LP-935509 |
رقم الكتالوجGC39256 |
LP-935509 هو مثبط فعال عن طريق الفم وانتقائي ومنافس للأدينوزين ثلاثي الفوسفات (ATP) وذو قدرة اختراق للدماغ، لبروتين المحول المهاجر 2 المرتبط بالأدابتور كيناز 1 (AAK1) بـ IC50 يبلغ 3.3 نانومتر و Ki يبلغ 0.9 نانومتر على التوالي.
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Cas No.: 1454555-29-3
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
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