| Bioactivity | MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia[1]. | ||||||||||||
| Invitro | 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 APPNLh/NLh × PSP264L/P264L knock-in mouse (with no overexpression of the amyloid precursor protein) exhibits RAWM behavior indistinguishable from WT mice[1]. Animal Model: | ||||||||||||
| Name | MW-150 | ||||||||||||
| CAS | 1628502-91-9 | ||||||||||||
| Formula | C24H23N5 | ||||||||||||
| Molar Mass | 381.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Roy SM, et al. Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimer's disease mouse models. ACS Chem Neurosci. 2015 Apr 15;6(4):666-80. |