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TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. It does not inhibit CaMKK isoforms. By inhibiting AAK1 kinase activity, TIM-098a disrupts AAK1-regulated endocytosis.
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| Description | TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. It does not inhibit CaMKK isoforms. By inhibiting AAK1 kinase activity, TIM-098a disrupts AAK1-regulated endocytosis. |
| Targets&IC50 | BIKE:5.99 μM, AAK1:0.24 μM, STK16:7.15 μM, GAK:1.04 μM |
| In vitro | TIM-098a effectively inhibits AAK1 activity in transfected cultured cells with an IC50 of 0.87 µM. In COS-7 cells expressing AAK1/GST-AP2μ2 (145-162), TIM-098a (0.26, 0.82, 2.6, 26 μM; 6 hours) suppresses AAK1-catalyzed phosphorylation of GST-AP2μ2 (145-162) Thr156 in a concentration-dependent manner. Furthermore, TIM-098a (10 μM; 6 hours) restores early endosome numbers in AAK1-transfected cells to levels observed in non-transfected wild-type cells. |
| Formula | C18H11N3O2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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