1. JAK/STAT Signaling
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  3. Pim1/AAK1-IN-1

Pim1/AAK1-IN-1  (Synonyms: LKB1/AAK1 dual inhibitor)

Cat. No.: HY-10371 Pureté: 98.40%
Instruction de manipulation Technical Support

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

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Pim1/AAK1-IN-1

Pim1/AAK1-IN-1 Chemical Structure

CAS No. : 1093222-27-5

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
50 mg En stock
100 mg   Obtenir un devis  
200 mg   Obtenir un devis  

* Veuillez sélectionner la quantité avant d'ajouter des articles.

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Based on 12 publication(s) in Google Scholar

Other Forms of Pim1/AAK1-IN-1:

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Description

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

IC50 & Target

PIM1

 

Cellular Effect
Cell Line Type Value Description References
Huh-7 CC50
>10 μM
Compound: 1
Cytotoxicity against human HuH7 cells infected with Ebolavirus Kikwit isolate after 48 hrs by Celltiter-glo reagent based luminescence assay
Cytotoxicity against human HuH7 cells infected with Ebolavirus Kikwit isolate after 48 hrs by Celltiter-glo reagent based luminescence assay
[PMID: 31136173]
Huh-7 CC50
>50 μM
Compound: 1
Cytotoxicity against human HuH7 cells infected with DENV2 New Guinea C by microplate alamar blue assay
Cytotoxicity against human HuH7 cells infected with DENV2 New Guinea C by microplate alamar blue assay
[PMID: 31136173]
Huh-7 CC50
>50 μM
Compound: 7
Cytotoxicity against human Huh-7 cells
Cytotoxicity against human Huh-7 cells
[PMID: 38377825]
Vero EC50
>10 μM
Compound: 1
Antiviral activity against Ebolavirus Kikwit isolate infected in African green monkey Vero cells assessed as plaque reduction after 48 hrs by neutral red-staining based assay
Antiviral activity against Ebolavirus Kikwit isolate infected in African green monkey Vero cells assessed as plaque reduction after 48 hrs by neutral red-staining based assay
[PMID: 31136173]
Vero C1008 CC50
>50 μM
Compound: 109
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 96 hrs by MTS assay
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 96 hrs by MTS assay
[PMID: 37981443]
In Vitro

Pim1/AAK1-IN-1 is multi-kinase inhibitor, and has Kd of 380 nM against LKB1 and 53 nM against AAK1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Masse moléculaire

339.35

Formule

C20H13N5O

CAS No.
Appearance

Solid

Color

White to gray

SMILES

N#CC1=CC=C(C2=CN=C3C(C(NC(C4=CC=CN=C4)=O)=CN3)=C2)C=C1

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (147.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9468 mL 14.7340 mL 29.4681 mL
5 mM 0.5894 mL 2.9468 mL 5.8936 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9468 mL 14.7341 mL 29.4681 mL 73.6703 mL
5 mM 0.5894 mL 2.9468 mL 5.8936 mL 14.7341 mL
10 mM 0.2947 mL 1.4734 mL 2.9468 mL 7.3670 mL
15 mM 0.1965 mL 0.9823 mL 1.9645 mL 4.9114 mL
20 mM 0.1473 mL 0.7367 mL 1.4734 mL 3.6835 mL
25 mM 0.1179 mL 0.5894 mL 1.1787 mL 2.9468 mL
30 mM 0.0982 mL 0.4911 mL 0.9823 mL 2.4557 mL
40 mM 0.0737 mL 0.3684 mL 0.7367 mL 1.8418 mL
50 mM 0.0589 mL 0.2947 mL 0.5894 mL 1.4734 mL
60 mM 0.0491 mL 0.2456 mL 0.4911 mL 1.2278 mL
80 mM 0.0368 mL 0.1842 mL 0.3684 mL 0.9209 mL
100 mM 0.0295 mL 0.1473 mL 0.2947 mL 0.7367 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Nom du produit:
Pim1/AAK1-IN-1
Cat. No.:
HY-10371
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