Bioactivity | BMS-901715 is a potent and selective adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 of 3.3 nM[1][2]. |
Target | IC50: 3.3 nM (Adapter protein-2 associated kinase 1 (AAK1)) |
Invitro | Adaptor associated kinase 1 (AAK1) is a member of the Ark1/Prk1 family of serine/threonine kinases. AAK1 mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAK1 is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAK1 modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[2]. |
Name | BMS-901715 |
CAS | 1699861-37-4 |
Formula | C22H28N10O |
Molar Mass | 448.52 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [2]. Carolyn Diane Dzierba, et al. Pyrrolotriazine kinase inhibitors. WO2015054358A1. |