DLK-IN-1是双亮氨酸拉链激酶(DLK,MAP3K12)的选择性抑制剂,其Ki值为3nM。DLK-IN-1保持着良好的中枢神经系统穿透能力,并且在脑内剂量过量后依旧耐受性良好,在阿尔兹海默症动物模型中有良好的活性。
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DLK-IN-1 is a selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer's Disease.
[1]. Patel S, et al. Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease. J Med Chem. 2017 Oct 12;60(19):8083-8102.
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