FR 180204

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 (11)
Reviews (1)

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for FR 180204

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

11 Citations: Showing 1 - 10

  1. 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
  2. Enhanced ins. receptor, but not PI3K, signalling protects podocytes from ER stress.
    Authors: Garner Et al.
    Sci Rep  2018;8:3902
  3. 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
  4. 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
  5. Inhibition of ERK1/2 down-regulates the Hippo/YAP signaling pathway in human NSCLC cells.
    Authors: You Et al.
    Oncotarget  2015;6:4357
  6. 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
  7. 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
  8. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    Microvasc Res  2014;171:5417
  9. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.
    Authors: Chaikuad Et al.
    Nat Chem Biol  2014;10:853
  10. HIF1A reduces acute lung injury by optimizing carbohydrate metabolism in the alveolar epithelium.
    Authors: Eckle Et al.
    J Biol Chem  2013;11:e1001665

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FR 180204 blocks LPA induced COX-2 expression
By Anonymous on 12/13/2018
Species: Human

MG-63 cells were pre-incubated with 10 µM FR 180204 for 30 min followed by treatment with 10 µM LPA for 3 h to follow COX-2 expression using Western blot. FR 180204 inhibited COX-2 induction by LPA.


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