PfGSK3/PfPK6-IN-1
Based on 1 Customer Validation
PfGSK3/PfPK6-IN-1 is a dual Plasmodium serine/threonine kinase inhibitor, with an IC50 of 97 nM against PfGSK3 and 8 nM against PfPK6 of Plasmodium falciparum. PfGSK3/PfPK6-IN-1 inhibits the proliferation of blood-stage parasites of Plasmodium falciparum 3D7. PfGSK3/PfPK6-IN-1 shows low cytotoxicity to hepatocytes at a concentration of 200 nM, and reduces cell viability at a concentration of 2 μM. PfGSK3/PfPK6-IN-1 is applicable to malaria-related research.
For research use only. We do not sell to patients.
- Purity: 99.38%
- CAS No.: 2797225-49-9
- Formula: C22H23Cl2N5O2S
- Molecular Weight:492.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Parasite Isoforms
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Biological Activity
PfGSK3/PfPK6-IN-1 (compound 23e) (0-5 μM; 72 h) inhibits the growth of Plasmodium falciparum 3D7 blood-stage parasites in vitro, with an EC50 value of 1400 nM[1].
PfGSK3/PfPK6-IN-1 (200 nM-2 μM; 48 h) exhibits certain cytotoxicity against HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:200 nM; 2 μM
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Incubation Time:48 h
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Result:Resulted in 102% cell viability at 200 nM.
Resulted in 65% cell viability at 2 μM.
Chemical Information
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CAS No. 2797225-49-9
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Appearance Solid
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Molecular Weight 492.42
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Formula C22H23Cl2N5O2S
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Color Light yellow to yellow
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SMILES
O=C(NCCCN1CCOCC1)C2=CC=C(NC3=NC=C(Cl)C(C4=CC=C(Cl)S4)=N3)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (50.77 mM; ultrasonic and warming and heat to 60°C; 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 (5.08 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 (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 2.0308 mL | 10.1539 mL | 20.3079 mL | 50.7697 mL |
| 5 mM | 0.4062 mL | 2.0308 mL | 4.0616 mL | 10.1539 mL | |
| 10 mM | 0.2031 mL | 1.0154 mL | 2.0308 mL | 5.0770 mL | |
| 15 mM | 0.1354 mL | 0.6769 mL | 1.3539 mL | 3.3846 mL | |
| 20 mM | 0.1015 mL | 0.5077 mL | 1.0154 mL | 2.5385 mL | |
| 25 mM | 0.0812 mL | 0.4062 mL | 0.8123 mL | 2.0308 mL | |
| 30 mM | 0.0677 mL | 0.3385 mL | 0.6769 mL | 1.6923 mL | |
| 40 mM | 0.0508 mL | 0.2538 mL | 0.5077 mL | 1.2692 mL | |
| 50 mM | 0.0406 mL | 0.2031 mL | 0.4062 mL | 1.0154 mL |