J30-8 is a potent c-Jun N-terminal kinase JNK3 subtype-selective inhibtior (human JNK3 IC50 = 40 nM, JNK1α1 & JNK2α2 IC50 >100 μM) that exhibits excellent kinome-wide selectivity (IC50 >7.7 μM against 398 kinase targets) and neuroprotective efficacy against Aβ25-35 toxicity in SH-SY5Y cultures (1 μM). When compared with the pan-JNK inhibitor SP600125 in the APPswe/PS1dE9 murine AD model in vivo (30 mg/kg ip.), J30-8 offers superior therapeutic efficacy and pharmacokinetic properties with longer retention time (elimination t1/2 = 16.11 vs 1.23 hrs; plasma conc = 41 ng/mL vs 22 ng/mL 24 hr post ip.) and greater brain-permeability (brain/plasma ratio = 0.40 vs. 0.14 8 hr post ip.).
Potent JNK3 subtype-selective c-Jun N-terminal kinase inhibtior with superior in vivo efficacy, pharmacokinetics and brain-permeability in AD mice than SP600125.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Journal of medicinal chemistry, 62(14), 6645-6664 (2019-07-04)
Alzheimer's disease (AD) is one of the most challenging diseases around the world with no effective clinical treatment. Previous studies have suggested c-Jun N-terminal kinase 3 (JNK3) as an attractive therapeutic target for AD. Herein, we report 3-substituted indolin-2-one derivatives
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