GSK-3 Inhibitor XIII
Based on 1 Customer Validation
GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM.
For research use only. We do not sell to patients.
- Purity: 98.79%
- CAS No.: 404828-14-4
- Formula: C18H15N5
- Molecular Weight:301.35
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COLO 205 | IC50 |
1.4 μM
Compound: 15
|
Antiproliferative activity against human COLO205 cells assessed as inhibition of thymidine uptake after 96 hrs
Antiproliferative activity against human COLO205 cells assessed as inhibition of thymidine uptake after 96 hrs
|
[PMID: 19320489] |
| DU-145 | IC50 |
7.99 μM
Compound: 3h
|
Antiproliferative activity against human DU145 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human DU145 cells after 48 hrs by CCK8 assay
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[PMID: 30196060] |
| HeLa | IC50 |
0.883 μM
Compound: 3h
|
Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay
Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay
|
[PMID: 30196060] |
| K562 | IC50 |
2.99 μM
Compound: 3h
|
Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
|
[PMID: 30196060] |
| MCF7 | IC50 |
6.16 μM
Compound: 3h
|
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay
|
[PMID: 30196060] |
| MDA-MB-231 | IC50 |
2.88 μM
Compound: 3h
|
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay
|
[PMID: 30196060] |
| MOLT-4 | IC50 |
5.15 μM
Compound: 3h
|
Antiproliferative activity against human MOLT4 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human MOLT4 cells after 48 hrs by CCK8 assay
|
[PMID: 30196060] |
| SK-BR-3 | IC50 |
2.54 μM
Compound: 3h
|
Antiproliferative activity against human SKBR3 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human SKBR3 cells after 48 hrs by CCK8 assay
|
[PMID: 30196060] |
Chemical Information
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CAS No. 404828-14-4
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Appearance Solid
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Molecular Weight 301.35
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Formula C18H15N5
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Color White to off-white
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SMILES
CC1=CC(NC2=C3C=CC=CC3=NC(C4=CC=CC=C4)=N2)=NN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (331.84 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (8.30 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Albert C Pierce, et al. CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor. J Med Chem. 2005 Feb 24;48(4):1278-81. [Content Brief]
[2]. Eduardo Cruz Moraes, et al. Kinase inhibitor profile for human nek1, nek6, and nek7 and analysis of the structural basis for inhibitor specificity. Molecules. 2015 Jan 13;20(1):1176-91. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3184 mL | 16.5920 mL | 33.1840 mL | 82.9600 mL |
| 5 mM | 0.6637 mL | 3.3184 mL | 6.6368 mL | 16.5920 mL | |
| 10 mM | 0.3318 mL | 1.6592 mL | 3.3184 mL | 8.2960 mL | |
| 15 mM | 0.2212 mL | 1.1061 mL | 2.2123 mL | 5.5307 mL | |
| 20 mM | 0.1659 mL | 0.8296 mL | 1.6592 mL | 4.1480 mL | |
| 25 mM | 0.1327 mL | 0.6637 mL | 1.3274 mL | 3.3184 mL | |
| 30 mM | 0.1106 mL | 0.5531 mL | 1.1061 mL | 2.7653 mL | |
| 40 mM | 0.0830 mL | 0.4148 mL | 0.8296 mL | 2.0740 mL | |
| 50 mM | 0.0664 mL | 0.3318 mL | 0.6637 mL | 1.6592 mL | |
| 60 mM | 0.0553 mL | 0.2765 mL | 0.5531 mL | 1.3827 mL | |
| 80 mM | 0.0415 mL | 0.2074 mL | 0.4148 mL | 1.0370 mL | |
| 100 mM | 0.0332 mL | 0.1659 mL | 0.3318 mL | 0.8296 mL |