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DYRK1-IN-1
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Catalog No. T60334Cas No. 2814486-79-6
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor that inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. It exhibits good permeability and cellular activity without P-glycoprotein liability, making it suitable for research on central nervous system penetrant DYRK1A chemical probes [1].
DYRK1-IN-1
Copy Product Info😃Good
Catalog No. T60334Cas No. 2814486-79-6
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor that inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. It exhibits good permeability and cellular activity without P-glycoprotein liability, making it suitable for research on central nervous system penetrant DYRK1A chemical probes [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 100 mg | $1,450 | 10-14 weeks | 10-14 weeks | |
| 200 mg | $1,942 | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor that inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. It exhibits good permeability and cellular activity without P-glycoprotein liability, making it suitable for research on central nervous system penetrant DYRK1A chemical probes [1]. |
| Targets&IC50 | DYRK1A:220 nM, DYRK1A:3 nM (Kd), DYRK1B:56 nM (Kd) |
| In vitro | DYRK1-IN-1 is a potent inhibitor of DYRK1A phosphorylation, achieving inhibition with an IC 50 value of 220 nM and demonstrating an ability to inhibit tau phosphorylation at an IC 50 of 0.59 μM. This compound exhibits good permeability and cellular activity, devoid of P-glycoprotein liability. It also possesses excellent physicochemical characteristics, including high enzymatic potency, favorable aqueous solubility, outstanding kinome selectivity, and robust on-target in vitro inhibition efficacy. In HEK293 cells, DYRK1-IN-1 shows satisfactory cellular activity with an IC 50 of 434 nM, in comparison to an enzymatic IC 50 of 75 nM. |
| In vivo | DYRK1-IN-1 (1 mg/kg; i.v.) exhibits high clearance in Sprague Dawley rats during pharmacokinetic analysis. |
| Molecular Weight | 240.26 |
| Formula | C12H12N6 |
| Cas No. | 2814486-79-6 |
| Smiles | N(C)(C)C=1N=C(C2=C3N(N=C2)N=CC=C3)C=CN1 |
| 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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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
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