| Name | LP-935509 |
| Description | 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). |
| In vitro | 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] |
| In vivo | 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 175 mg/mL (441.43 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (10.09 mM), Sonication is recommended.
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| Keywords | threoninkinase | threonin kinase | streptozotocin | spinal nerve ligation | SNL | Serinekinase | Serine kinase | SARS-CoV | SARS coronavirus | pain | orally active | LP-935509 | LP935509 | LP 935509 | Inhibitor | inhibit | infection | GAK | formalin | Cyclin G-associated Kinase (GAK) | chronic constriction injury | brain-penetrant | BIKE | Auxilin 2 | ATP-competitive | AP2associatedkinase1 | AP2-associated kinase 1 | AP2 associated kinase 1 | Antinociceptive | Adaptor-associated Kinase 1 | AAK1(AP2associatedkinase1) | AAK1 (AP2 associated kinase 1) | AAK1 |
| Inhibitors Related | Nirmatrelvir | EIDD-1931 | Remdesivir | Molnupiravir | Silymarin | Umifenovir hydrochloride | Hydroxychloroquine | Ritonavir | Chloroquine phosphate | Dexamethasone acetate | α-Cyclodextrin | Dexamethasone |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Kinase Inhibitor Library | Multi-Target Compound Library | Anti-Viral Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Metabolism Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library |
United States
