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).
Compound Libraries
FR 180204 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.73 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 327.34. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
Keywords: FR 180204, supplier, selective, ERK, inhibitors, inhibits, MAPK, signalling, signaling, ERK1, ERK2, FR180204, ERK, ERK, Tocris Bioscience
