| 名称 | LP-935509 |
| 描述 | LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM). |
| 体外活性 | METHODS: The effects of LP-935509 on the activities of the two most closely related kinases, BIKE and GAK kinases, were evaluated; the ability of 1 μM LP-935509 to inhibit the binding of 389 kinases to ATP-binding probes was measured.
RESULTS LP-935509 is a potent inhibitor of BIKE (IC50= 14 nM) and a modest inhibitor of GAK (IC50= 320 ± 40 nM), and LP-935509 inhibited the binding of more than 70% of the probes to 13 kinases, including BIKE. [1] |
| 体内活性 | METHODS: LP-935509 (10, 30, and 60 mg/kg) was administered orally (10 ml/kg), and Von Frey tests were performed at 0, 30, and 120 min after administration.
RESULTS Oral administration of LP-935509 resulted in a dose-dependent reduction in phase II paw withdrawal that was significantly lower than that in vehicle-treated animals (Figure 3A). In particular, 30 mg/kg and 60 mg/kg of LP-935509 resulted in a significant reduction in pain behavior. [1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 175 mg/mL (441.43 mM), Sonication is recommended.
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| 关键字 | orally active | AP2-associated kinase 1 | Inhibitor | brain-penetrant | SARS coronavirus | LP 935509 | pain | spinal nerve ligation | SARS-CoV | Cyclin G-associated Kinase (GAK) | Antinociceptive | AAK1 | LP935509 | infection | chronic constriction injury | inhibit | streptozotocin | formalin | Auxilin 2 | LP-935509 | ATP-competitive | SNL | Adaptor-associated Kinase 1 |
| 相关产品 | Nafamostat mesylate | Piceatannol | SBC-115076 | Fasudil hydrochloride | Camostat mesylate | SRPIN340 | HA-1004 | FOY 251 | SGC-AAK1-1 | BMT-124110 Formate | Benzamidine hydrochloride | Cetraxate hydrochloride |
| 相关库 | 经典已知活性库 | 疼痛相关化合物库 | 神经信号分子库 | 激酶抑制剂库 | 抑制剂库 | 已知活性化合物库 | 抗癌化合物库 |
United States
