LP-935509 是一种小分子衔接蛋白-2 相关激酶1 (AAK1) 选择性和脑渗透抑制剂 (IC50=3.3 nM)，一种 ATP 竞争性抑制剂，其 Ki 为 0.9 nM。 LP-935509 是 BIKE 的有效抑制剂 (IC50=14 nM) 和适度的 GAK 抑制剂 (IC50=320 nM)。 LP-935509 可逆转 SNL 手术后的疼痛。
LP-935509 is a small-molecule adapter protein-2 associated kinase 1 (AAK1) selective and brain-penetrantinhibitor (IC50=3.3 nM), a ATP-competitive inhibitor with a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure[1].
[1]. Kostich W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86.
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