| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
GSK3β Amyloid-β oligomers
Cu(II)GTSM targets GSK3β as a significant inhibitor. By inhibiting GSK3β activity, the compound reduces phosphorylation of tau protein. It also suppresses levels of neurotoxic amyloid β-trimers, which are implicated in Alzheimer's disease pathology. The compound's mechanism involves copper-mediated modulation of kinase activity and protein aggregation pathways. It has shown neuroprotective and cytotoxic effects depending on concentration and context, making it a valuable tool in models of Alzheimer's disease and ALS. |
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| ln Vitro |
Cu(II)GTSM causes GSK3β phosphorylation at serine-9 (ser9) via its upstream kinase, protein kinase B (Akt), and aslo increases the phosphorylation of the associated extracellular signal-related kinase 1/2 (ERK1/2) in SH -SY5Y cells. Tau phosphorylation at ser404 was lowered in CuII(gtsm)-treated cells by 64%[2].
In vitro, Cu(II)GTSM (25, 50, 100 nM, 18 hours) was tested in PC12 cells treated with NGF for 48 hours. MTT assays showed that at 25 and 50 nM, there was a small but significant loss of MTT reduction; LDH assays showed that at 100 nM, LDH release actually decreased slightly but significantly. The compound significantly inhibits GSK3β activity and suppresses levels of neurotoxic amyloid β-trimers and phosphorylated tau. These activities make it a valuable tool for studying neurodegenerative disease mechanisms. |
| ln Vivo |
Cu(II)GTSM can cure cognitive impairments in APP/PS1 transgenic AD mice and reduce brain Aβ trimer levels in AD animals[2].
In vivo, Cu(II)GTSM (10 mg/kg) treatment of Alzheimer's disease (AD) mice reduces brain Aβ trimer levels and restores cognitive abilities to levels expected of healthy, cognitively normal mice. The compound reverses cognitive deficits in APP/PS1 transgenic AD mice. It is used in biomedical research to study copper homeostasis, oxidative stress, and neurodegenerative disease mechanisms. These findings support the potential of Cu(II)GTSM for studying Alzheimer's disease and related neurodegenerative conditions. |
| Enzyme Assay |
For GSK3β kinase activity assays, recombinant human GSK3β enzyme is incubated with appropriate peptide substrates and varying concentrations of Cu(II)GTSM in the presence of ATP. Kinase activity is measured by quantifying substrate phosphorylation using radioactive or luminescent methods. IC50 values are calculated from dose-response curves. For amyloid β aggregation assays, the compound's ability to suppress neurotoxic amyloid β-trimer formation can be assessed using Thioflavin T fluorescence or electron microscopy. Assays are performed in triplicate with appropriate vehicle controls.
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| Cell Assay |
For in vitro cellular assays, PC12 cells or other neuronal cell lines are cultured in appropriate media under standard conditions (37°C, 5% CO2). Cu(II)GTSM is dissolved in DMSO and diluted in culture medium to desired concentrations (e.g., 25, 50, 100 nM). Cells are treated with compound for specified durations (e.g., 18 hours). Cell viability is assessed using MTT assays, and cell membrane integrity is assessed using LDH release assays. Amyloid β and phosphorylated tau levels can be measured by Western blot or ELISA. Each concentration is tested in replicate wells with vehicle controls.
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| Animal Protocol |
Animal/Disease Models: AD mice (K670N, M671L; 5-6 months old)[2]
Doses: 10 mg/kg Route of Administration: Daily; po Experimental Results: Restores cognitive performance of the AD mice to levels expected for healthy, cognitively normal mice. For in vivo animal studies, Cu(II)GTSM is typically formulated in suitable vehicles and administered via intraperitoneal (i.p.) injection at doses such as 10 mg/kg. In Alzheimer's disease models such as APP/PS1 transgenic mice, animals are treated with compound and cognitive function is assessed using behavioral tests (e.g., Morris water maze). Brain Aβ trimer levels and phosphorylated tau levels are measured by biochemical analysis. All procedures must follow institutional animal care and use committee guidelines. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cu(II)GTSM are characteristic of a copper-containing complex. The compound has a molecular weight of 293.86, formula C6H10CuN6S2, and CAS number 68341-14-0. Purity: 99.21%. Appearance: brown solid. Storage: powder at -20°C for 3 years; at 4°C for 2 years. Solubility: DMSO 60 mg/mL with ultrasonic. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are reported in the primary literature.
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| Toxicity/Toxicokinetics |
According to available safety information, Cu(II)GTSM 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 |
Cu(II)GTSM is a cell-permeable copper complex that significantly inhibits GSK3β activity and suppresses neurotoxic amyloid β-trimers and phosphorylated tau. It reverses cognitive deficits in Alzheimer's disease mouse models at 10 mg/kg. It has a molecular weight of 293.86 and formula C6H10CuN6S2. It is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C6H10CUN6S2
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| Molecular Weight |
293.859797954559
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| Exact Mass |
292.97
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| CAS # |
68341-14-0
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| PubChem CID |
22864880
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| Appearance |
Light brown to brown solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
15
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| Complexity |
247
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N(C1=N[N]2=CC=[N]3N=C(S[Cu+2]32S1)NC)C
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| InChi Key |
MNLAJDKBIQOELG-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C6H12N6S2.Cu/c1-7-5(13)11-9-3-4-10-12-6(14)8-2;/h3-4H,1-2H3,(H2,7,11,13)(H2,8,12,14);/p-2
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| Chemical Name |
copper;N-methyl-N'-[2-[[methylamino(sulfido)methylidene]hydrazinylidene]ethylideneamino]carbamimidothioate
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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 | 3.4030 mL | 17.0149 mL | 34.0298 mL | |
| 5 mM | 0.6806 mL | 3.4030 mL | 6.8060 mL | |
| 10 mM | 0.3403 mL | 1.7015 mL | 3.4030 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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