2. Metabolic Enzyme/Protease Anti-infection Stem Cell/Wnt PI3K/Akt/mTOR
  3. Ser/Thr Kinase Parasite GSK-3
  4. PfGSK3/PfPK6-IN-1

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.

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PfGSK3/PfPK6-IN-1

PfGSK3/PfPK6-IN-1 Estructura química

No. CAS : 2797225-49-9

Tamaño Precio Stock Cantidad
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
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

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PfGSK3/PfPK6-IN-1 Related Antibodies

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GSK-3 GSK-3α GSK-3β

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Descripciòn

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[1].

In Vitro

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.

PfGSK3/PfPK6-IN-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HepG2
Concentration: 200 nM; 2 μM
Incubation Time: 48 h
Result: Resulted in 102% cell viability at 200 nM.
Resulted in 65% cell viability at 2 μM.
Peso molecular

492.42

Fòrmula

C22H23Cl2N5O2S
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCCCN1CCOCC1)C2=CC=C(NC3=NC=C(Cl)C(C4=CC=C(Cl)S4)=N3)C=C2
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0308 mL 10.1539 mL 20.3079 mL
5 mM 0.4062 mL 2.0308 mL 4.0616 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, 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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 (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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Pureza y Documentación
Referencias

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
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PfGSK3/PfPK6-IN-1 Related Classifications

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.

Keywords:

PfGSK3/PfPK6-IN-12797225-49-9Ser/Thr KinaseParasiteGSK-3Protein Serine-Threonine KinaseGlycogen synthase kinase-3Glycogen synthase kinase 3HepG2 cellshuman kinase targetsPfGSK3liver cellsrecombinant PfGSK3PfPK6Inhibitorinhibitorinhibit

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Nombre del producto:
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