| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
(E/Z)-GSK-3β inhibitor 1 targets glycogen synthase kinase 3β (GSK-3β), a serine/threonine protein kinase involved in glycogen metabolism, Wnt signaling, and insulin signaling. GSK-3β inhibition has been shown to improve insulin sensitivity and glucose metabolism, making it a therapeutic target for diabetes. The compound has an IC50 of 4.9 nM for GSK-3β.
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| ln Vitro |
(E/Z)-GSK-3β inhibitor 1 demonstrates potent in vitro activity against GSK-3β with an IC50 of 4.9 nM. It exhibits high antidiabetic efficacy in vitro. As a GSK-3β inhibitor, it is expected to modulate glycogen metabolism and insulin signaling pathways. The compound is used in research to study the role of GSK-3β in diabetes and related metabolic disorders.
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| ln Vivo |
(E/Z)-GSK-3β inhibitor 1 demonstrates in vivo antidiabetic efficacy. As a GSK-3β inhibitor with an IC50 of 4.9 nM, it is expected to improve insulin sensitivity and glucose metabolism in animal models of diabetes. The compound may be used to study the therapeutic potential of GSK-3β inhibition for diabetes and related metabolic disorders.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cell-based) assay for (E/Z)-GSK-3β inhibitor 1 involves assessing its inhibition of GSK-3β kinase activity. Recombinant GSK-3β is incubated with the compound, ATP, and a substrate peptide. Kinase activity is measured by detecting phosphorylated substrate using techniques such as radiometric assays or fluorescence-based assays. The IC50 value of 4.9 nM is determined from dose-response curves.
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| Cell Assay |
The in vitro cell-based assay for (E/Z)-GSK-3β inhibitor 1 involves treating cells with the compound and measuring GSK-3β-dependent signaling and functional responses. Cells are treated with the compound, and downstream phosphorylation of GSK-3β substrates (such as glycogen synthase) is assessed by Western blotting. Insulin signaling and glucose uptake may also be measured to evaluate the compound’s antidiabetic effects.
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| Animal Protocol |
In vivo animal experiments for (E/Z)-GSK-3β inhibitor 1 are conducted in diabetic animal models to evaluate its antidiabetic efficacy. Diabetic animals are administered the compound via appropriate routes, and blood glucose levels, insulin sensitivity, and glucose tolerance are measured. The compound’s ability to inhibit GSK-3β and improve metabolic parameters is assessed.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of (E/Z)-GSK-3β inhibitor 1 are not extensively reported. The compound has a molecular weight of 222.24 g/mol and a molecular formula of C14H10N2O. Further pharmacokinetic studies are needed to determine its half-life, bioavailability, and tissue distribution. The compound is typically used for research purposes only.
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| Toxicity/Toxicokinetics |
Toxicological data for (E/Z)-GSK-3β inhibitor 1 are not extensively documented. As a research compound, its safety profile is evaluated in standard cytotoxicity and acute toxicity assays. The compound is classified for research use only and is not intended for human therapeutic use. Comprehensive toxicological characterization would be required prior to any clinical development.
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| References | |
| Additional Infomation |
(E/Z)-GSK-3β inhibitor 1 (CAS 3367-88-2) is a racemic compound of (E)- and (Z)-GSK-3β inhibitor 1 isomers. GSK-3β inhibitor 1 (compound 3a) is a GSK-3β inhibitor with an IC50 of 4.9 nM and demonstrates high antidiabetic efficacy. It has a molecular weight of 222.24 g/mol and a formula of C14H10N2O. It is used in diabetes research and is not approved for clinical use.
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| Molecular Formula |
C14H10N2O
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|---|---|
| Molecular Weight |
222.24
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| Exact Mass |
222.079
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| CAS # |
3367-88-2
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| Related CAS # |
GSK-3β inhibitor 1;187325-53-7
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| PubChem CID |
5796182
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| Appearance |
Orange to red solid powder
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| Density |
1.291g/cm3
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| Boiling Point |
457.2ºC at 760 mmHg
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| Flash Point |
230.3ºC
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| Index of Refraction |
1.693
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| LogP |
2.712
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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 |
C1=CC=C2C(=C1)/C(=C/C3=CC=CC=N3)/C(=O)N2
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 50 mg/mL (224.98 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (11.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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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