| Size | Price | Stock | Qty |
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| Other Sizes |
| Targets |
GSK-3β 10.02 μM (IC50)
GSK-3β inhibitor 11 targets glycogen synthase kinase-3β (GSK-3β) as a potent inhibitor with an IC50 of 10.02 μM. GSK-3β is a serine/threonine kinase involved in various cellular processes including glycogen metabolism, neuronal signaling, and inflammation. The compound's inhibition of GSK-3β modulates signaling pathways involved in neurodegenerative diseases. Its mechanism involves competitive inhibition at the ATP-binding site of the kinase. The compound's activity makes it a valuable tool for studying the role of GSK-3β in neurodegeneration. |
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| ln Vitro |
In vitro, GSK-3β inhibitor 11 is a potent inhibitor of GSK-3β with an IC50 of 10.02 μM. The compound demonstrates potential utility in the field of neurodegenerative disease research. It plays a significant role in modulating signaling pathways involved in neurodegenerative diseases. Detailed in vitro characterization data, including enzyme inhibition assays and cellular pathway analyses, are available in the primary literature. The compound can be used to investigate GSK-3β-mediated signaling in neurodegeneration.
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| ln Vivo |
In vivo studies of GSK-3β inhibitor 11 are limited in publicly available literature. The compound can be used in neurodegenerative disease research, suggesting potential applications in animal models of neurodegenerative conditions. GSK-3β inhibitors have been studied in models of Alzheimer's disease, Parkinson's disease, and other neurodegenerative disorders for their neuroprotective effects. However, specific in vivo efficacy data and detailed animal model studies for this compound have not been extensively reported. Further research is needed to establish its in vivo activity profile.
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| Enzyme Assay |
For GSK-3β kinase activity assays, recombinant human GSK-3β enzyme is incubated with appropriate peptide substrates and varying concentrations of GSK-3β inhibitor 11 in the presence of ATP. Kinase activity is measured by quantifying substrate phosphorylation using radioactive [γ-33P]-ATP or by luminescent ADP-Glo assays. IC50 values (10.02 μM) are calculated from dose-response curves. Assays are performed in triplicate with appropriate vehicle controls and reference inhibitors as positive controls.
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| Cell Assay |
For in vitro cellular assays, neuronal cell lines or other relevant cells are cultured in appropriate media under standard conditions (37°C, 5% CO2). GSK-3β inhibitor 11 is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. GSK-3β activity is assessed by measuring phosphorylation levels of GSK-3β substrates such as tau protein by Western blot. Cell viability and neuroprotection can be assessed using standard assays. Each concentration is tested in replicate wells with vehicle controls.
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| Animal Protocol |
For in vivo animal studies of GSK-3β inhibitor 11, no specific published protocols are available. For general in vivo administration of GSK-3β inhibitors in neurodegenerative disease models, compounds are typically formulated in suitable vehicles and administered via intraperitoneal (i.p.) injection, oral gavage, or intravenous (i.v.) injection. Dosing regimens vary by study objective. Behavioral assessments and neuropathological analyses may be performed. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GSK-3β inhibitor 11 are characteristic of a small-molecule kinase inhibitor. The compound has a molecular weight of 393.42, formula C20H15N3O4S, and CAS number 536731-65-4. Purity: 98.02%. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Solubility: soluble in DMSO and other organic solvents. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are not extensively reported in publicly available sources.
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| Toxicity/Toxicokinetics |
According to available safety information, GSK-3β inhibitor 11 is intended for research purposes only and is not for human use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
GSK-3β inhibitor 11 (compound 21) is a potent GSK-3β inhibitor with an IC50 of 10.02 μM. It has a molecular weight of 393.42 and formula C20H15N3O4S. The compound demonstrates potential utility in neurodegenerative disease research. It is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C20H15N3O4S
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|---|---|
| Molecular Weight |
393.42
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| Exact Mass |
393.078
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| CAS # |
536731-65-4
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| PubChem CID |
1579446
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.686
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| LogP |
3.76
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
607
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC(=C1)C2=CSC(=N2)NC(=O)CN3C(=O)C4=CC=CC=C4C3=O
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| InChi Key |
OLPPQDIVHUSKKX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15N3O4S/c1-27-13-6-4-5-12(9-13)16-11-28-20(21-16)22-17(24)10-23-18(25)14-7-2-3-8-15(14)19(23)26/h2-9,11H,10H2,1H3,(H,21,22,24)
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| Chemical Name |
2-(1,3-dioxoisoindol-2-yl)-N-[4-(3-methoxyphenyl)-1,3-thiazol-2-yl]acetamide
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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: 20.83 mg/mL (52.95 mM)
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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 | 2.5418 mL | 12.7091 mL | 25.4181 mL | |
| 5 mM | 0.5084 mL | 2.5418 mL | 5.0836 mL | |
| 10 mM | 0.2542 mL | 1.2709 mL | 2.5418 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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