| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
GSK-3β inhibitor 1 (compound 3a in literature): Glycogen synthase kinase 3β (GSK-3β) (IC₅₀ = 4.19 nM) [1]
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|---|---|
| ln Vitro |
1. In the enzyme activity assay of GSK-3β, GSK-3β inhibitor 1 exhibited potent inhibitory activity against GSK-3β with an IC₅₀ value of 4.19 nM, showing high targeting ability to the kinase [1]
2. In the leucocyte toxicity assay, GSK-3β inhibitor 1 showed no significant toxic effect on leucocytes at a concentration of 10 μM, indicating good biocompatibility with normal blood cells [1] 3. In the cytotoxicity assay against A549 lung cancer cells, GSK-3β inhibitor 1 presented moderate cytotoxicity, showing potential anticancer activity to a certain extent [1] |
| ln Vivo |
1. In obese streptozotocin-treated rats (an experimental diabetes model), administration of GSK-3β inhibitor 1 at a dose of 50 mg/kg body weight demonstrated high antidiabetic efficacy; specifically, the compound significantly improved the glucose tolerance of the model rats, suggesting its potential value for diabetes treatment [1]
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| Enzyme Assay |
1. First, the purified GSK-3β enzyme was prepared for the activity detection system; then, serial concentrations of GSK-3β inhibitor 1 were added to the reaction system containing the specific substrate of GSK-3β, and the mixture was incubated under appropriate reaction conditions (temperature and time consistent with the enzyme's optimal activity requirements); after the reaction was terminated, the enzymatic activity of GSK-3β was detected by corresponding detection methods, and the data were collected and analyzed to calculate the IC₅₀ value of the compound for GSK-3β inhibition [1]
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| Cell Assay |
1. Leucocyte toxicity test: Isolate and culture leucocytes in an appropriate culture system; after the cells reached a stable state, add GSK-3β inhibitor 1 to the culture medium to make the final concentration reach 10 μM, and set a blank control group without the compound; after a certain period of incubation, detect the viability of leucocytes using relevant cell activity detection methods to evaluate the toxic effect of the compound on normal leucocytes [1]
2. A549 cell cytotoxicity test: Inoculate A549 lung cancer cells into the corresponding culture plate and culture them until they enter the logarithmic growth phase; add different concentrations of GSK-3β inhibitor 1 to the cell culture system, set multiple replicate wells and a control group; after continuous incubation for a specified time, use a suitable cell viability or cytotoxicity detection method to assess the inhibitory effect of the compound on A549 cell proliferation and its cytotoxicity [1] |
| Animal Protocol |
1. First, establish the obese streptozotocin-treated rat model of experimental diabetes; then prepare GSK-3β inhibitor 1 into the corresponding administration preparation (the specific dissolution formula and dosage form were not detailed in the literature); administer the compound to the model rats at a dose of 50 mg/kg body weight,after the administration, perform the glucose tolerance test on the rats at the specified time point to evaluate the antidiabetic efficacy of the compound [1]
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| Toxicity/Toxicokinetics |
1. In vitro experiments showed that 10 μM GSK-3β inhibitor 1 had no significant toxic effect on leukocytes; it showed moderate cytotoxicity to A549 lung cancer cells, but no more detailed toxicity data were provided [1].
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| References | |
| Additional Infomation |
1. GSK-3β inhibitor 1 belongs to the class of 3-aryl-2-oxindole derivatives and is a novel GSK-3β inhibitor with good biological activity[1]. 2. This compound is a lead compound worthy of further structural optimization and has potential application prospects in the treatment of diabetes and cancer (GSK-3β is a key molecular target of these diseases, and inhibiting GSK-3β can exert anti-diabetic and anti-cancer effects)[1]. 3. GSK-3β is a widely studied molecular target of various diseases (including Alzheimer's disease, cancer and diabetes), and inhibiting its activity is an attractive therapeutic strategy for related diseases[1].
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| Molecular Formula |
C14H10N2O
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|---|---|
| Molecular Weight |
222.242
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| Exact Mass |
222.079
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| CAS # |
187325-53-7
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| PubChem CID |
5796182
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| Appearance |
Yellow to orange solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
337
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1NC2=CC=CC=C2/C1=C/C3=NC=CC=C3
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| InChi Key |
YKQONSWBHGBDSB-XFXZXTDPSA-N
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| InChi Code |
InChI=1S/C14H10N2O/c17-14-12(9-10-5-3-4-8-15-10)11-6-1-2-7-13(11)16-14/h1-9H,(H,16,17)/b12-9-
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| Chemical Name |
(3Z)-3-(pyridin-2-ylmethylidene)-1H-indol-2-one
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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)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~149.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4996 mL | 22.4982 mL | 44.9964 mL | |
| 5 mM | 0.8999 mL | 4.4996 mL | 8.9993 mL | |
| 10 mM | 0.4500 mL | 2.2498 mL | 4.4996 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.
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