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CLK1-IN-3

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Catalog No. T72039Cas No. 2922550-28-3

Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).

CLK1-IN-3

CLK1-IN-3

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Purity: 99.76%
Catalog No. T72039Cas No. 2922550-28-3
Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$64In StockIn Stock
5 mg$158In StockIn Stock
10 mg$257In StockIn Stock
25 mg$523In StockIn Stock
50 mg$870In StockIn Stock
100 mg$1,390-In Stock
200 mg$1,870-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.76%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).
Targets&IC50
DYRK1A:1521 nM, CLK1:5 nM, CLK2:42 nM, CLK4:108 nM
In vitro
CLK1-IN-3 (compound 10ad) demonstrates anti-tumor potential through dual inhibition of Clk1 and Clk2. At concentrations ranging from 10 μM to 1000 μM, it effectively binds to Clk1 protein and inhibits its degradation dose-dependently. Additionally, CLK1-IN-3 (0-10 μM, 24 h) induces autophagy in Hela, BNLCL.2, and HCT 116 cells and stimulates the degradation of SQSTM1/p62 (autophagy marker)[1].
In vivo
CLK1-IN-3 (0-40 mg/kg, intraperitoneal injection, single dose) significantly inhibits acute liver injury induced by acetaminophen (APAP) in the ALI model, and there is no apparent hepatocyte death observed[1].
CLK1-IN-3 (10 mg/kg; intravenous injection, oral administration, intraperitoneal injection, single dose) exhibits acceptable pharmacokinetic characteristics, with a relatively long half-life (T1/2) of 5.29 hours and an oral bioavailability of 19.5%[1].
Chemical Properties
Molecular Weight430.48
FormulaC24H23FN6O
Cas No.2922550-28-3
SmilesO=C(NC=1C=NC=2NC=C(C=3C=NC=C(F)C3)C2C1)C4=CC=C(C=C4)N5CCN(C)CC5
Relative Density.1.345 g/cm3 at 20℃ (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (127.76 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.65 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
1mg5mg10mg50mg
1 mM2.3230 mL11.6149 mL23.2299 mL116.1494 mL
5 mM0.4646 mL2.3230 mL4.6460 mL23.2299 mL
10 mM0.2323 mL1.1615 mL2.3230 mL11.6149 mL
20 mM0.1161 mL0.5807 mL1.1615 mL5.8075 mL
50 mM0.0465 mL0.2323 mL0.4646 mL2.3230 mL
100 mM0.0232 mL0.1161 mL0.2323 mL1.1615 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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