MW-150

MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a K_i of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia^[1]. IC50 & Target: Ki: 101nM (p38α MAPK)^[1] In Vitro: MW-150 inhibits in a concentration-dependent manner the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia^[1].
MW-150 blocks in a concentration-dependent manner the increased IL-1β production by activated glia. The IC₅₀ values are 332 nM and 936 nM for MK2 and IL-1β, respectively^[1]. In Vivo: MW-150 (2.5 mg/kg; oral daily for 3-4 months) improves the APP/PS1 transgenic (Tg) mice performance in radial arm water maze (RAWM) and contextual fear conditioning tests^[1].
MW-150 (2.5 mg/kg; given i.p.; daily for 14 days) treatment in APP^NLh/NLh × PS^P264L/P264L knock-in mouse (with no overexpression of the amyloid precursor protein) exhibits RAWM behavior indistinguishable from WT mice^[1].