ERK5-IN-1

Key Product Details

Product Description

ERK5-IN-1 is a 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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Product Specifications for ERK5-IN-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for ERK5-IN-1

The following data is based on the product molecular weight 638.80.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Elkins X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J.Med.Chem. 2013 PMID: 23656407
• Deng 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. 2013 PMID: 24239623

Product Documents for ERK5-IN-1