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BMS 911172 is an AP2-associated kinase 1 (AAK1) inhibitor that reduces the phosphorylation of AP-2 complex subunit mu2 (AP2M2) in HEK293 cells overexpressing AAK1 and AP2M2 (IC50 = 0.051 µM).1 It is selective for AAK1 over a panel of 219 kinases, including BMP2-inducible kinase (BIKE), cyclin G-associated kinase (GAK), and serine/threonine kinase 16 (STK16; IC50s = 0.120, 1.06, and 15.8 µM, respectively). BMS 911172 also inhibits AP2M2 phosphorylation in mouse brain lysates (ED50 = 6 mg/kg). In vivo, BMS 911172 (30 mg/kg) reduces formalin-induced paw flinching and biting in a rat model of persistent pain. It also reduces thermal and mechanical hyperalgesia, as well as cold and mechanical allodynia, in a rat model of chronic constriction injury when administered at a dose of 60 mg/kg.
WARNING This product is not for human or veterinary use.
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