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MW-150 dihydrochloride dihydrate

Names

[ CAS No. ]:
1661020-92-3

[ Name ]:
MW-150 dihydrochloride dihydrate

Biological Activity

[Description]:

MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective inhibitor of p38αMAPK isoform with a ki of 101 nM[1].

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Research Areas >> Neurological Disease

[Target]

p38α:101 nM (Ki)


[In Vitro]

MW-150 dihydrochloride dihydrate inhibits in a concentration-dependent manner the ability of the endogenous p38αMAPK to phosphorylate an endogenous substrate MK2 in activated glia[1]. MW-150 dihydrochloride dihydrate 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 dihydrochloride dihydrate (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 dihydrochloride dihydrate (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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H29Cl2N5O2

[ Molecular Weight ]:
490.43

[ Storage condition ]:
2-8℃


Related Compounds

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