MW-150 (MW01-18-150SRM) 是一种选择性，口服有效的，可透过神经系统的 p38α MAPK 抑制剂，Ki 值为 101 nM。MW-150 抑制内源性 p38α MAPK 在活化的神经胶质中磷酸化内源性底物 MK2 的能力。
货号:ajcx39304
CAS:1628502-91-9
分子式:C24H23N5
分子量：381.47
溶解度:DMSO : 40 mg/mL (104.86 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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].

[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.