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Submit ReviewFR 180204
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% (HPLC)
Biological Activity for FR 180204
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).
Compound Libraries for FR 180204
FR 180204 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for FR 180204
| M. Wt | 327.34 |
| Formula | C18H13N7 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 865362-74-9 |
| PubChem ID | 11493598 |
| InChI Key | XVECMUKVOMUNLE-UHFFFAOYSA-N |
| Smiles | NC1=NNC2=C1C=C(C3=C(C=CC=C5)N5N=C3C4=CC=CC=C4)N=N2 |
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.
Solubility Data for FR 180204
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.73 | 100 |
Preparing Stock Solutions for FR 180204
The following data is based on the product molecular weight 327.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.05 mL | 15.27 mL | 30.55 mL |
| 5 mM | 0.61 mL | 3.05 mL | 6.11 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.05 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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Product Datasheets for FR 180204
References for FR 180204
References are publications that support the biological activity of the product.
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
Perrett et al (2013) Signaling to Extracellular Signal-regulated Kinase from ErbB1 Kinase and Protein Kinase C. J Biol Chem. 19 288 PMID: 23754287
If you know of a relevant reference for FR 180204, please let us know.
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Keywords: FR 180204, FR 180204 supplier, selective, ERK, inhibitors, inhibits, MAPK, signalling, signaling, ERK1, ERK2, FR180204, 3706, Tocris Bioscience
11 Citations for FR 180204
Citations are publications that use Tocris products. Selected citations for FR 180204 include:
Yuede et al (2021) Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease. J.Neurochem. 156 658 PMID: 33278025
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
Chaikuad et al (2014) A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nat Chem Biol 10 853 PMID: 25195011
Shaw and Lloyd (2012) Post-transcriptional regulation of placenta growth factor mRNA by hydrogen peroxide. Genes Dev 84 155 PMID: 22683469
Thotakura et al (2019) FGF Gradient Controls Boundary Position Between Proliferating and Differentiating Cells and Regulates Lacrimal Gland Growth Dynamics. Front Genet 10 362 PMID: 31191595
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
Garner et al (2018) Enhanced ins. receptor, but not PI3K, signalling protects podocytes from ER stress. Sci Rep 8 3902 PMID: 29500363
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
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
Do you know of a great paper that uses FR 180204 from Tocris? Please let us know.
Reviews for FR 180204
Average Rating: 5 (Based on 2 Reviews.)
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Used to block ERK signaling..
By
MARINA KOUTSIOUMPA on 10/13/2022
Assay Type: In Vitro
Species: Human
Pancreatic cancer cells were pretreated for 2 hours with FR 180204 followed by conventional chemotherapeutics. MEK inhibition had an additive effect on cancer cell’s viability upon 3 days of treatment.
FR 180204 blocks LPA induced COX-2 expression.
By
Anonymous on 12/13/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma
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.
Literature in this Area
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MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for FR 180204
