MW-150

Cas No.:	1628502-91-9
Chemical Name:	6-(4-methylpiperazin-1-yl)-3-(naphthalen-2-yl)-4-(pyridin-4-yl)pyridazine
Synonyms:	MW01-18-150SRM;MW 150;MW150
SMILES:	C1(C(C2=CC=NC=C2)=CC(N2CCN(C)CC2)=NN=1)C1C=C2C=CC=CC2=CC=1
Formula:	C24H23N5
M.Wt:	381.47
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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.

Description:	MW150 (MW01-18-150SRM) is a selective inhibitor of p38αMAPK isoform with a ki of 101 nM[1].
Target:	p38α:101 nM (Ki)
In Vivo:	MW150 (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]. MW150 (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: APP/PS1 transgenic (Tg) mouse (overexpresses amyloid-beta)[1] Dosage: 2.5 mg/kg Administration: Oral daily; 3-4 months (until cognitive impairment is present) Result: Improved the Tg mice performance in radial arm water maze (RAWM) and contextual fear conditioning tests.
In Vitro:	MW150 inhibits in a concentration-dependent manner the ability of the endogenous p38αMAPK to phosphorylate an endogenous substrate MK2 in activated glia[1]. MW150 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].
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.