An inhibitor of p38α MAPK
MW-150 is an inhibitor of p38α MAPK (Ki = 101 nM).1 It is 6-, 10-, and 14-fold selective for p38α MAPK over the serine/threonine protein kinase NLK, p38β MAPK, and p38δ MAPK, respectively, and is also selective over the enzymatically normal mutant p38α MAPKT106M. It inhibits p38α MAPK phosphorylation of the endogenous substrate MAPK-activated protein kinase 2 (MK2) in LPS-activated glia in a concentration-dependent manner and decreases the levels of IL-1β in the same cells. MW-150 (2.5 mg/kg per day, i.p.) reduces the number of errors made in the spatial reference memory version of the radial arm water maze in aged amyloid precursor protein/presenilin 1 (APP/PS1) knock-in mice as a model of Alzheimer’s disease.
1.Roy, S.M., Grum-Tokars, V.L., Schavocky, J.P., et al.Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimer's disease mouse modelsACS Chem. Neurosci.6(4)666-680(2015)
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