| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GSK-3β inhibitor 28 (Compound 7f) showed strong inhibitory activity against SW480, MDA-MB-231 and A549 cells, with IC50 values of 14.58, 14.61 and 19.15 μM, respectively, while its activity against MoLM13 cells (IC50 = 25.75 μM) and HepG2 cells (IC50 = 51.51 μM) was weak [1]. GSK-3β inhibitor 28 (1 μM) showed good selectivity against most kinases (MAPK, EGFR, Src), except for GSK-3α, and showed only a moderate inhibition rate (58.0%) against GSK-3α [1]. GSK-3β inhibitor 28 (0.78-25 μM, 72 h) showed IC50 values greater than 25 μM for both LX-2 (hepatic stellate cells) and MIHA (normal hepatocytes) [1]. GSK-3β inhibitor 28 (5-20 μM, 24 h) inhibited the migration of SW480 cells and reduced the number of colonies [1]. GSK-3β inhibitor 28 (5-20 μM, 24 h) induced apoptosis in SW480 cells and arrested them in the G1 phase [1]. GSK-3β inhibitor 28 (10-20 μM, 72 h) upregulated the expression of p-GSK-3β in SW480 cells and downregulated the expression of p-NF-κB, P65, C-myc, Cyclin D1 and XIAP proteins [1].
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|---|---|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: SW480 cells Tested Concentrations: 5, 10 and 20 μM Incubation Duration: 24 h Experimental Results: Increased proportion of cells in G1 phase. Decreased proportions in S and G2 phases. |
| Molecular Formula |
C21H16CLN3O3S
|
|---|---|
| Molecular Weight |
425.89
|
| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3480 mL | 11.7401 mL | 23.4802 mL | |
| 5 mM | 0.4696 mL | 2.3480 mL | 4.6960 mL | |
| 10 mM | 0.2348 mL | 1.1740 mL | 2.3480 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.