets

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Citations for FR 180204

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

23 Citations: Showing 1 - 10

  1. ERK contributes to B cell receptor-induced cell spreading in the A20 mouse B cell line.
    Authors: Michael R Et al.
    MicroPubl Biol  2022;2022
  2. PD-1-induced T cell exhaustion is controlled by a Drp1-dependent mechanism.
    Authors: Claudio Et al.
    Mol Oncol  2022;16:188-205
  3. Corticostriatal dysfunction and social interaction deficits in mice lacking the cystine/glutamate antiporter.
    Authors: Lutgarde Et al.
    Mol Psychiatry  2021;26:4754-4769
  4. Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease.
    Authors: Yuede Et al.
    J.Neurochem.  2021;156:658
  5. Acute effects of cell stretch on keratin filaments in A549 lung cells.
    Authors: Edward Et al.
    FASEB J  2020;34:11227-11242
  6. Polypharmacological Perturbation of the 14-3-3 Adaptor Protein Interactome Stimulates Neurite Outgrowth.
    Authors: Alyson E Et al.
    Cell Chem Biol  2020;27:657-667.e6
  7. JNK1 and ERK1/2 modulate lymphocyte homeostasis via BIM and DRP1 upon AICD induction.
    Authors: Benedetta Et al.
    Cell Death Differ  2020;27:2749-2767
  8. Serotonin Receptor 2A Activation Promotes Evolutionarily Relevant Basal Progenitor Proliferation in the Developing Neocortex.
    Authors: Wieland B Et al.
    Neuron  2020;108:1113-1129.e6
  9. Direct Reprogramming of Human Neurons Identifies MARCKSL1 as a Pathogenic Mediator of Valproic Acid-Induced Teratogenicity.
    Authors: Thomas C Et al.
    Cell Stem Cell  2019;25:103-119.e6
  10. Trapping, tagging and tracking: Tools for the study of proteins during early development of the sea urchin.
    Authors: Gary Et al.
    Methods Cell Biol  2019;151:283-304
  11. FGF Gradient Controls Boundary Position Between Proliferating and Differentiating Cells and Regulates Lacrimal Gland Growth Dynamics.
    Authors: Thotakura Et al.
    Front Genet  2019;10:362
  12. Extracellular Matrix Components HAPLN1, Lumican, and Collagen I Cause Hyaluronic Acid-Dependent Folding of the Developing Human Neocortex.
    Authors: Wieland B Et al.
    Neuron  2018;99:702-719.e6
  13. Enhanced ins. receptor, but not PI3K, signalling protects podocytes from ER stress.
    Authors: Garner Et al.
    Sci Rep  2018;8:3902
  14. 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
  15. 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
  16. Inhibition of ERK1/2 down-regulates the Hippo/YAP signaling pathway in human NSCLC cells.
    Authors: You Et al.
    Oncotarget  2015;6:4357
  17. Dynamic membrane depolarization is an early regulator of ependymoglial cell response to spinal cord injury in axolotl.
    Authors: Tiago Et al.
    Dev Biol  2015;408:14-25
  18. 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
  19. 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
  20. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    Microvasc Res  2014;171:5417
  21. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.
    Authors: Chaikuad Et al.
    Nat Chem Biol  2014;10:853
  22. HIF1A reduces acute lung injury by optimizing carbohydrate metabolism in the alveolar epithelium.
    Authors: Eckle Et al.
    J Biol Chem  2013;11:e1001665
  23. Post-transcriptional regulation of placenta growth factor mRNA by hydrogen peroxide.
    Authors: Shaw and Lloyd
    Genes Dev  2012;84:155

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