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LP-935509
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Catalog No. T15781Cas No. 1454555-29-3
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).
LP-935509
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Purity: 99.64%
Catalog No. T15781Cas No. 1454555-29-3
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).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $46 | In Stock | In Stock | |
| 10 mg | $80 | In Stock | In Stock | |
| 25 mg | $159 | In Stock | In Stock | |
| 50 mg | $296 | In Stock | In Stock | |
| 100 mg | $431 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $50 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.64%
Appearance:Solid
Color:White to Yellow
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Product Introduction
LP-935509 AI Summary
LP-935509 shows a high ratio of drug level in the brain to the drug level in the plasma in rats, with a Brain-to-Plasma Ratio (BPR) greater than 2.0. This indicates good potential for crossing the blood-brain barrier and exerting pharmacological effects in the brain. Additionally, LP-935509 inhibits the recombinant human GST-Xa-tagged-AAK1 protein with an IC50 value of 3.3 nM. The inhibition is achieved by blocking the activity of the substrate (5-FAM)-Aha-KEEQSQITSQVTGQIGWR-NH2 in the presence of ATP, over a 3-hour incubation period, as determined by electrophoretic analysis..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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). |
| Targets&IC50 | BIKE:14 nM, AAK1:0.9 nM(Ki), AAK1:3.3 nM, GAK:320 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] |
| Molecular Weight | 396.44 |
| Formula | C20H24N6O3 |
| Cas No. | 1454555-29-3 |
| Smiles | COc1ncccc1-c1cnn2ccc(nc12)N1CCN(CC1)C(=O)OC(C)C |
| Relative Density. | 1.34 g/cm3 (Predicted) |
| Storage | 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. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.09 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Keywords
threoninkinasethreonin kinasestreptozotocinspinal nerve ligationSNLSerinekinaseSerine kinaseSARS-CoVSARS coronaviruspainorally activeLP-935509LP935509LP 935509InhibitorinhibitinfectionGAKformalinCyclin G-associated Kinase (GAK)chronic constriction injurybrain-penetrantBIKEAuxilin 2ATP-competitiveAP2associatedkinase1AP2-associated kinase 1AP2 associated kinase 1AntinociceptiveAdaptor-associated Kinase 1AAK1(AP2associatedkinase1)AAK1 (AP2 associated kinase 1)AAK1
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