Topic summary
ERK5
Extracted from the Wikipedia article MAPK7.
ERK5 (= MAPK7) Inhibitors
XMD8-92 was one of the first described ERK5 inhibitors and was used in several pharmacological studies as tool compound. However, XMD8-92 hits BRD4 as an off-target leading to false or inconclusive results. Consequently, ERK5 inhibitors with improved selectivity (void of the BRD4 off-target effect) such as AX15836 and BAY-885 were developed and should preferably be used for future pharmacological studies. BAY-885 fulfils the quality criteria for a 'Donated Chemical Probe' as defined by the Structural Genomics Consortium. In 2020, it was demonstrated that ATP-competitive inhibitors paradoxically activate ERK5 signalling. A recent review discussed the modulation of ERK5 activity as a therapeutic anti-cancer strategy.