| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
GSK3-IN-4 targets both isoforms of glycogen synthase kinase 3, GSK-3α and GSK-3β, as a potent inhibitor. GSK-3 is a key regulator of various cellular processes including metabolism, cell differentiation, and apoptosis. By inhibiting GSK-3 activity, GSK3-IN-4 modulates downstream signaling pathways including Wnt/β-catenin and insulin signaling. The compound's inhibition of both GSK-3 isoforms makes it a valuable tool for studying the overlapping and distinct functions of these kinases in psychiatric disorders and other conditions.
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| ln Vitro |
In vitro, GSK3-IN-4 is a potent GSK-3 inhibitor with IC50 values of 0.101-1 μM for GSK-3α and GSK-3β in Caliper assays. As a potent GSK3 inhibitor, it modulates key cellular processes including metabolism, cell differentiation, and apoptosis. The compound's activity against both GSK-3 isoforms makes it a valuable research tool for studying the role of GSK-3 in various biological pathways. Detailed in vitro characterization data, including enzyme inhibition assays and cellular pathway analyses, are available in the primary literature.
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| ln Vivo |
In vivo studies of GSK3-IN-4 are limited in publicly available literature. As a potent GSK-3 inhibitor, it may have potential for in vivo investigations of psychiatric disorders and other conditions where GSK-3 dysregulation is implicated. GSK-3 inhibitors have been studied in animal models of mood disorders, schizophrenia, and neurodegenerative diseases. However, specific in vivo efficacy data and detailed animal model studies for this particular compound are not extensively reported. Further research is needed to establish its in vivo activity profile and therapeutic potential.
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| Enzyme Assay |
For GSK-3 kinase activity assays using the Caliper assay format, recombinant human GSK-3α or GSK-3β enzymes are incubated with fluorescently labeled peptide substrates and varying concentrations of GSK3-IN-4 in the presence of ATP. Following incubation, the reaction mixture is analyzed by capillary electrophoresis using a Caliper LabChip system to separate phosphorylated substrate from unphosphorylated substrate. The ratio of phosphorylated to total substrate is measured, and IC50 values 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, cell lines of interest are cultured in appropriate media under standard conditions (37°C, 5% CO2). GSK3-IN-4 is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. GSK-3 activity is assessed by measuring phosphorylation levels of GSK-3 substrates such as glycogen synthase or β-catenin by Western blot. Cell viability and proliferation can be assessed using MTT or CCK-8 assays. For psychiatric disorder research, relevant neuronal cell models may be used. Each concentration is tested in replicate wells with vehicle controls.
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| Animal Protocol |
For in vivo animal studies of GSK3-IN-4, no specific published protocols are available. For general in vivo administration of GSK-3 inhibitors, compounds are typically formulated in suitable vehicles such as DMSO/PEG300/saline or CMC-Na suspensions and administered via oral gavage, intraperitoneal (i.p.) injection, or intravenous (i.v.) injection. Dosing regimens vary by study objective. For psychiatric disorder models, behavioral assessments may be performed. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GSK3-IN-4 are characteristic of a small-molecule GSK-3 inhibitor. The compound has a molecular weight of 308.38, formula C18H20N4O, and CAS number 748145-19-9. Purity: 98.33%. Appearance: white solid. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Solubility: DMSO 50 mg/mL (162.14 mM) with sonication. Density: 1.28 g/cm³ (predicted). 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, GSK3-IN-4 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 |
GSK3-IN-4 (compound 0715) is a potent GSK-3 inhibitor with IC50 values of 0.101-1 μM for GSK-3α and GSK-3β. It has a molecular weight of 308.38 and formula C18H20N4O. The compound can be used for psychiatric disorder research. GSK-3 is a key regulator of metabolism, cell differentiation, and apoptosis. GSK3-IN-4 is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C18H20N4O
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|---|---|
| Molecular Weight |
308.38
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| Exact Mass |
308.163
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| CAS # |
748145-19-9
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| PubChem CID |
3809721
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
541
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C2C(C3=C(CC(CC3=O)(C)C)NC2=NN1)C4=CN=CC=C4
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| InChi Key |
GKEYTFDKZJPLCV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20N4O/c1-10-14-15(11-5-4-6-19-9-11)16-12(20-17(14)22-21-10)7-18(2,3)8-13(16)23/h4-6,9,15H,7-8H2,1-3H3,(H2,20,21,22)
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| Chemical Name |
3,7,7-trimethyl-4-pyridin-3-yl-4,6,8,9-tetrahydro-2H-pyrazolo[3,4-b]quinolin-5-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) |
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 | 3.2428 mL | 16.2138 mL | 32.4275 mL | |
| 5 mM | 0.6486 mL | 3.2428 mL | 6.4855 mL | |
| 10 mM | 0.3243 mL | 1.6214 mL | 3.2428 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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