1-Azakenpaullone
Based on 3 publication(s) in Google Scholar
1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM.
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- Pureté : 99.61%
- CAS No.: 676596-65-9
- Formule: C15H10BrN3O
- Masse moléculaire:328.16
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) 1-Azakenpaullone
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Activité biologique
Description
IC50 & Target
[1]|
GSK-3β 18 nM (IC50) |
CDK1/cyclin B 2 μM (IC50) |
CDK5/p25 4.2 μM (IC50) |
In Vitro
1-Azakenpaullone (2.5 μM, 48 h) stimulates proliferation in irradiated zebrafish lateral line neuromasts[2].
1-Azakenpaullone (3 μM, 48 h) induces the osteoblastic differentiation and mineralization of human human mesenchymal stem cells (MSCs), by activating Wnt signaling[3].
1-Azakenpaullone (30 μM, 24 h) reduces S6K1 phosphorylation in HCC1806 cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:human MSCs
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Concentration:3 µM
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Incubation Time:48 h
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Result:Increased gene expression of osteoblast-specific marker genes (ALP, OC, ON, COL1A1, and OPN).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 676596-65-9
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Appearance Solid
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Masse moléculaire 328.16
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Formule C15H10BrN3O
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=CN=C12)CC3=C2NC4=C3C=C(Br)C=C4
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Synonyms
1-Akp
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (3)
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Journal Impact Factor
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Most Recent
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Stem Cell Rev Rep
Dual-specificity Tyrosine Phosphorylation-regulated Kinase Inhibitor ID-8 Promotes Human Somatic Cell Reprogramming by Activating PDK4 Expression. [Abstract]2022 Aug;18(6):2074-2087. PMID: 35080746 -
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Solvant et solubilité
In Vitro:
DMSO : 200 mg/mL (609.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.67 mg/mL (5.09 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kunick C, et al. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6. [Content Brief]
[2]. Li R, et al. Ionizing Radiation Blocks Hair Cell Regeneration in Zebrafish Lateral Line Neuromasts by Preventing Wnt Signaling. Mol Neurobiol. 2018 Feb;55(2):1639-1651. [Content Brief]
[3]. AlMuraikhi N, et al. Inhibition of GSK-3β Enhances Osteoblast Differentiation of Human Mesenchymal Stem Cells through Wnt Signalling Overexpressing Runx2. Int J Mol Sci. 2023 Apr 12;24(8):7164. [Content Brief]
[4]. Chan MH, et al. Inhibition of glycogen synthase kinase-3 attenuates psychotomimetic effects of ketamine. Schizophr Res. 2012 Apr;136(1-3):96-103. [Content Brief]
[5]. Shin S, et al. Glycogen synthase kinase-3β positively regulates protein synthesis and cell proliferation through the regulation of translation initiation factor 4E-binding protein 1. Oncogene. 2014 Mar 27;33(13):1690-9. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0473 mL | 15.2365 mL | 30.4729 mL | 76.1823 mL |
| 5 mM | 0.6095 mL | 3.0473 mL | 6.0946 mL | 15.2365 mL | |
| 10 mM | 0.3047 mL | 1.5236 mL | 3.0473 mL | 7.6182 mL | |
| 15 mM | 0.2032 mL | 1.0158 mL | 2.0315 mL | 5.0788 mL | |
| 20 mM | 0.1524 mL | 0.7618 mL | 1.5236 mL | 3.8091 mL | |
| 25 mM | 0.1219 mL | 0.6095 mL | 1.2189 mL | 3.0473 mL | |
| 30 mM | 0.1016 mL | 0.5079 mL | 1.0158 mL | 2.5394 mL | |
| 40 mM | 0.0762 mL | 0.3809 mL | 0.7618 mL | 1.9046 mL | |
| 50 mM | 0.0609 mL | 0.3047 mL | 0.6095 mL | 1.5236 mL | |
| 60 mM | 0.0508 mL | 0.2539 mL | 0.5079 mL | 1.2697 mL | |
| 80 mM | 0.0381 mL | 0.1905 mL | 0.3809 mL | 0.9523 mL | |
| 100 mM | 0.0305 mL | 0.1524 mL | 0.3047 mL | 0.7618 mL |
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