Potent and selective ERK5 inhibitor; inhibits EGFR-induced ERK5 autophosphorylation (EC50 = 90 nM) and ERK5 enzymatic activity (IC50 = 162 nM). Exhibits at least 30-fold selectivity for ERK5 over LRRK2 in a cell based assay. Also selective for ERK5 over a panel of other kinases. Orally bioavailable.
Sold under license from Dana-Farber Cancer Institute.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 638.8. 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||1.57 mL||7.83 mL||15.65 mL|
|5 mM||0.31 mL||1.57 mL||3.13 mL|
|10 mM||0.16 mL||0.78 mL||1.57 mL|
|50 mM||0.03 mL||0.16 mL||0.31 mL|
References are publications that support the products' biological activity.
Deng et al (2013) Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur.J.Med.Chem. 70 758 PMID: 24239623
Elkins et al (2013) X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J.Med.Chem. 56 4413 PMID: 23656407
If you know of a relevant reference for ERK5-IN-1, please let us know.
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Keywords: ERK5-IN-1, supplier, potent, selective, ERK5, extracellular, regulated, kinases, MAPK7, inhibitors, inhibits, ERK, ERK, Tocris Bioscience
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Literature in this Area
MAPK Signaling Scientific Review
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.