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Overview
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Background
ERK5-IN-1 is a potent and selective ERK5 inhibitor. In vitro, ERK5-IN-1 effectively inhibits ERK5 biochemically with an IC50 of 162 nM. In cell experiments, ERK5-IN-1 has a cellular EC50 for inhibiting epidermal growth factor induced ERK5 autophosphorylation of 0.09 μM. In cell-based analysis, it is at least 30 times more selective for ERK5 than LRRK2. It is also ERK5 selective for a group of other kinases. Available Oral Bioavailability.
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- Properties
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Overview