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Description: BAY-885 is a novel, highly potent and selective ERK5/MAPK7 inhibitor with IC50 of 40 nM. The availability of a chemical probe to study the role of a specific domain of a protein in a concentration- and time-dependent manner is of high value. BAY-885 was identified by high-throughput screening and subsequent structure-based optimization. ERK5 is a key integrator of cellular signal transduction, and it has been shown to play a role in various cellular processes such as proliferation, differentiation, apoptosis, and cell survival. The inhibition of ERK5 kinase and transcriptional activity with a small molecule did not translate into antiproliferative activity in different relevant cell models, which is in contrast to the results obtained by RNAi technology.
References: J Med Chem. 2019 Jan 24; 62(2):928-940.
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