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J30-8 是一种高效的,具有亚型选择性的 JNK3 抑制剂,其 IC50 值为 40 nM,选择性比 JNK1α1 和 JNK2α2 亚型高 2500 倍。J30-8 在体外有神经保护活性,具有治疗神经退行性疾病的潜力。
J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases[1]. JNK3|40 nM (IC50)
[1]. Dou X, et al. Multistage Screening Reveals 3-Substituted Indolin-2-one Derivatives as Novel and Isoform-Selective c-Jun N-terminal Kinase 3 (JNK3) Inhibitors: Implications to Drug Discovery for Potential Treatment of Neurodegenerative Diseases. J Med Chem. 2019 Jul 25;62(14):6645-6664.
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