J30-8，5MG，SML2688-5MG，Sigma

Biochem/physiol Actions

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 t_1/2 = 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.