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 biological activity of the product.
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.
View Related Products by Product Action
Keywords: ERK5-IN-1, ERK5-IN-1 supplier, potent, selective, ERK5, extracellular, regulated, kinases, MAPK7, inhibitors, inhibits, ERK, 5393, Tocris Bioscience
Citations for ERK5-IN-1
Citations are publications that use Tocris products.
Currently there are no citations for ERK5-IN-1. Do you know of a great paper that uses ERK5-IN-1 from Tocris? Please let us know.
Reviews for ERK5-IN-1
There are currently no reviews for this product. Be the first to review ERK5-IN-1 and earn rewards!
Have you used ERK5-IN-1?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.