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Pim1/AKK1-IN-1

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Catalog No. T5093Cas No. 1093222-27-5
Alias MDK-2275, LKB1/AAK1 dual inhibitor

Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.

Pim1/AKK1-IN-1

Pim1/AKK1-IN-1

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Purity: 98.69%
Catalog No. T5093Alias MDK-2275, LKB1/AAK1 dual inhibitorCas No. 1093222-27-5
Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$82In StockIn Stock
2 mg$133In StockIn Stock
5 mg$193In StockIn Stock
10 mg$292In StockIn Stock
25 mg$515In StockIn Stock
50 mg$747In StockIn Stock
100 mg$1,050In StockIn Stock
1 mL x 10 mM (in DMSO)$213In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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:98.69%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Pim1/AKK1-IN-1 AI Summary
Pim1/AKK1-IN-1 exhibits multi-target kinase inhibition and binding affinity. It shows high affinity for human PIM1, TNIK, and MPSK1, with moderate affinities for LKB1 (Kd of 380.0 nM), AAK1 (Kd of 53.0 nM), and CAMK1D. Additionally, it inhibits several protein kinases such as ERK1, JNK3, FLT4, FMS, and CK1gamma1. The compound also demonstrates significant binding to BMP2K, GAK, and STK16. Notably, Pim1/AKK1-IN-1 exhibits antiviral activity against Dengue virus 2, showing low cytotoxicity against Ebolavirus-infected cells, and also inhibits the SARS-CoV-2 3CL-Pro protease and reduces SARS-CoV-2 induced cytotoxicity in VERO-6 cells..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
Targets&IC50
LKB1:380 nM (Kd), Pim1:35 nM (Kd), MST2:75 nM (Kd), AKK1:53 nM (Kd)
SynonymsMDK-2275, LKB1/AAK1 dual inhibitor
Chemical Properties
Molecular Weight339.35
FormulaC20H13N5O
Cas No.1093222-27-5
SmilesO=C(Nc1c[nH]c2ncc(cc12)-c1ccc(cc1)C#N)c1cccnc1
Relative Density.1.42
Storage & Solubility Information
Storagestore at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 15 mg/mL (44.2 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.89 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 mM2.9468 mL14.7341 mL29.4681 mL147.3405 mL
5 mM0.5894 mL2.9468 mL5.8936 mL29.4681 mL
10 mM0.2947 mL1.4734 mL2.9468 mL14.7341 mL
20 mM0.1473 mL0.7367 mL1.4734 mL7.3670 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:
mg/kg
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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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